Drug delivery systems for instillation in the urinary bladder comprising active pharmaceutical ingredients

Abstract

The present invention relates to a composition, especially to a pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder.

Description

[0001] DRUG DELIVERY SYSTEMS FOR INSTILLATION IN THE URINARY BLADDER COMPRISING ACTIVE PHARMACEUTICAL INGREDIENTS

[0002] The present invention relates to the medical therapeutic area of prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, particularly diseases and / or dysfunctions of the urinary bladder.

[0003] In particular, the present invention relates to a composition, especially to a pharmaceutical composition, which is in particular suitable for the prophylactic and / or therapeutic treatment of preferably inflammatory diseases of the urogenital tract, especially of inflammatory diseases of the bladder, preferably of cystitis, and respective uses thereof as well as methods related thereto.

[0004] Further, the present invention relates to a drug delivery system (DDS), particularly a sustained-release drug delivery system (SR-DDS), preferably an in s / Yu-forming implant (ISFI ), as well as respective uses thereof and methods related thereto.

[0005] Also further, the present invention relates to an application device, in particular syringe, preferably ready-to-use piston syringe, as well as a packaging unit and a kit- of-parts, each related to the composition according to the invention.

[0006] Finally, the present invention relates to an active agent for intravesical application into the urinary bladder as well as respective uses thereof and methods related thereto, and to the use of a composition, especially pharmaceutical composition, for intravesical application of at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API) into the urinary bladder.

[0007] Urologic diseases or dysfunctions can affect a range of organs including the bladder, the urethra, the kidneys and / or the reproductive organs. Among the most common urologic diseases or dysfunctions for which human patients seek treatment are urinary tract infections and urinary incontinence, specifically caused as a result of neurogenic dysfunctions.

[0008] Infections and inflammatory diseases of the urogenital tract, which relate in particular to the urinary tract, are particularly widespread in the population. Due to their anatomical conditions, women are more frequently related to these than men. Infections of the urinary tract are caused by pathogens. If the urinary bladder is related to the infection, the infection is referred to as cystitis, which is caused by bacteria in particular.

[0009] In most cases, a urinary tract infection occurs through the ascent of pathogens via the urethra, which is also referred to as an ascending infection. The pathogens that cause urinary tract infections are gram-negative bacteria or pathogens in particular, wherein Escherichia coli is the most common pathogen causing urinary tract infections, accounting for 80 % of cases. However, urinary tract infections can also be caused by gram-positive cocci, mycoplasma, ureaplasma, yeasts, chlamydia, viruses and the like.

[0010] In general, the infection often occurs when pathogens reach the external urethral opening and travel from there up the urethra into the bladder, where they can lead to cystitis, for example.

[0011] A further large field is interstitial cystitis, especially since this affects a large circle of individuals. Interstitial cystitis is sometimes also defined as "chronic idiopathic bladder inflammation of uncertain genesis". Interstitial cystitis is difficult to diagnose, and its treatment options are regarded as challenging. Interstitial cystitis is also subsumed under the expression "painful bladder syndrome". With respect to etiology, there are sometimes still no completely reliable findings. In this regard, various hypotheses are under discussion, such as a release of inflammatory substances due to mast cell activation owing to different stimuli; occult infections; increase in the permeability of the bladder wall for toxic substances; immunological processes and also a hypersensitivity of nerve fibers with increase in nerve fiber density. Besides urination record and pain diary with VAS (visual analog scale) and besides bacteriological testing to rule out a urinary tract infection and urine cystology to rule out a carcinoma, the diagnostic spectrum for interstitial cystitis encompasses cystoscopy to be carried out under anesthesia with or without associated biopsy. Interstitial cystitis is a chronic inflammatory disease of the bladder without any detectable bacteria in the urine. Consequently, what is concerned here is cystitis of nonbacterial origin. It is a disease which has not been fully explained to date, and patients often suffer worse from said disease than from a tumor disease. The US National Health Institute has also classified interstitial cystitis as a higher-priority disease. Quality of life can be extremely impaired by severe urinary urgency, frequent urination during the day and at night, and increasing pain. It becomes apparent that complications associated with urinary tract infections are extensive and can sometimes be very serious, or at least distressing for the affected individual: for example, an infection of the urethra itself causes pain when urinating or triggers an unpleasant itching sensation. In addition, the flow of urine is often reduced.

[0012] On the other hand, as an example for neurogenic dysfunctions of the urinary tract, neurogenic bladder dysfunction (nBFS) or neurogenic bladder emptying disorders represent a pathological situation of the urinary bladder and the anatomical structures involved in urine storage and excretion that often requires therapy. Neurogenic bladder dysfunctions are particularly those dysfunctions of the urinary bladder or the relevant anatomical structures that occur as a result of a malfunction or injury of the nervous system, for example as a result of spinal cord injury, spina bifida ("open back"), diabetes, multiple sclerosis, stroke or Parkinson's disease. The suffering of patients associated with urinary bladder dysfunction is sometimes very great, especially since the quality of life, which is often already limited, is further worsened by the complaints associated with the dysfunction.

[0013] In general, neurogenic bladder dysfunction (nBFS) is thus defined as a disorder of urine storage or urination caused in particular by neurological changes or injuries in the area of the spinal cord or in the sections of the brain relevant to bladder function or in the area of the periphery, whereby normal nervous signal transmission to control the urinary bladder is often impaired or impeded. As a result of the underlying neurological damage, the natural function of the urinary bladder is disturbed with regard to its functional states, namely a (urinary) filling phase on the one hand and a (urinary) emptying or micturition phase on the other. The physiological process of bladder filling and emptying can even be impaired or prevented at several levels.

[0014] As a result of the neurological dysfunction, detrusor hyperactivity and / or detrusorsphincter dyssynergy is often present in neurogenic bladder dysfunction (nBFS). This is often accompanied by a disturbance in the interplay or coordination of the anatomical structures relevant to natural bladder function.

[0015] The detrusor (musculus detrusor vesicae or "expeller of the bladder") is a powerful muscle system that surrounds or forms part of the urinary bladder. The detrusor is a smooth muscle that plays a major role in a physiological situation during micturition or bladder emptying and thus urine expulsion. In this process, signals from the parasympathetic nervous system cause the muscle system to tense, putting the bladder contents under pressure. In addition, the detrusor is influenced by an intrinsic nerve plexus, which is located in the bladder wall and adjusts the tone to the filling state of the urinary bladder.

[0016] In the pathological situation, detrusor hyperactivity is often present in neurogenic bladder dysfunction, which in this context is also referred to as neurogenic detrusor overactivity (NDO). Detrusor hyperactivity associated with a relevant underlying neurological disease is accompanied in particular by pollakiuria, nocturia and excessive urge symptoms.

[0017] In detrusor-sphincter dyssynergia (DSD), the interaction of the anatomical structures involved in bladder emptying is also disturbed, whereby detrusor overactivity is confronted with spastic dysfunction of the pelvic floor muscles or the external bladder sphincter, leading to obstruction of the bladder outlet with simultaneous micturition effort. Typical of detrusor-sphincter dyssynergia is a frequently interrupted urinary stream and difficulty in initiating micturition. In addition, pollakiuria and residual urine formation are often present.

[0018] In addition to the aforementioned symptoms, neurogenic bladder dysfunction is often associated with high intravesical pressures, i.e., excessive pressure is built up in the urinary bladder due to detrusor hyperactivity or detrusor-sphincter dyssynergia. Last but not least, this also poses a risk to the upper urinary tract, so excessively high intravesical pressures are often associated with or cause kidney damage.

[0019] In the light of the above, there is thus a great need for the provision of therapeutic concepts which, in the presence of a neurogenic bladder dysfunction, lead to a normalization or improvement of the bladder function or to a reduction of the symptoms, both with regard to the problems with urination and the present high pressures in the urinary bladder. In addition to improving micturition, a major goal is also to reduce intrinsic pressure in order to prevent any kidney damage or the like.

[0020] In this context, the therapy of neurogenic bladder dysfunction pursues several goals, in particular the protection of the upper urinary tract and kidney function, the improvement of the continence situation, the restoration or improvement of the function of the lower urinary tract and, last but not least, the enhancement of the quality of life. In addition to conservative measures, such as regular exercise, targeted bladder training or similar, pharmacotherapeutic measures are also used to treat neurogenic bladder dysfunction. For example, based on minimally invasive methods, an injection with botulinum toxin into the bladder wall can be performed to reduce detrusor activity. However, the administration is challenging, as the active substance has to be injected into the bladder wall in a relatively complex manner. Minimally invasive methods are also used in the form of sacral neuromodulation, in which a pacemaker is implanted in the upper buttock area and delivers weak electrical impulses to the sacral nerves via an electrode. However, the field of application is limited with regard to the underlying diseases. In addition, this is a not insignificant surgical procedure, which is associated with further risks.

[0021] In addition, pharmacological therapies based on anticholinergics are used. In this context, particular reference is made to the administration of oxybutynin or oxybutynin hydrochloride, trospium chloride, propiverine, tolterodine or the like. More specifically, there are systemic and local options available for NDO therapy, with oxybutynin hydrochloride being the most commonly used active agent. Oxybutynin (also known as 4-diethylaminobut-2-inyl-2-cyclohexyl-2-hydroxy-2-phenylethanoate) or oxybutynin hydrochloride is an anticholinergic agent used for the treatment of bladder dysfunction, in particular bladder dysfunction associated with detrusor hyperactivity and / or detrusor-sphincter dyssynergia. It can be administered orally (Ditropan®). However, this method is associated with adverse effects such as constipation, dry mouth, dizziness, and facial flushing, which often lead to treatment interruption.

[0022] Further, systemic administration of anticholinergics is disadvantageous in so far as the administered active substance is metabolized during its first passage in the gastrointestinal tract or in the liver (so-called first pass metabolism), whereby sometimes non-active metabolites are formed, so that the bioavailability at the site of action is lower or the amount of active substance at the site of action is difficult to adjust or prescribe. Consequently, systemic dosage forms for patients sometimes cannot be adequately adjusted.

[0023] An alternative option to oral systemic application is intravesical, local application of an active agent, which has a lower risk of side effects during treatment. The market- available oxybutynin-based drug Vesoxx® is currently the only product that provides an alternative to oral administration. The intravesical application results in higher compliance, but the urinary bladder remains a challenging site for application. Due to regular urination, any liquid formulation applied is flushed out of the bladder, necessitating repeated catheterization and medication application, often up to five times per day. On the other hand, formulations need to be somewhat liquid to be able to be instilled into the urinary bladder, which on the contrary is associated with a higher risk of voiding and early elimination of a drug composition. Next to these application related challenges, the urinary bladder as application site also has a varying pH between 4 and 8, depending on the urine, as well as a frequently different composition of its salt and amino acid content. Both these aspects are highly dependent on an individual’s diet and thus not controllable from the outside.

[0024] For the aforementioned reasons, effective intravesical application of drugs remains particularly challenging. This applies even more if a prolonged drug effect is envisioned.

[0025] Sustained drug release is a measure that is considered in cases where prolonged action of a drug is desired. However, for the urinary tract, one of the main challenges faced by pharmaceutical dosage forms with the aim of a sustained release is - as for all intravesically applied formulations - the risk of voiding of the bladder causing elimination of the sustained release formulation. Other, more permanent options are implants. These however typically show only slow or even no degradation and may thus require surgical removal, rendering this option challenging form the viewpoint of application.

[0026] The above limitations for the intravesical treatment of neurogenic disorders apply likewise for the treatment of infections or inflammations of the urinary bladder, which are also challenging to be treated efficiently.

[0027] Overall, therefore, there is a great need in the state of the art for corresponding concepts that reliably ensure sustained drug release, in particular specifically to the urogenital tract, preferably the urinary bladder, while being applicable and / or removable without the need for excessive invasive effort. Against this background, it is thus an object of the present invention to provide a concept and specifically a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, particularly being suited for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the problems and disadvantages existing in the context of the state of the art are avoided, or at least mitigated.

[0028] In this context, it is a particular object of the present invention to provide a concept, in particular by means of a composition, that can be intravesically applied and is particularly suited for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein this concept overcomes the risk of early voiding from the urinary bladder.

[0029] Further, according to another object of the present invention, it is envisaged to provide a concept, in particular by means of a respective composition, that is particularly suited for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the concept allows for sustained drug release and thus, for prophylactic and / or curative treatment over an extended or prolonged period of time, while at the same time being associated with better handleable application.

[0030] As a solution to the object described, the present invention thus proposes - according to a f i r s t aspect of the present invention - a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder. Further advantageous embodiments and configurations of this aspect of the invention are subject matter of the respective secondary or dependent claims.

[0031] Further subject matter of the present invention - according to a s e c o n d , t h i r d and f o u r t h aspect of the present invention - is the use of a composition according to the invention for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as the use of a composition according to the invention for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as a respective method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder.

[0032] Again further subject matter of the present invention - according to a f i f t h aspect of the present invention - is the use of a composition according to the invention for forming a drug delivery system (DDS), particularly a sustained-release drug delivery system (SR-DDS), preferably an in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0033] Moreover - according to a s i x t h aspect of the present invention - subject matter of the present invention is a drug delivery system (DDS), particularly sustained- release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder. Further advantageous embodiments and configurations of this aspect of the invention are subject matter of the respective secondary or dependent claims.

[0034] Further subject matter of the present invention - according to a s e v e n t h , e i g h t h and n i n t h aspect of the present invention - is the use of a drug delivery system according to the invention for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as the use of a drug delivery system according to the invention for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as a respective method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder. Again, further subject matter of the present invention - according to a tenth, eleventh and twelfth aspect of the present invention - is an application device, in particular syringe, preferably ready-to-use piston syringe, comprising a composition, especially pharmaceutical composition, according to the invention, as well as a packaging unit comprising at least one pack and at least one application device according to the invention as well as a kit-of-parts comprising an instillation system.

[0035] Moreover, subject matter of the present invention - according to a thirteenth aspect of the present invention - is an active agent (active ingredient), particularly pharmaceutical active ingredient (API), for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder.

[0036] Further subject matter of the present invention - according to a fourteenth, fifteenth and sixteenth aspect of the present invention - is the use of an active agent according to invention for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as the use of an active agent according to the invention for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, as well as a respective method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder.

[0037] Finally, further subject matter of the present invention - according to a seventeenth and eighteenth aspect of the present invention - is the use of a composition, especially pharmaceutical composition, for intravesical application of at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API) into the urinary bladder, and are the methods and uses described herein characterized each by one or more of the features of the composition according to the invention. It goes without saying that configurations, embodiments, advantages and the like, which are described below for the purpose of avoiding repetition with respect to one aspect of the invention, naturally also apply accordingly with respect to the other aspects of the invention, without this requiring separate mention.

[0038] Furthermore, with regard to the following description of the present invention, it is also the case that the features of the present invention cited in each case in connection with the particular configurations, embodiments, advantages, examples or the like are also considered disclosed in their combination. Thus, superordinate combinations of individual or several features, which are indicated for respective configurations, embodiments, examples of use or the like, are also considered disclosed herein.

[0039] In the case of all relative or percentage weight-related data mentioned below, in particular quantity or concentration data, it should furthermore be noted that these are to be selected by the skilled person within the scope of the present invention in such a way that in sum, including all components or ingredients, they add up or complement each other, in particular as defined below, to 100% or 100% wt. %; however, this is self-evident to the skilled person.

[0040] Furthermore, for the description of the present invention, the features of the present invention mentioned in the context of the specific configurations, embodiments, advantages, examples or the like are also deemed to be disclosed in their combination. Thus, superordinate combinations of individual or several features which are cited for respective configurations, embodiments, examples of use or the like are also deemed to be disclosed in the present case. In particular, for the features characterizing the invention, all possible combinations of these features are deemed to be disclosed, wherein embodiments of comparable or according to preference of the various features are preferably combined (e.g. quantities or quantity ranges of the related parameters of the same preference or the like).

[0041] In particular, it is also the case that for the following details relating to the various parameters of the method according to the invention or the like with the same preference or the same preference level, respective combinations relating to the various parameters are also disclosed with according to preference or preference. Likewise, all other combinations (i.e. combinations onto different preferences or different levels of preference) are also disclosed. In addition, it applies that all values or parameters or the like mentioned in the following can in principle be measured or determined with standardized or explicitly stated determination methods and otherwise with determination or measurement methods familiar to the person skilled in the art in this field. Unless otherwise stated, the underlying values or parameters are determined under standard conditions (i.e. in particular at a temperature of 20 °C and / or at a pressure of 1 ,013.25 hPa or 1 .01325 bar) or atmospheric pressure.

[0042] With these provisos in mind, the present invention will be explained in detail hereinbelow:

[0043] The present invention - according to a f i r s t aspect of the present invention - relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing

[0044] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0045] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0046] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0047] Hence, according to the invention, it is envisioned that the drug delivery system is configured to release the active agent over a period of time that is significantly longer or more extended than drug delivery of the active agent as such and / or without the polymer matrix around.

[0048] The composition, especially pharmaceutical composition, of the present invention may be, for instance, in the form of a drug, medicament or pharmaceutical, respectively. The term of "drug" or "medicament" (also synonymously "pharmaceutical(s)"), as used in the context of the present invention, is to be understood in a very extensive manner and encompasses not only drugs or pharmaceuticals as such (i.e. with respect to drug legislation), but particularly also so-called medical products and / or medical devices as well. In other words, the composition according to the invention can thus be present in the form of a drug or medicament (i.e. a pharmaceutical), a medical product, a medical device and / or a homeopathic product. Further, in the context of the present invention, also the term "solution" is to be understood broadly in a sense that it encompasses solutions ranging from such solutions, in which all components are present in complete dissolution, to such solutions, in which parts of the components are not dissolved, i.e. solutions which have characteristics of dispersions, in particular suspensions.

[0049] It is generally envisioned that the solutions are in liquid state, wherein liquid state means water-liquid to viscous liquid, wherein such liquid solutions in the context of the present invention mainly are envisioned to fulfil the requirement to be applicable by means of instillation, in particular by means of a catheterizing device (catheter).

[0050] The present invention is associated with a range of advantages the applicant surprisingly realized:

[0051] By means of the composition according to the invention, a concept for reliable extended and / or prolonged application of an active agent to a urinary bladder to be treated can be ensured. It is specifically possible in the context of the present invention to provide a prophylactic or therapeutic treatment concept which allows for prolonged and / or long-term therapeutic treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, directly locally, i.e. in the urinary bladder and / or urogenital tract. The composition according to the invention consequently is envisioned to be applied directly to a urinary bladder or urogenital tract to be treated and is configures such that it remains at the application site and thereby releases an active agent over a prolonged or extended period of time.

[0052] Hence, the inventive concept in particular is directed at an advantageous drug delivery system (DDS) for sustained drug release, i.e. a sustained-release drug delivery system (SR-DDS), with which diseases or dysfunctions of the urogenital tract and / or the urinary bladder can be treated effectively as well as directly locally. Based on this application mode, side effects of active agents can be diminished and effectiveness of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, can be increased. Further, metabolic effects like first-pass effects or early drug degradation can be circumvented, allowing thus also for the effective application of such active agents that have no or only limited effectiveness and / or efficacy upon systemic application, e.g. through oral administration.

[0053] Further advantageous, the composition according to the invention can lead or contribute to better handling and treatment of persistent acute or chronic diseases of the urogenital tract as well as neurogenic dysfunctions, as the composition advantageously is configured to form a polymer matrix comprising an active agent that is released over an extended period of time from the matrix.

[0054] Accordingly, the polymer matrix advantageously comprises a certain stability against degradation in the urinary bladder, allowing generally for sustained drug release to the urogenital tract. Further, by means of forming a three-dimensional matrix, the composition according to the invention advantageously ensures entrapment or encapsulation of the active agent contained in the composition upon application to the urinary bladder. Through the polymer matrix, the active agent advantageously is released slowly over time, such that a truly sustained-release drug delivery system (SR-DDS) can be provided by means of the present invention. Hence, the present invention for the first time provides an application-friendly and reliably prolonged- acting DDS that is specifically adapted for application to the urinary bladder and / or treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder.

[0055] This is particularly remarkable, since the urinary bladder, as stated above, is a challenging site for direct drug application as it poses a number of challenges to be overcome. Advantageously in this context, the present invention provides a composition that can overcome the risk of early voiding from the urinary bladder based on the formation of a polymer matrix upon contact of the composition with urine. By means of the polymer matrix formed, the active agent is entrapped in the matrix, while the matrix itself forms an in particular rigid and / or solidified three- dimensional structure which is insensitive or resistant to being emptied or flushed out of the bladder. Thus, the DDS according to the present invention can also be understood as an implant, i.e. a composition constituting a type of medical device provided and / or manufactured to in particular enhance an existing biological structure, here the urinary bladder. Furthermore, since the implant is formed upon application directly at the application site - the urinary bladder - this can even more advantageously be considered an in s / Yu-forming implant (ISFI).

[0056] The polymer matrix formation at the application site, in particular the in s / Yu-forming characteristic, of the composition according to the invention goes along with the particular advantage, that application of the implant is comparably well manageable, specifically by means of a catheterizing device (catheter), such that in the context of the present invention advantageously no extensive surgical effort is necessary to provide a urinary bladder to be treated with the composition, specifically the ISFI- DDS, according to the invention.

[0057] Further advantageous, due to the nature of the polymers envisioned for use in the composition according to the invention, the polymer matrix formed in the urinary bladder, specifically the DDS or ISFI, degrade naturally over time by means of hydrolysis in the urine present in the urinary bladder. Therefore, no surgical effort is needed for removal of the implant. This makes the inventive concept particularly well- handleable and gently applicable, which is particularly beneficial and may pose a significant relief for patients that need frequent medication instilled into the urinary bladder due to chronic disease or neurogenic dysfunction. The inventive concept thus provides an especially beneficial concept for patients that so far need to rely on frequent instillation of medication to the urinary bladder for treatment of in particular neurogenic dysfunctions like neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), and neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome. Beyond that, the inventive concept also allows for novel approaches for the local long-term treatment of e.g. cancer or tumor diseases of the urinary tract, which allows for better and more direct drug effects on the affected tissues while at the same time stress through invasive procedures can be reduced.

[0058] Further advantageously, the components of the inventive composition, in particular polymer and solvent, are specifically selected such that side effects originating from these components are not to be expected. The composition according to the present invention is based on physiologically well-tolerated components, specifically with a focus on the polymer and solvents preferred in the context of the present invention. It is further advantageously the case, that degradation products from the polymer or solvent residues are ensured to be excreted from the urinary bladder and the body as a whole within comparably short time, such that also no long-term effects of components of the composition according to the present invention are to be expected. For the active agents envisioned to be used in the context of the present invention, their potential side-effects can as well be minimized due to the site-specific and local application directly at the side of action.

[0059] Overall, the present invention thus achieves to in particular provide a highly effective and at the same time well-tolerable and gently to apply medication concept for the prolonged and / or extended prophylactic and / or therapeutic treatment of diseases or dysfunctions associated with the urogenital tract and in particular the urinary bladder. Specifically, the present invention provides such a composition that can be applied via instillation to a urinary bladder to be treated, to form an in particular long-acting DDS in the urinary bladder, which especially can also be perceived as an ISFI, and which degrades gradually over time such that sustained medication is ensured while no surgical removal or the like is necessary. This overall advantageously constitutes an immense relief for those patients, who need to rely on frequent instillations, partially multiple times per day, due to their respective conditions, that by means of the present invention can be addressed in an improved manner.

[0060] As stated above, the present invention relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing

[0061] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0062] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0063] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0064] In the context of the present invention it proved particularly effective for the composition according to the invention and its respective application, if the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder. Thus, by means of the present invention, in particular the composition according to the invention, an effective treatment option for a broad range of diseases and / or dysfunctions of the urogenital tract, in particular the urinary bladder, can be provided wherein, with the present invention, especially such diseases and / or dysfunctions can be treated particularly effectively that are chronic or persistent conditions and thus require long-term treatment and / or drug application. Especially for such diseases and / or dysfunctions, the present invention constitutes an advantageous option to provide a more effective and less challenging treatment, particularly in view of the site-specific and direct or local application of the inventive composition and the thus preferably formed DDS, in particular SR-DDS and / or ISF I , to the urinary bladder as the relevant target site for the above listed diseases and / or dysfunctions, while at the same time the application of the composition can be performed by one-time catheterization for treatment of a patient over a prolonged period of time.

[0065] Further in the context of the present invention, it is preferably provided that the three- dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, at least 35 %, in particular at least 45 %, preferably at least 55 %, more preferably at least 60 %, of the active agent contained in the composition. Likewise, it has proven well, if the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, up to 100 %, in particular up to 98 %, preferably up to 95 %, more preferably up 93 %, of the active agent contained in the composition. Thus, overall good results are achieved, if the three-dimensional matrix, in particular the three- dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, 35 % to 100 %, in particular 45 % to 98 %, preferably 55 % to 95 %, more preferably 60 % to 93 %, of the active agent contained in the composition. For determination of the listed proportions, it proved well if the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, is determined by means of injecting the composition into artificial urine, taking a sample of the composition immediately after injection, analyzing the proportion of free and / or non-entrapped and / or nonembedded, especially non-encapsulated, active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, based on the proportion of free and / or non-entrapped and / or non-embedded, especially nonencapsulated, active agent.

[0066] The present invention thus advantageously achieves a beneficial level of active agent entrapment and / or encapsulation to ensure reliably high long-term or extended-period active agent release to the urinary bladder. Further advantageously, the preferably achieved proportions of active agent entrapment and / or encapsulation allow for an efficient, well-controllable and easy-to-dose preparation of the inventive composition in view of a certain active agent level or dosage to be reached for adequate disease and / or dysfunction treatment. At the same time, by means of the present invention, the proportion of active agent comprised and / or entrapped in the polymer matrix, in particular the DDS, in particular SR-DDS and / or ISFI, can be adjusted such, that a so-called initial drug-burst, i.e. an initial active agent release, can be achieved by means of which a first, comparably high dosage of an active agent can be released to the urinary bladder to reach a first, acute treatment of a condition followed by longer term treatment. This mode of action can be particularly beneficial for infections and inflammations of the urogenital tract, cystitis and also tumor or cancer treatments which may require an initial high dosage of a respective agent, followed by prolonged continuous drug release.

[0067] Preferably the composition according to the invention is designed such, that the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent is formed within a time period of at most 45 minutes, in particular of at most 35 minutes, preferably of at most 25 minutes, more preferably of at most 20 minutes, after the composition has been contacted with urine present in the urinary bladder. Likewise, it proved advantageous, if the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent is formed within a time period of from 0.01 seconds to 45 minutes, in particular within a time period of from 0.05 seconds to 35 minutes, preferably within a time period of from 0.1 seconds to 25 minutes, more preferably within a time period of from 0.2 seconds to 20 minutes, after the composition has been contacted with urine present in the urinary bladder. The composition of the present invention is thus associated with the advantage that the polymer matrix, in particular DDS, in particular SR-DDS and / or ISFI, based on the polymers preferably used in the present invention, forms comparably and reliably quick, which especially also ensures the preferred active agent entrapment and / or encapsulation proportions described above. Furthermore, the above polymer matrixformation times ease application of the composition according to the invention and thus contribute to the aspect of a gentle and convenient application which may pose a particular relief for those patients, who rely of frequent medication due to e.g. neurogenic dysfunctions and thus, at current times, are limited to treatment options which require drug application or medication several times per day, which can be overcome by the present invention.

[0068] The composition of the present invention further preferably is configured such, that the composition undergoing in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / tu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release, releases the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours. In this context, it is in particular envisioned that a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release, preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

[0069] In the context of the present invention, it is thus advantageously ensured, that within the time periods given a reliably controllable amount of active agent is released into the urinary bladder, which allows for effective treatment of a patient and reliable design of treatment plans. Further advantageous, over the entire lifespan of the polymer matrix, in particular DDS, in particular SR-DDS and / or ISFI, the active agent is released entirely to the urinary bladder, such that no loss of active agent can occur which contributes as well to reliable planning and design of medication of a patient. According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing

[0070] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0071] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0072] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

[0073] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0074] Further, it proved well in the context of the present invention if the composition comprises one (single) continuous phase and / or is monophasic and / or is composed of a single phase. Likewise, it is preferably envisioned that the composition is not multiphasic, in particular is not biphasic, and / or is not composed of more than one phase.

[0075] Respective compositions show advantageous matrix formation patterns as well as balanced and well-handleable application characteristics. Biphasic systems may in particular pose difficulties in connection with an application via a catheterizing device, in particular due to uneven flow behavior or the like. Further, even contact of a biphasic composition with urine cannot be ensured which would accordingly obstruct proper formation of a continuous and structurally integer polymer matrix, which however is important for a reliably prolonged active agent release. Accordingly, good results are obtained in the context of the present invention, when single phased compositions are provided. According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution, in particular continuously phased and / or monophasic and / or single phased solution, containing

[0076] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0077] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0078] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard; and / or wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, at least 35 %, in particular at least 45 %, preferably at least 55 %, more preferably at least 60 %, of the active agent contained in the composition, and / or comprises and / or entraps and / or embeds, especially encapsulates, up to 100 %, in particular up to 98 %, preferably up to 95 %, more preferably up 93 %, of the active agent contained in the composition; in particular wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, 35 % to 100 %, in particular 45 % to 98 %, preferably 55 % to 95 %, more preferably 60 % to 93 %, of the active agent contained in the composition; preferably wherein the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, is determined by means of injecting the composition into artificial urine, taking a sample of the composition immediately after injection, analyzing the proportion of free and / or non-entrapped and / or non-embedded, especially non-encapsulated, active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, based on the proportion of free and / or non-entrapped and / or nonembedded, especially non-encapsulated, active agent.

[0079] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0080] Regarding the active agent, it is preferred in the context of the present invention, if the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or antiinflammatory agents, in particular from the group consisting of non-steroidal antiinflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof.

[0081] Specifically, it is preferably the case that the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0082] For the listed active agents, it is advantageously found, that these display an improved effectiveness when applied locally and / or site specifically to the target site, in this case the urinary bladder, since metabolic processes influencing the active agents can be excluded in the context of the present invention. Therefore, the listed active agent proved particularly suitable for integration into the composition, in particular DDS, in particular SR-DDS and / or ISFI, according to the present invention. According to a preferred embodiment of the present invention, it is further envisioned that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0083] Even more preferred it is such, that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent is selected from oxybutynin as well as salts and esters thereof.

[0084] Very good results are obtained in the context of the present invention, if the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and if the active agent is selected oxybutynin as well as salts and esters thereof.

[0085] For these preferred configurations and / or embodiment of the present invention, particularly good effects on the treatment of the named diseases and / or dysfunctions are achieved by means of application of the listed active agents in compositions according to the invention.

[0086] Further it proved advantageous, if the active agent, particularly the pharmaceutical active ingredient (API), is present and / or used in neutral and / or uncharged molecular form and / or in form of the active agent as such or in the form of a pharmaceutically acceptable salt or ester or mixtures or combinations thereof. By means of this feature, it can advantageously be achieved that the release of the active agent into urine present in the urinary bladder can be even more retarded, such that the prolonged release effect envisioned in the context of the present invention is achieved even more reliably. Specifically, it is envisioned that active agents with a molecular structure or form that is associated with a neutral or even positive charge per se on the one hand require a distinct amount of time to dissolve in urine, in particular even precipitate initially in urine and then gradually resolve over time in the polymer matrix and from there diffuse into the urinary bladder upon which the therapeutic effect is displayed. By means of this mode of action, sustained release of the active agent from the polymer matrix formed, in particular the DDS, in particular SR-DDS and / or ISFI, in urine can be ensured such that an effective and especially continuous long-term action of the active agent can beneficially be provided. On the other hand, positively charged active agents allow for interaction with the polymer contained in the inventive composition which likewise results in a more pronounced sustained release effect and thus as well contributes to a reliable long-term action of the active agent against the indications given above.

[0087] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing

[0088] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof, in particular wherein the active agent, particularly the pharmaceutical active ingredient (API), is present and / or used in neutral and / or uncharged molecular form and / or in form of the active agent as such or in the form of a pharmaceutically acceptable salt or ester or mixtures or combinations thereof;

[0089] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0090] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0091] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above. Further in the context of the present invention, it proved advantageous, if the active agent, particularly the pharmaceutical active ingredient (API), is net-positively charged; or if the active agent, particularly the pharmaceutical active ingredient (API), is net- neutral; or if the active agent, particularly the pharmaceutical active ingredient (API), is net- negatively charged; or if the active agent, particularly the pharmaceutical active ingredient (API), is a mixture of net-positively charged, net-negatively charged and net-neutral active agents.

[0092] It is preferred in this context, if the pharmaceutical active ingredient (API), is net- positively charged; or if the active agent, particularly the pharmaceutical active ingredient (API), is net- neutral; or if the active agent, particularly the pharmaceutical active ingredient (API), is a mixture of net-positively charged, net-negatively charged and net-neutral active agents

[0093] According to a preferred configuration and / or embodiment of the present invention it is envisioned in this context, that net-positive, net-negative or net-neutral charge of the active agent is induced by means of modification of the agent, in particular by means of chemical reaction, in particular derivatization or masking of charged functional groups; neutralizing treatment or alkalizing treatment, in particular by means of salt formation, ion-exchange, esterification and / or precipitation.

[0094] The respective advantages are as described before, in that a reliable and even more pronounced sustained release of the active agent from the polymer matrix can be achieved.

[0095] If further proved well in the context of the present invention, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at least 0.05 wt.%, in particular in amounts of at least 0.1 wt.%, preferably in amounts of at least 0.2 wt.%, more preferably in amounts of at least 0.3 wt.%, based on the total composition. Likewise, good results are obtained, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at most 50 wt.%, in particular in amounts of at most 35 wt.%, preferably in amounts of at most 25 wt.%, more preferably in amounts of at most 20 wt.%, based on the total composition. It is particularly preferred, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts in a range of from 0.05 wt.% to 50 wt.%, in particular in amounts in a range of from 0.1 wt.% to 35 wt.%, preferably in amounts in a range of from 0.2 wt.% to 25 wt.%, more preferably in amounts in a range of from 0.3 wt.% to 20 wt.%, based on the total composition.

[0096] Amounts of the active agent in the aforementioned regions advantageously combine well-configured release patterns from polymer matrixes formed from the composition in urine with suitable active agent levels for effective treatment of diseases or dysfunctions of the urinary bladder.

[0097] Further with regard to the polymer, it is preferred in the context of the present invention, if the composition comprises a mixture of biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymers selected from the group consisting of matrix-forming polymers, preferably selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co- glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic- co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG),

[0098] (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer; or if the composition comprises one single type of biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, preferably selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co- polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co- glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL),

[0099] (vii) poly(lactide-co-caprolactone) copolymer, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)). Further, it is in particular preferred, if the mixture of biodegradable and / or biocompatible polymers or the single type of biodegradable and / or biocompatible polymer is composed of one or more polymer fractions of a / the single polymer, in particular wherein the polymer fractions differ in one or more aspects selected form the group consisting of molecular weight, chemical modification, end-group configuration and / or end-group modification, net-charge, molecular shape, in particular branching, monomer ratio, in particular in case of co-polymers.

[0100] By means of the polymers preferably used in the context of the present invention, polymer matrix formation as well as biodegradation of the polymer in the urinary bladder can advantageously be adjusted and / or controlled with regard to the desired characteristics of the polymer matrix, in particular the DDS, SR-DDS, specifically ISFI, obtained from the composition. In particular, it is advantageously found in the context of the present invention, that the polymer, its composition as such and / or the use of a mixture of polymers allows for modification of the polymer matrix formed in terms of e.g. stability and / or duration of matrix formation, as well as for modification of the degradation behavior of the polymer, in particular in terms of time period over which degradation proceeds. Accordingly, the inventive composition by means of the polymer used therein advantageously allows for controlled and / or targeted variation of the polymer matrix, in particular the DDS, SR-DDS, specifically ISFI, obtained from the composition, such that depending on the indication to be treated variations in the composition can be performed to adapt the composition preferably ideally its envisioned purpose.

[0101] Further in this regard, it proved advantageous, if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at least 500 g / mol, in particular of at least 750 g / mol, preferably of at least 1 ,500 g / mol, preferably of at least 3,000 g / mol, preferably of at least 5,000 g / mol, preferably of at least 6,000 g / mol, more preferably of at least 7,000 g / mol. Likewise, it is preferred, if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at most 200,000 g / mol, in particular of at most 100,000 g / mol, preferably of at most 75,000 g / mol, more preferably of at most 50,000 g / mol. Particularly good results are thus obtained in the context of the present invention, if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwin a range of from 500 g / mol to 200,000 g / mol, in particular in a range of from 750 g / mol to 200,000 g / mol, preferably in a range of from 1 ,500 g / mol to 200,000 g / mol, preferably in a range of from 3,000 g / mol to 200,00 g / mol, preferably in a range of from 5,000 g / mol to 100,000 g / mol, preferably in a range of from 6,000 g / mol to 75,000 g / mol, more preferably in a range of from 7,000 g / mol to 50,000 g / mol. In particular it is envisioned here that the weight average molecular weight Mwis determined by means of size-exclusion chromatography, preferably in accordance with standard ISO 16014 of 2019.

[0102] Further with regard to the polymer, it proved well if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer comprises a chemical modification, in particular an end-group modification and / or capping. Particularly good results are obtained in this context, if the chemical modification, in particular end-group modification and / or capping, is selected from branching, in particular graft copolymerization, esterification, in particular by means of short-chain alcohols, etherization, PEGylation, salt formation, in particular ion exchange to physiologically compatible and / or physiologically tolerable counter ions, and / or acid-functionalization, in particular by means of carboxylic acids, preferably by means of acrylic acid and / or methacrylic acidmodification.

[0103] By means of this feature, the chemical properties of polymers used in the context of the present invention can advantageously be influenced such, that matrix formation as well as the degradation behavior can be tuned in accordance with the envisioned purpose of the composition according to the invention, in particular in accordance with the time period over which the release of the active agent should proceed. Accordingly, the present invention, by means of the polymer used in the inventive composition, provides a flexible and adaptable treatment option specifically for longterm applications.

[0104] In the context of the present invention, it is further preferred, if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is net-negatively charged; or if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is net-neutral; or if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is a mixture of net-negatively charged and net-neutral polymers.

[0105] In this context it proved particularly well, if net-negative or net-neutral charge of the polymer is induced by means of chemical modification, in particular end-group modification and / or capping, of the polymer, preferably wherein the chemical modification, in particular end-group modification and / or capping, is selected from branching, in particular graft copolymerization, esterification, in particular by means of short-chain alcohols, etherization, PEGylation, salt formation, in particular ion exchange to physiologically compatible and / or physiologically tolerable counter ions, and / or acid-functionalization, in particular by means of carboxylic acids, preferably by means of acrylic acid and / or methacrylic acid-modification.

[0106] For polymers with the aforementioned properties a particularly suited balance between matrix stability as well as stability in urine, and biodegradability, in particular duration until in particular essentially complete biodegradation, can be achieved in view of the application site of the inventive composition, i.e. the urinary bladder, vis- a-vis the indication, for which the inventive composition is envisioned to be applied for.

[0107] Further in this regard, it proved advantageous if the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is a copolymer selected from the group consisting of matrixforming polymers, preferably wherein the copolymer is selected from the group consisting of (poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG), poly(lactic-co-glycolide acid) copolymer (PLGA), poly(lactide-co-caprolactone) copolymer; in particular wherein the copolymer has a ratio of first monomer : second monomer in a range of from 99 : 1 to 1 : 99, in particular in a range of from 85 : 15 to 15 : 85, preferably in a range of from 60 : 30 to 30 : 60, more preferably in a range of from 55 : 45 to 45 : 55.

[0108] It was advantageously found that by means of the monomer ratio in a copolymer, the physiologic stability and / or tendency for degradation under the conditions present in the urinary bladder can be influenced and in particular can be tailored to specific needs associated with the intended use of the inventive composition. According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing

[0109] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of nonsteroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;

[0110] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is a copolymer selected from the group consisting of matrix-forming polymers, preferably wherein the copolymer is selected from the group consisting of (poly(lactide- co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co- polyethylene glycol) copolymer (PLA-PEG), poly(lactic-co-glycolide acid) copolymer (PLGA), poly(lactide-co-caprolactone) copolymer; in particular wherein the copolymer has a ratio of first monomer : second monomer in a range of from 99 : 1 to 1 : 99, in particular in a range of from 85 : 15 to 15 : 85, preferably in a range of from 60 : 30 to 30 : 60, more preferably in a range of from 55 : 45 to 45 : 55; and / or in particular wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at least 500 g / mol, in particular of at least 750 g / mol, preferably of at least 1 ,500 g / mol, preferably of at least 3,000 g / mol, preferably of at least 5,000 g / mol, preferably of at least 6,000 g / mol, more preferably of at least 7,000 g / mol, and / or has a weight average molecular weight Mwof at most 200,000 g / mol, in particular of at most 100,000 g / mol, preferably of at most 75,000 g / mol, more preferably of at most 50,000 g / mol, preferably wherein the weight average molecular weight Mwis determined by means of size-exclusion chromatography, preferably in accordance with ISO 16014 of 2019;

[0111] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0112] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0113] Further in the context of the present invention, it is preferably the case that the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is linear; or that the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is branched, in particular graft- copolymerized, comb-like or in a dendrimeric manner. By means of a respectively configured polymer, physiologic stability as well as matrix formation characteristics and degradation properties advantageously can be further modified in relation the intended use of the composition according to the invention.

[0114] Compositions according to the invention with advantageous characteristics are in particular obtained, if the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at least 5 wt.%, in particular in amounts of at least 10 wt.%, preferably in amounts of at least 12.5 wt.%, more preferably in amounts of at least 15 wt.%, based on the total composition.

[0115] Good results are likewise obtained, if the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at most 50 wt.%, in particular in amounts of at most 40 wt.%, preferably in amounts of at most 35 wt.%, more preferably in amounts of at most 30 wt.%, based on the total composition. It is specifically preferred, if the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts in a range of from 5 wt.% to 50 wt.%, in particular in a range of from 10 wt.% to 40 wt.%, preferably in a range of from 12.5 wt.% to 35 wt.%, more preferably in a range of from 15 wt.% to 30 wt.%, based on the total composition.

[0116] Compositions with polymer amounts in the aforementioned ranges advantageously are configured such that stable and comparably compact or dense polymer matrixes can be formed upon contact with urine which proved advantageous in view of drug release patterns, in particular on the long-term.

[0117] Still, it is advantageously ensured that a continuous release of active agent can be provided by means of diffusion of the active agent through pores or voids or the like in the polymer matrix network. Further, polymer amounts in the aforementioned ranges contribute to well-applicable compositions, specifically for application to the urinary bladder by means of a catheterizing device, wherein compositions with a balanced viscosity and adequate flow behavior are obtained, that in addition form sufficiently fast polymer matrixes comprising the active agent upon contact with urine. In the context of the present invention it proved particularly well, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1.5 to 1 : 500, preferably in a range of from 1 : 1.75 to 1 : 200, more preferably in a range of from 1 : 2 to 1 : 50, particularly based on the weight percentage of the respective components (i.e. active agent and polymer).

[0118] Active agent to polymer-ratios in the aforementioned ranges advantageously give compositions with well-balanced application properties. In particular can such compositions be obtained that display sustained release-characteristics for the active agent from the polymer matrix formed upon contact with urine that span time periods well-adapted to the diseases and / or dysfunctions to be treated by means of the inventive composition. Further, a continuous and uniform and / or consistent active agent release can be achieved with the aforementioned ratios, which contributes to an effective and well-plannable treatment.

[0119] With regard now to the solvent used in the composition according to the present invention, if proved well, if the solvent is selected from protic or aprotic solvents having a polarity lesser than the polarity of water and / or lesser than the polarity of urine.

[0120] In particular, it was found advantageous, if the solvent has a relative polarity value E? of less than 1 and / or more than 0.1. Even more preferably, it is such that the solvent has a relative polarity value E? of at most 0.95, in particular of at most 0.9, preferably at most 0.85, more preferably of at most 0.8. Good results are also obtained, if the solvent has a relative polarity value E? of at least 0.15, in particular of at most 0.2, preferably at most 0.25, more preferably of at most 0.3.

[0121] Particular preferably, the solvent has a relative polarity value E? in a range of from 0.15 to 0.95, in particular in a range of from 0.2 to 0.9, preferably in a range of from 0.25 to 0.85, more preferably in a range of from 0.3 to 0.8. In this context it is especially envisioned that the relative polarity value E? is obtained from the £r(30)-value normalized to the polarity extremes tetramethylsilane set as zero (= 0) and water set as 1 (= 1 ), wherein the £r(30)-value is defined as the transition energy of the long-wavelength VIS / NIR absorption band in a solution comprising the negative solvatochromic Reichardt dye (Betaine 30) at standard conditions (20 °C, 1.013 bar) indicated in the unit kcal / mol.

[0122] Solvents with the aforementioned polarity properties display an in the context of the present invention advantageous miscibility with urine as well as solubility for the active agent and polymer contained in the composition according to the invention. It is thus advantageously ensured that active agent and polymer are evenly distributed and especially dissolved in the solvent, forming thus an in particular at least essentially homogenous solution which can be smoothly and safely applied to a urinary bladder to be treated, in particular by means of a catheterizing device. Likewise, solvents with a polarity as mentioned above diffuse rapidly and completely in urine upon contact thus advantageously facilitating a comparably rapid polymer matrix formation from the composition as a result of changing polarities from solvent and urine upon contacting the solution with urine and consequent solidification and aggregation of the polymer. Within this process, active agent is enclosed and / or entrapped in the solidifying and aggregating polymer resulting in the polymer matrix that mediates prolonged and or long-term release of the active agent.

[0123] In the context of the present invention it is preferably envisioned that the solvent is selected from the group consisting of A / -Methyl-2-pyrrolidon (NMP); dimethyl sulfoxide (DMSO); alkylene carbonates, in particular ethylene carbonate (EC), propylene carbonate (PC) and mixtures thereof, preferably propylene carbonate (PC); dihydrolevoglucosenone (Cyrene™); dimethyl sulfone (DMSO2); glycofurol (GF); ethanol (EtOH), isopropanol (IPA) and mixtures thereof; in particular propylene carbonate (PC), glycofurol (GF) and mixtures thereof.

[0124] The aforementioned solvents display particularly beneficial properties in the context of the present invention in that the solvents are miscible with urine, able to dissolve active agent and polymer sufficiently, in particular especially as at least substantially completely, and furthermore the solvents are, in particular in the amounts applied in the context of the present invention, physiologically tolerable and do not go along with relevant side effects.

[0125] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing

[0126] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0127] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0128] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine, wherein the solvent is selected from protic or aprotic solvents having a polarity lesser than the polarity of water and / or lesser than the polarity of urine; in particular wherein the solvent has a relative polarity value E? of less than 1 and / or more than 0.1 ; and / or in particular wherein the solvent has a relative polarity value E? in a range of from 0.15 to 0.95, in particular in a range of from 0.2 to 0.9, preferably in a range of from 0.25 to 0.85, more preferably in a range of from 0.3 to 0.8 (wherein the relative polarity value E? is obtained from the £r(30) -value normalized to the polarity extremes tetramethylsilane set as zero (= 0) and water set as 1 (= 1), wherein the £r(30)-value is defined as the transition energy of the long-wavelength VIS / NIR absorption band in a solution comprising the negative solvatochromic Reichardt dye (Betaine 30) at standard conditions (20 °C, 1.013 bar) indicated in the unit kcal / mol), in particular wherein the solvent is selected from the group consisting of N- Methyl-2-pyrrolidon (NMP); dimethyl sulfoxide (DMSO); alkylene carbonates, in particular ethylene carbonate (EC), propylene carbonate (PC) and mixtures thereof, preferably propylene carbonate (PC); dihydrolevoglucosenone (Cyrene™); dimethyl sulfone (DMSO2); glycofurol (GF); ethanol (EtOH), isopropanol (I PA) and mixtures thereof; in particular propylene carbonate (PC), glycofurol (GF) and mixtures thereof; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0129] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0130] Particularly good results are obtained in the context of the present invention, if the composition comprises the solvent in amounts of at least 40 wt.%, in particular in amounts of at least 50 wt.%, preferably in amounts of at least 55 wt.%, more preferably in amounts of at least 60 wt.%, based on the total composition. Likewise, it proved well, if the composition comprises the solvent in amounts of at most 90 wt.%, in particular in amounts of at most 80 wt.%, preferably in amounts of at most 75 wt.%, more preferably in amounts of at most 70 wt.%, based on the total composition. It is particularly preferred, if the composition comprises solvent in amounts in a range of from 40 wt.% to 90 wt.%, in particular in a range of from 50 wt.% to 80 wt.%, preferably in a range of from 55 wt.% to 75 wt.%, more preferably in a range of from 60 wt.% to 70 wt.%, based on the total composition.

[0131] Compositions comprising the solvent in the aforementioned amounts advantageously combine good dissolution of active agent and polymer with particularly suitable application properties in terms of ability to be applied via a catheterizing device (catheter) into the urinary bladder, as well as ability to form a polymer matrix comprising the active agent in adequately short time upon application in the urinary bladder from the composition according to the invention.

[0132] Specifically, for the aforementioned amounts of solvents in compositions according to the invention, rapid dissipation of the solvent in urine advantageously is ensured such that a structurally integer and in particular at least essentially compact polymer matrix that effectively entraps and / or encloses the active agent results.

[0133] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing

[0134] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of nonsteroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;

[0135] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co- polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co- polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co- glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0136] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release; and wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at least 0.05 wt.%, in particular in amounts of at least 0.1 wt.%, preferably in amounts of at least 0.2 wt.%, more preferably in amounts of at least 0.3 wt.%, based on the total composition, and / or in amounts of at most 50 wt.%, in particular in amounts of at most 35 wt.%, preferably in amounts of at most 25 wt.%, more preferably in amounts of at most 20 wt.%, based on the total composition; and / or wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at least 5 wt.%, in particular in amounts of at least 10 wt.%, preferably in amounts of at least 12.5 wt.%, more preferably in amounts of at least 15 wt.%, based on the total composition, and / or in amounts of at most 50 wt.%, in particular in amounts of at most 40 wt.%, preferably in amounts of at most 35 wt.%, more preferably in amounts of at most 30 wt.%, based on the total composition; and / or wherein the composition comprises the solvent in amounts of at least 40 wt.%, in particular in amounts of at least 50 wt.%, preferably in amounts of at least 55 wt.%, more preferably in amounts of at least 60 wt.%, based on the total composition, and / or in amounts of at most 90 wt.%, in particular in amounts of at most 80 wt.%, preferably in amounts of at most 75 wt.%, more preferably in amounts of at most 70 wt.%, based on the total composition.

[0137] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0138] Further in the context of the present invention, it proved particularly well, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the solvent in an active agent : solvent (weight) ratio in a range of from 1 : 1 to 1 : 10,000, in particular in a range of from 1 : 2 to 1 : 5,000, preferably in a range of from 1 : 3,5 to 1 : 1 ,000, more preferably in a range of from 1 : 5 to 1 : 500, in particular based on the weight percentage of components.

[0139] The aforementioned ratios advantageously ensure stable and reliable dissolution of the active agent in the composition such that good application properties can be realized and / or guaranteed.

[0140] In addition, it further proved well, if the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer and the solvent in an polymer : solvent (weight) ratio in a range of from 1 .5 : 1 to 1 :100, in particular in a range of from 1 : 1 to 1 : 75, preferably in a range of from 1 : 1.5 to 1 : 50, more preferably in a range of from 1 : 1.2 to 1 : 25, in particular based on the weight percentage of components. Ratios in the aforementioned regions contribute to in particular a least essentially complete dissolution of the polymer in the solvent such, that an in particular a least essentially homogenous solution is obtained that is easy to handle, in particular in terms of application. Furthermore, by means of the aforementioned ratios it is particularly ensured that a comparably fast matrix formation can be achieved upon contact of the composition according to the invention with urine.

[0141] Further in the context of the present invention, particularly good results are obtained, if the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer, and the solvent in an active agent + polymer : solvent (weight) ratio in a range of from 2 : 1 to 1 :50, in particular in a range of from 1.5 : 1 to 1 : 25, preferably in a range of from 1 : 1 to 1 : 15, more preferably in a range of from 1 : 1.2 to 1 : 10, in particular based on the weight percentage of components.

[0142] Compositions comprising such ratios advantageously show good dissolution of the components in the solvent, such that compositions with adequate viscosity for application by means of a catheterizing device (catheter) are obtained. Furthermore, an efficient ratio of active components to the solvent as a carrier can be reached, which contributes to adequate dosage sizes and improved handling of the composition while application.

[0143] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a composition, especially pharmaceutical composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition as previously described, wherein the composition comprises or at least essentially consists of a solution containing (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of nonsteroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids;

[0144] (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;

[0145] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co- polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co- polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co- glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG),

[0146] (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0147] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, and wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1 .5 to 1 : 500, preferably in a range of from 1 : 1 .75 to 1 : 200, more preferably in a range of from 1 : 2 to 1 : 50, particularly based on the weight percentage of the respective components; and / or wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer, and the solvent in an active agent + polymer : solvent (weight) ratio in a range of from 2 : 1 to 1 :50, in particular in a range of from 1.5 : 1 to 1 : 25, preferably in a range of from 1 : 1 to 1 : 15, more preferably in a range of from 1 : 1.2 to 1 : 10, in particular based on the weight percentage of components.

[0148] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred composition according to the present invention stated above.

[0149] Further in the context of the present invention, it proved well, if the composition has a viscosity of at least 10 mPas, in particular of at least 15 mPas, preferably of at least 20 mPas, more preferably of at least 25 mPas. Further preferred it may be that the composition has a viscosity of at least 100 mPas, in particular of at least 150 mPas, preferably of at least 175 mPas, more preferably of at least 190 mPas. Also, it is preferably such, that the composition has a viscosity of at most 15,000 mPas, in particular of at most 10,000 mPas, preferably of at most 7,500 mPas, preferably of at most 6,000 mPas, preferably of at most 5,000 mPas. Further preferred it may be that the composition has a viscosity of at most 1 ,500 mPas, in particular of at most 1 ,250 mPas, preferably of at most 1 ,100 mPas, more preferably of at most 1 ,000 mPas. Particularly good results are thus obtained in the context of the present invention, if the composition has a viscosity in a range of from 10 mPas to 15,000 mPas, in particular in a range of from 15 mPas to 15,000 mPas, preferably in a range of from 20 mPas to 15,000 mPas, more preferably in a range of from 25 mPas to 15,000 mPas. Also, it is preferably such, that the composition has a viscosity in a range of from 100 mPas to 15,000 mPas, in particular in a range of from 150 mPas to 7,500 mPas, preferably in a range of from 175 mPas to 6,000 mPas, preferably in a range of from 190 mPas to 5,000 mPas. Further preferred it may be, that the composition has a viscosity in a range of from 100 mPas to 1 ,500 mPas, in particular in a range of from 150 mPas to 1 ,250 mPas, preferably in a range of from 175 mPas to 1 ,100 mPas, more preferably in a range of from 190 mPas to 1 ,000 mPas. In this regard, is in particular envisioned that the viscosity is measured by means of rotational viscometry, preferably in accordance with ISO 3219 of 2021.

[0150] Viscosities in the aforementioned ranges advantageously go along with well-suited application properties of inventive compositions, specifically with a view on application of the composition by means of a catheterizing device (catheter), while at the same time it is ensured, that the composition is only so liquid or viscous that a reliable matrix formation can be assured, i.e. the composition is not too liquid such that the formation of a polymer matrix could be prevented or impeded due to overly fast dissipation of the solvent casing disruption of the polymer chains.

[0151] It proved further advantageous for the inventive composition, if the composition comprises or at least essentially consists of a solution containing in addition to the components (a), (b) and (c)

[0152] (d) at least one, particularly physiologically compatible and / or physiologically tolerable, adjuvant, in particular selected from the group consisting of pH- adjusting agents, surfactants, coagulants, wetting agents, excipients and mixtures thereof, preferably selected from pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids and / or acidic amino acids, amine sugars, in particular derived from aldohexoses, physiologically compatible and / or physiologically tolerable organic and / or inorganic acids and / or basis, and mixtures thereof.

[0153] Particularly preferred in the context of the present invention is the use of alkaline amino acids like lysine, arginine or histidine, especially lysine, as adjuvants. Likewise preferred is the use of amine sugars, in particular derived from aldohexoses, specifically such as meglumine, dimethyl meglumine, glucosamine, galactosamine, mannosamine and mixtures thereof, preferably meglumine, dimethyl meglumine and mixtures thereof. Thus it proved well, if pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids, are selected from the group consisting of lysine, arginine, histidine or mixtures thereof, in particular lysine, and / or wherein pH-adjusting agents and / or excipients selected from the group consisting of amine sugars, in particular derived from aldohexoses, are selected from the group consisting of meglumine, dimethyl meglumine, glucosamine, galactosamine, mannosamine and mixtures thereof, preferably meglumine, dimethyl meglumine and mixtures thereof.

[0154] These adjuvants advantageously allow for controlled and specifically tailored release of the active agent from the composition according to the invention. In particular, it is possible to adjust the speed or rate, with which the active agent is released from the formed drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI). As such, the use of adjuvants allows to further tune and tailor the characteristics of compositions according to the invention with regard to drug release.

[0155] Preferably, the inventive composition in general as well as all aforementioned preferred embodiments of the inventive composition may comprise the component (d) as previously described, such that the respective combinations are also included herein.

[0156] Furthermore, it proved advantageous in the context of the present invention, if a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts sufficient for the composition to be pharmaceutically effective over an extended and / or prolonged period of time and / or by diffusion-controlled release, in particular wherein a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts of at least 0.5 mg, in particular in amounts of at least 1 mg, preferably in amounts of at least 2 mg, more preferable in amounts of at least 5 mg. Likewise, good results are obtained, if a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts of at most 500 mg, in particular in amounts of at most 375 mg, preferably in amounts of at most 250 mg, more preferable in amounts of at most 200 mg. Specifically it is preferably the case, that a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts in a range of from 0.5 mg to 500 mg, in particular in a range of from 1 mg to 375 mg, preferably in a range of from 2 mg to 250 mg, more preferable in a range of from 5 mg to 200 mg.

[0157] The present invention - according to a s e c o n d aspect of the present invention - further relates to the use of a composition as previously described herein for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0158] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0159] The present invention - according to a t h i r d aspect of the present invention - further relates to the use of a composition as previously described herein for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0160] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0161] The present invention - according to a f o u r t h aspect of the present invention - further relates to a method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder, wherein a composition as previously described herein is intravesically, preferably via instillation by means of a catheterizing device (catheter), applied into the urinary bladder of a subject in need thereof, wherein the composition after intravesical application is contacted with urine present in the urinary bladder, and forms, in particular by means of the polymer, a three- dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0162] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0163] The present invention - according to a f i f t h aspect of the present invention - further relates to the use of a composition as previously described herein for forming a drug delivery system (DDS), particularly a sustained-release drug delivery system (SR-DDS), preferably an in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the drug delivery system is formed from the composition being contacted after intravesical application with urine present in the urinary bladder, in particular by means of a polymer, as a three-dimensional matrix, in particular as three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0164] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect. The present invention - according to a s i x t h aspect of the present invention - further relates to a drug delivery system (DDS), particularly a sustained-release drug delivery system (SR-DDS), preferably an in s / tu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the drug delivery system comprises or at least essentially consists of

[0165] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0166] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; especially wherein the drug delivery system is formed in situ in a urinary bladder to be treated. The present invention by means of the DDS, in particular SR-DDS and / or ISFI, according to the present invention provides a treatment concept for the urogenital tract that advantageously is specifically configured to enable prolonged and / or longterm treatment of diseases and / or dysfunctions of the urinary bladder or the urogenital tract in a directed and site-specific manner as by means of the DDS, in particular SR-DDS and / or ISFI, a locally restricted active agent application is achieved, by means of which effectiveness of the active agent may be enhanced and side-effects and in particular effectiveness-reducing effects like metabolic degradation can be circumvented.

[0167] Further advantageously, the DDS, in particular SR-DDS and / or ISFI according to the invention is designed such, that it forms a composition in form of a solution that is intravesically applied, and that converts and / or transforms into the DDS, in particular SR-DDS and / or ISFI, upon contact with urine, i.e. forms in situ at the application site which enables a gentle and comparably smooth application of the DDS, in particular SR-DDS and / or ISFI. At the same time, the DDS, in particular SR-DDS and / or ISFI further advantageously is designed such, that it is overall biodegradable, wherein the DDS, in particular SR-DDS and / or ISFI, comprises a distinct physiological stability, i.e. biodegradation of the DDS, in particular SR-DDS and / or ISFI proceeds gradually over a prolonged duration of time, during which the active agent contained in the DDS, in particular SR-DDS and / or ISFI, is released evenly and continuously. Due to the temporary persistent nature of the DDS, in particular SR-DDS and / or ISFI, this can also be perceived as an implant for sustained drug release, wherein the type of DDS, in particular SR-DDS and / or ISFI, provided with the present invention goes along with the great advantage that it does not require active removal from the site of action, as it degrades over time by itself. This contributes a further special advantage of the DDS, in particular SR-DDS and / or ISFI, according to the invention as this may pose particular relief for those patients who rely on frequent medication with respect to diseases and / or dysfunctions of the urinary bladder, in particular even multiple times per day, and to which by means of the DDS, in particular SR-DDS and / or ISFI, according to the present invention a medical composition and / or device is offered that alleviates treatment pressure and frequency.

[0168] In the context of the present invention, it proved particularly well, if the drug delivery system is formed in situ in a urinary bladder to be treated when a composition as previously described herein is contacted after intravesical application with urine present in the urinary bladder. Further, the DDS, in particular SR-DDS and / or ISFI according to the present invention was found to be particularly beneficial in those cases, where the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0169] Specifically, the aforementioned indications can particularly benefit from the site- direct and prolonged release of an active agent from the DDS, in particular SR-DDS and / or ISFI, according to the present invention, such that improved curative or prophylactic effects can be observed.

[0170] It further proved well in the context of the present invention, if the drug delivery system (DDS), particularly the sustained-release drug delivery system (SR-DDS), preferably the in s / tu-forming implant (ISFI), is configured for and / or is capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours. Herein it is particularly envisioned, that a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release, preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV- detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard. The DDS, in particular SR-DDS and / or ISFI, according to the present invention, thus enables reliable prolonged and / or sustained release of the active agent for efficient long-term treatment of diseases and / or dysfunctions of the urogenital tract and / or in particular the urinary bladder. Advantageously in this regard, it is overall ensured that in total the entire amount of active agent is released from the DDS, in particular SR- DDS and / or ISFI, according to the present invention, in the course of its lifespan, i.e. once the DDS, in particular SR-DDS and / or ISFI, according to the present invention, degraded completely, the entire amount of active agent will be released into the urinary bladder, such that precise dosing is well possible in the context of the present invention.

[0171] Further in the context of the present invention it proved well, if the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta- 3 agonists, in particular Mirabegron; and mixtures thereof.

[0172] Especially, it is envisaged that the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0173] Particularly good results are obtained, if the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and if the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0174] For the listed active agents, it is advantageously found, that these display an improved effectiveness when applied locally and / or site specifically to the target site, in this case the urinary bladder, since metabolic processes influencing the active agents can be excluded in the context of the present invention. Therefore, the listed active agent proved particularly suitable for integration into the composition in particular DDS, in particular SR-DDS and / or ISFI, according to the present invention, which accounts specifically for the last-mentioned active agents in combination with the respective indications.

[0175] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in situ- forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular drug delivery system as previously described, wherein the drug delivery system comprises or at least essentially consists of

[0176] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof;

[0177] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; especially wherein the drug delivery system is formed in situ in a urinary bladder to be treated.

[0178] For advantages and beneficial technical effects with respect to this preferred embodiment of the present invention, reference is made to the specifications above, which apply likewise with respect to the preferred DDSs according to the present invention stated above.

[0179] According to a very preferred embodiment of the present invention it is envisioned that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent is oxybutynin as well as salts and esters thereof.

[0180] Even more preferably it is the case that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent is oxybutynin as well as salts and esters thereof. The advantages of the DDS, in particular SR-DDS and / or ISFI, according to the present invention, are specifically pronounced for the aforementioned preferred embodiments of the present invention.

[0181] It further proved particularly well, if the drug delivery system comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1.5 to 1 : 500, preferably in a range of from 1 : 1.75 to 1 : 200, more preferably in a range of from 1 : 2 to 1 : 50, particularly based on the weight percentage of the respective components (i.e. active agent and polymer).

[0182] Ratios of active agent and polymer in the aforementioned regions advantageously ensure a particularly beneficial release pattern for the active agent from the DDS, in particular SR-DDS and / or ISFI, according to the present invention, which contributes especially to effective treatment of the indications envisioned to be addressed by means of the present invention.

[0183] It proved further advantageous if the drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI), comprises or at least essentially consists of a solution containing in addition to the components (a) and (b)

[0184] (d) at least one, particularly physiologically compatible and / or physiologically tolerable, adjuvant, in particular selected from the group consisting of pH- adjusting agents, surfactants, coagulants, wetting agents, excipients and mixtures thereof, preferably selected from pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids and / or acidic amino acids, amine sugars, in particular derived from aldohexoses, physiologically compatible and / or physiologically tolerable organic and / or inorganic acids and / or basis, and mixtures thereof.

[0185] Particularly preferred in the context of the present invention is the use of alkaline amino acids like lysine, arginine or histidine, especially lysine, as adjuvants. Likewise preferred is the use of amine sugars, in particular derived from aldohexoses, specifically such as meglumine, dimethyl meglumine, glucosamine, galactosamine, mannosamine and mixtures thereof, preferably meglumine, dimethyl meglumine and mixtures thereof. Thus it proved well, if pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids, are selected from the group consisting of lysine, arginine, histidine or mixtures thereof, in particular lysine, and / or wherein pH-adjusting agents and / or excipients selected from the group consisting of amine sugars, in particular derived from aldohexoses, are selected from the group consisting of meglumine, dimethyl meglumine, glucosamine, galactosamine, mannosamine and mixtures thereof, preferably meglumine, dimethyl meglumine and mixtures thereof.

[0186] These adjuvants advantageously allow for controlled and specifically tailored release of the active agent from the DDS, SR_DDS or ISFI, respectively, according to the invention. In particular, it is possible to adjust the speed or rate, with which the active agent is released from the drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI). As such, the use of adjuvants allows to further tune and tailor the respective characteristics with regard to drug release.

[0187] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to a drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in situ- forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular drug delivery system as previously described, wherein the drug delivery system is obtained from a composition as described herein before, in particular wherein the drug delivery system is obtained from the composition as described herein before via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated.

[0188] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect. The present invention - according to a s e v e n t h aspect of the present invention - further relates to the use of a drug delivery system as previously described herein for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0189] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0190] The present invention - according to a e i g h t h aspect of the present invention - further relates to the use of a drug delivery system as previously described herein for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0191] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0192] The present invention - according to an n i n t h aspect of the present invention - further relates to a method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder, wherein a drug delivery system as previously described herein is intravesically, preferably via instillation by means of a catheterizing device (catheter), formed in the urinary bladder of a subject in need thereof

[0193] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect. The present invention - according to a t e n t h aspect of the present invention - further relates to an application device, in particular syringe, preferably ready-to-use piston syringe, comprising a composition, especially pharmaceutical composition, as previously described herein.

[0194] According to the present aspect, by means of a preferred embodiment, the present invention as well relates to an application device, in particular syringe, preferably ready-to-use piston syringe, comprising a composition, especially pharmaceutical composition, in particular a composition as previously described herein, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing

[0195] (a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;

[0196] (b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));

[0197] (c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0198] In the context of the present invention, it further proved well if the application device is a syringe, preferably a ready-to-use piston syringe, and / or if the application device has a volume in a range of from 2 ml to 25 ml; and / or if the application device comprises the composition in an amount in a range of from 2 ml to 25 ml.

[0199] It may be further preferred, that the application device is a dual chamber-syringe. Alternatively, it may also be that the composition of the invention is applied in two separate syringes, i.e. that the application device is composed of two syringes, in particular wherein the two syringes, specifically for and / or while application of the composition, are connected by means of an adapter device particularly configured for mixing the components of the composition for application.

[0200] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0201] The present invention - according to an e l e v e n t h aspect of the present invention - further relates to a packaging unit comprising at least one pack and at least one application device as previously described herein, wherein the application device is inserted into the pack and / or is present in the pack. For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0202] The present invention - according to a t w e l f t h aspect of the present invention - further relates to a kit-of-parts comprising an instillation system, wherein the instillation system comprises

[0203] (i) at least one composition for intravesical application into the urinary bladder as previously described herein, present in an application device as previously described herein;

[0204] (ii) at least one catheterizing device (catheter) connectable to the application device; and

[0205] (iii) at least one instillation manual comprising application instructions.

[0206] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0207] The present invention - according to a t h i r t e e n t h aspect of the present invention - further relates to an active agent (active ingredient), particularly pharmaceutical active ingredient (API), for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder; and wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is applied to a urinary bladder to be treated via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in s / Yu-formed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, wherein the in s / Yu-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; and wherein the at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is not miscible with urine and / or is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co- glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic- co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)).

[0208] Thus, the present invention advantageously provides an active agent tailored for long-term application in the urinary bladder for prophylactic or curative treatment of diseases or dysfunctions of the urogenital tract, wherein the active agent displays a comparably improved effectiveness over regular, e.g. systemic, application. This can advantageously be attributed to the application design of the active agent as a component within a DDS, in particular SR-DDS or ISFI, which provides for sustained release of the active agent on the one hand, and on the other hand allows for site- directed application of the active agent specifically to the urinary bladder. Further by means of the application design, gentle application with less frequency compared to methods currently available without the need of active removal of the DDS, in particular SR-DDS or ISFI, can beneficially be ensured such that overall significant relief can be achieved for those patients who rely on frequent and in particular multiple times per day repeated treatment of their respective diseases and / or e.g. neurogenic dysfunctions of the urogenital tract.

[0209] Preferably it is envisioned in the context of the present invention that the drug delivery system is obtained from a composition as previously described herein, in particular wherein the drug delivery system is obtained from the composition as previously described herein via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated.

[0210] Further, it proved well in the context of the present invention, if the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0211] Also, it is preferably the case that the drug delivery system (DDS), particularly the sustained-release drug delivery system (SR-DDS), preferably the in s / Yu-forming implant (ISFI), is configured for and / or is capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours, in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard. Particularly good results are obtained in the context of the present invention, if the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta- 3 agonists, in particular Mirabegron; and mixtures thereof.

[0212] Especially, it proved well if the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0213] According to a preferred embodiment of the present invention it is envisioned, that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

[0214] According to the present aspect, by means of a preferred embodiment, the present invention in view of the above as well relates to an active agent (active ingredient), particularly pharmaceutical active ingredient (API), for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular active agent as previously described herein, wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof, and is applied to a urinary bladder to be treated via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in s / Yu-formed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, wherein the in s / Yu-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; wherein the at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is not miscible with urine and / or is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co- glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic- co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)). Further preferably it is further envisioned that the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and that the active agent is oxybutynin as well as salts and esters thereof.

[0215] It proved particularly well if the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is oxybutynin as well as salts and esters thereof.

[0216] In the context of the present invention, it is particularly preferred if the active agent is contained in a composition as previously described herein, and / or if the active agent is contained in a drug delivery system obtained from a composition as previously described herein, in particular wherein the drug delivery system is obtained from the composition as previously described herein via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated; and / or if the active agent is contained in a drug delivery system as previously described herein.

[0217] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0218] The present invention - according to a f o u r t e e n t h aspect of the present invention - further relates to the use of an active agent as previously described herein for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0219] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0220] The present invention - according to a f i f t e e n t h aspect of the present invention - further relates to the use of an active agent as previously described herein for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

[0221] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect. The present invention - according to a s i x t e e n t h aspect of the present invention - further relates to a method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder, wherein an active agent as previously described herein is intravesically, preferably via instillation by means of a catheterizing device (catheter), applied into the urinary bladder of a subject in need thereof via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in s / Yu-formed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, wherein the in s / Yu-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three- dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent.

[0222] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect. The present invention - according to a s e v e n t e e n t h aspect of the present invention - further relates to the use of a composition, especially pharmaceutical composition, for intravesical application of at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); and at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

[0223] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0224] Finally, the present invention - according to an e i g h t e e n t h aspect of the present invention - further relates to the methods and uses as previously described herein, wherein the methods and uses each are characterized by one or more of the features of the composition as previously described herein.

[0225] For more details as well as advantages and technically beneficial features in relation with this aspect of the present invention, reference is also made to the specifications relating to the further aspects of the present invention, which apply accordingly with respect to the present aspect.

[0226] Further configurations, modifications and variations and also advantages of the present invention are readily identifiable and realizable for a person skilled in the art upon reading the description, without said person departing from the scope of the present invention while doing so.

[0227] The following figures and exemplary embodiments serve to illustrate the present invention and associated advantages further, without restricting the present invention thereto.

[0228] It is shown in

[0229] Fig. 1 A-D Viscosities of compositions according to the invention with a polymer load of 15 wt.% and 30 wt.% and a varying active agent load (0 wt.%, 1 .5 wt.%, 3 wt.%, 7.5 wt.% and 15 wt.%). Fig. 1 A shows compositions with PLGA polymer type RG 502 and GF as solvent. Fig. 1 B shows compositions with PLGA polymer type RG 502H and GF as solvent. Fig. 1 C and 1 D show viscosity measurements for solutions with PLGA polymer type RG 502 and PC as solvent, and PLGA polymer type RG 502H with PC as solvent;

[0230] Fig. 2 A-D Proportions of drug released over 7 d for different compositions according to the invention with PLGA type RG 502 as polymer, a polymer load of 30 wt.%, GF as solvent and different active agent contents, varying between 1.5 wt.% and 15 wt.%, in artificial urine with a pH of 6 (Fig. 2A), evaluation of the initial release after 1 d and the final amount of released drug after 7 d (Fig. 2B), the content of lactic acid in the release medium over 7 d (Fig. 2C), and a comparison of the compositions regarding their final content of lactic acid correlated to the amount of lactic acid per g PLGA (Fig. 2D);

[0231] Fig. 3 A-D Proportions of drug released over 7 d for different compositions according to the invention with PLGA type RG 502 as polymer, a polymer load of 30 wt.%, GF as solvent, an active agent contents of 7.5 wt.%, in artificial urine with a pH of 4, 6 or 8 (Fig. 3A), evaluation of the initial release after 1 d and the final amount of released drug after 7 d (Fig. 3B), the content of lactic acid in the release medium over 7 d (Fig. 3C), and a comparison of the compositions regarding their final content of lactic acid correlated to the amount of lactic acid per g PLGA (Fig. 3D);

[0232] Fig. 4 A-D Proportions of drug released over 7 d for different compositions according to the invention with PLGA type RG 502 or RG 502H as polymers, a polymer load of 30 wt.%, GF or PC as solvent, an active agent contents of 7.5 wt.%, in artificial urine with a pH of 6 (Fig. 4A), evaluation of the initial release after 1 d and the final amount of released drug after 7 d (Fig. 4B), the content of lactic acid in the release medium over 7 d (Fig. 4C), and a comparison of the compositions regarding their final content of lactic acid correlated to the amount of lactic acid per g PLGA (Fig. 4D); Fig. 5 A-D Proportions of drug released over 7 d for different compositions according to the invention with PLGA type RG 502 or RG 502H as polymers, a polymer load of 30 wt.%, GF as solvent, an active agent contents of 15 wt.%, in artificial urine with a pH of 6 (Fig. 5A), evaluation of the initial release after 1 d and the final amount of released drug after 7 d (Fig. 5 B ) , the content of lactic acid in the release medium over 7 d (Fig. 5C), and a comparison of the compositions regarding their final content of lactic acid correlated to the amount of lactic acid per g PLGA (Fig. 5D);

[0233] Fig. 6 A / B Proportions of solvent released over 7 d for different compositions according to the invention with PLGA type RG 502 and RG 502H as polymers, a polymer load of 30 wt.%, GF or PC as solvent, an active agent contents of 1.5 wt.%, 5 wt.%, and 7.5 wt.%, in artificial urine with a pH of 6 (Fig. 6A and 6B).

[0234] Examples:

[0235] A. Material and Methods:

[0236] 1. Materials

[0237] Oxybutynin hydrochloride was obtained from Klosterfrau Healthcare Group (Berlin, Germany). Poly(lactic-co-glycolide acid) copolymers (PLGA, ratio of first monomer : second monomer 50 : 50) with the tradenames Resomer® RG 502 and Resomer® RG 502H, respectively, were obtained from Evonik AG (Ingelheim, Germany). Glycofurol (tetrahydrofurfuryl alcohol polyethylene glycol ether, GF), urea, sodium chloride, lactic acid and hydrochloric acid were obtained from Sigma Aldrich (Steinheim, Germany). T ri-sodium phosphate dodecahydrate was obtained from Carl Roth (Karlsruhe, Germany). Propylene carbonate (PC) was obtained from Acros Organics (Geel, Belgium). Triethylamine (TEA) and acetonitrile were obtained from Fisher Chemicals (Schwerte, Germany). Orthophosphoric acid was obtained from Th. Geyer GmbH & Co. KG (Renningen, Germany). Chemicals used for the preparation of compositions according to the invention and related buffers or the like were of analytical grade or higher.

[0238] 2. Preparation of the active agent

[0239] Oxybutynin is used as exemplary active agent in the exemplary, preferred embodiments of compositions according to the present invention. More specifically, oxybutynin is applied in the form of the free base, i.e. in its molecular form as such, in the preferred embodiment of the composition according to the present invention.

[0240] To obtain oxybutynin in its free form as such, oxybutynin hydrochloride was dissolved under stirring in ultra-pure water (MilliQ). After adding sodium hydroxide and adjusting the oxybutynin hydrochloride solution to a pH of 10, the free base of oxybutynin precipitated. The active agent was extracted by means of a separating funnel and chloroform as solvent for oxybutynin base. Chloroform was removed under reduced pressure (rotary evaporator, 48 °C, 600-650 mbar) and the obtained crude oxybutynin dried in vacuum at 40 °C for 24 h. 3. Preparation of compositions according to the invention

[0241] For the preparation of compositions according to the present invention, oxybutynin base was dissolved under continuous stirring in GF or PC for 24 h. To the solution, Resomer® RG 502 or Resomer® RG 502H was added, and the composition was stirred further for 24 h. Finally, the solution was ultrasonicated for 2 h.

[0242] Amounts of oxybutynin used, were 1 .5 wt.%, 3.0 wt.%, 7.5 wt.% and 15 wt.%, based on the total composition.

[0243] Amounts of Resomer® RG 502 or Resomer® RG 502H used, were 30 wt.% and 15 wt.%, based on the total composition.

[0244] 4. Viscosity of compositions according to the invention

[0245] Viscosity measurements were performed by means of rotational viscometry, preferably in accordance with ISO 3219 of 2021 . Used was the rotational viscometer MCR92 from Anton Paar (Graz, Austria). The compositions prepared according to section 3. were analyzed with a cone-plate (CP-50-1 ) measuring device. The plate had a diameter of 49.965 mm and the cone angle was 1.001°. Solutions were analyzed at a plate temperature of 25 °C. With a cone truncation of 0.097 mm the shear rate was increased from 1 s’1to 200 s’1, where the final viscosity was measured.

[0246] 5. In-Vitro active agent release testing from polymer matrix after application of the composition to urine

[0247] The release of the active agent from the compositions was assessed using a shaking bath at a temperature of 37 °C to mimic the temperature inside a urinary bladder. Compositions according to the invention as prepared under section 3. were injected into glass vials containing 20 mL freshly prepared artificial urine as release medium. Upon injection, the compositions formed a three-dimensional matrix, in which the active agent was entrapped and / or embedded, especially encapsulated. Specifically, the composition underwent in s / Yu-formation of a drug delivery system (DDS), particularly configured for sustained drug release, thus constituting a SR-DDS, and preferably constituting in s / Yu-forming implants (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release. The artificial urine consisted of 24.25 g / L urea, 16.1 g / L sodium chloride, 14.84 g / L tris sodium phosphate dodecahydrate. The pH of the obtained solution was adjusted to pH 4.0, pH 6.0 and pH 8.0, each via addition of respective amounts of hydrochloric acid.

[0248] From the glass vials comprising the compositions according to the present invention and artificial urine, samples of 0.4 mL were taken after the following specific points of time: 1 h, 2 h, 4 h, 8 h, 12 h, 24 h, and after that daily. The respective samples were analyzed by HPLC regarding active agent release, polymer matrix degradation and overall behavior of the DDS.

[0249] In the glass vials, the volume removed for sampling was replaced with new release medium. After the daily sample was collected, the complete release medium was replaced with fresh artificial urine to simulate one urination per day.

[0250] 6. Degradation of PLGA

[0251] The release medium collected daily from the active agent release test samples was analyzed for lactic acid by means of HPLC. Therefore, the pH of the release medium was adjusted with 1 mL concentrated hydrochloric acid to ensure that the lactic acid was present in monomeric form. To increase the degradation of lactic acid oligomers or PLGA-microparticles, that were formed upon injection of the compositions according to the invention into the artificial urine, the samples were stored for 5 days at an elevated temperature of 60 °C. Subsequently, the samples were analyzed for lactic acid content using a HPLC.

[0252] 7. High-Performance Liquid Chromatography (HPLC) analysis

[0253] High performance liquid chromatography (HPLC) analysis for contents of oxybutynin released from the polymer matrix and lactic acid originating from polymer matrix degradation were performed on a Shimadzu, LC-2030C 3D Plus (Kyoto, Japan) as reversed-phase (RP) chromatography on an RP18-column (LiChrospher 100 RP 18- 5 p EC, 250 x 4.6 mm) with a RP18 pre-column (LiChrospher 100 RP 18-5 p EC, 10 x 4 mm). Active agent detection was performed by means of UV-detection at 203 nm. The column temperature was set to 40 °C.

[0254] For oxybutynin, the mobile phase was composed of ultra-pure water with 0.2 vol.% TEA and adjusted to a pH of 3.0 with ortho-phosphoric acid, and acetonitrile in a ration of 40 : 60 vol.%). Elution was performed with an isocratic flow of 1 .0 mL / min. The sample size injected was 10 pL. Analysis of lactic acid contents was performed with ultra-pure water (plus 0.2 vol.% TEA, adjusted to a pH of 3.0 with ortho phosphoric acid). The flow rate was set to 0.7 mL / min and the injected sample volume was 30 pL.

[0255] 8. Gas Chromatography (GC)

[0256] Gas chromatography (GC) analysis was performed on both PC and GF samples using an Agilent 6890N gas chromatograph equipped with an Agilent 7683 auto sampler. The analysis was performed on a FS-CS-624 30 m x 0.25 mm ID x 1 .8 pm capillary column as stationary phase, and with a constant nitrogen flow of 2 mL / min as carrier gas. Detection was performed via flame ionization at 270 °C.

[0257] For the analysis of PC, the initial oven temperature was set to 80 °C for 1.5 min. Successively, the temperature was increased by 10 °C / min until it reached 200 °C, with a total run time of 13.5 minutes. The injector was set to 270 °C and a volume of 0.2 pL was injected each run. The injector operated in split-less mode with a purge time of 1 .7 minutes.

[0258] For the analysis of GF, the initial oven temperature of 80 °C was maintained for 1.5 minutes before increasing by 10 °C / min to 150 °C. This temperature was maintained for 5 minutes before rising by 5 °C / min to 200 °C, which was maintained for 20 minutes. Finally, the temperature was increased by 20 °C / min to 235 °C for an additional 8 minutes and a total run time of 53.25 minutes. The injector was set to 250 °C and a volume of 0.2 pL was injected each run. The injector operated in splitless mode with a purge time of 1 .3 minutes.

[0259] 9. Statistical evaluation

[0260] Examples were conducted at least as triplicate. GraphPad Prism 8 software was used for the statistical analysis for significance. For the analysis a Mann-Whitney U test and a Kruskal-Wallis-Dunn test were performed. It was considered a significant difference if p < 0.05 and very significant if p < 0.01 , marked with either one or two asterisks. B. Results and Discussion:

[0261] 1. Viscosity of compositions according to the invention (see Fig. 1a to 1D)

[0262] For compositions with GF, a decrease in viscosity with increasing amount of active agent was observed, independent of the polymer used.

[0263] A difference in viscosity could further be seen with a change in PLGA type, as seen for sample “502 GF 30 / 0” (comprising 30 wt.% Resomer® RG 502 in GF) with a viscosity of 517.18 mPa*s + / - 17.11 mPa*s compared to sample “502H GF 30 / 0” (comprising 30 wt.% Resomer® RG 502H in GF) with 976.75 mPa*s + / -13.58 mPa*s.

[0264] A decrease in viscosity was observed up to an active agent loading of 7.5 wt.%, with 199.73 mPa*s + / - 0.30 mPa*s for sample “502 GF 30 / 7.5” (comprising 30 wt.% Resomer® RG 502 and 7.5 wt.% active agent in GF) and 437.21 mPa*s + / - 0.53 mPa*s for “502H GF 30 / 7.5” (comprising 30 wt.% Resomer® RG 502H and 7.5 wt.% active agent in GF). No lower viscosity was measured when the amount of active agent was further increased to 15 %.

[0265] Formulations with PC as solvent showed a different behavior regarding their viscosity with increasing active agent load. No difference was observed between PLGA types 502 and 502H, as the viscosity for sample “502 PC 30 / 0” (comprising 30 wt.% Resomer® RG 502 in PC) was 192.40 mPa*s + / - 0.23 mPa*s and for sample “502H PC 30 / 0” (comprising 30 wt.% Resomer® RG 502H in PC) was 242.86 mPa*s + / - 0.39 mPa*s. Increasing the amount of active agent from 0 wt.% to 7.5 wt.% did not affect the viscosity of these formulations, see values of 206.91 mPa*s + / -1.34 mPa*s for sample “502 PC 30 / 7.5” (comprising 30 wt.% Resomer® RG 502 and 7.5 wt.% active agent in PC) and 242.67 mPa*s + / - 1.90 mPa*s for sample “502H PC 30 / 7.5” (comprising 30 wt.% Resomer® RG 502 and 7.5 wt.% active agent in PC). Increasing the amount of active agent to 15 wt.% did not change the viscosity, regardless of the PLGA grade.

[0266] Decreasing the polymer content from 30 wt.% to 15 wt.%, decreased the viscosity, but varying the amount of active agent did not increase or decrease the viscosity. 2. Influence of different active agent-loads (see Fig. 2a to 2D)

[0267] Drug release (i.e. release of the active agent) and lactic acid content tests of different drug delivery systems (DDS), specifically in the form of in s / Yu-forming implants (ISFI), formed from the prepared compositions with increasing active agent loading were performed in artificial urine at pH 6 as shown in Figure 2. Assuming burst release, the DDSs showed a significant difference between drug loading of 3 wt.% and 7.5 wt.% (proportions of 27.12 % + / - 2.39 % to 41.64 % + / - 2.66 % of drug released in the release medium), but there was no significant increase in the released drug content in the artificial urine above an active agent content of 7.5 wt.%. The final amount of active agent released increases with the active agent content in the composition, and a significant difference (46.90 % + / - 1.87 % and 72.96 % + / - 2.28 % released oxybutynin as active agent) was measured between 1 .5 wt.% and 7.5 wt.%. With a further increase in active agent content, the total amount of active agent released did not increase significantly. All release profiles showed a logarithmic curve progression.

[0268] In contrast, an increase in drug load resulted in a higher lactic acid content in the artificial urine, which is related to the degraded mass of PLGA in the ISFI-composition but is no longer visible above a certain active agent load. With a linear curve progression, the highest lactic acid amount measured was 33.29 % + / - 3.74 % after 7 d for the ISFI-compositions with a drug load of 15 wt.%. A significant difference was found between 1.5 wt.% and 15 wt.% as well as 3 wt.% and 15 wt.% (0 % + / - 0 % and 33.29 % + / -3.74 % lactic acid content).

[0269] 3. Influence of different pH of artificial urine (see Fig. 3A to 3D)

[0270] The pH of the release medium was changed to pH 4 and pH 8 for the formulation of a DDS, specifically ISFI, formed from a composition with PLGA type RG 502 as polymer, GF as solvent, a polymer load of 30 wt.% and an oxybutynin content of 7.5 wt.%. As described previously, the released amount of the active agent was measured, and in terms of initial release after 1 d there was a significant difference between pH 4 and pH 8 (48.68 % + / - 1.45 % versus 7.47 % + / - 0.61 % active agent released). This behavior was also observed for the cumulative amount of released oxybutynin, with 76.01 % + / - 1.64 % measured for pH 4 and 41.01 % + / - 6.37 % for pH 8 after 7 d. As a function of pH, the measured content of lactic acid released from PLGA increased significantly with higher pH, resulting in a total lactic acid content of 31.22 % + / - 1.67 % after 7 d for pH 8 compared to 6.40 % + / - 0.33 % at pH 4. 4. Influence of different solvent and polymer (see Fig. 4A to 4D)

[0271] Changing the solvent from GF to PC had no significant effect on oxybutynin release from DDS, specifically ISFI, regardless of the polymer. Nevertheless, a tendency to decrease the initial release is observed for samples “502 GF 30 / 7.5” and “502 PC 30 / 7.5” (oxybutynin release of 41.64 % + / - 2.66 % and 9.50 % + / - 0.10 %). A similar effect was also observed for PLGA type RG 502H polymer, where solvent exchange reduced the released amount of active agent from 34.85 % + / - 2.93 % for GF to 10.23 % + / - 0.16 % for PC after 1 d. Furthermore, the final amount of oxybutynin released was higher for the solutions with GF as solvent. For PLGA type RG 502 polymer, oxybutynin release decreased from 72.96 % + / - 2.28 % to 41.87 % + / - 1.97 %, and for PLGA type RG 502H polymer active agent release decreased from 71.16 % + / - 6.00 % to 53.72 % + / - 1.22 % with the replacement of GF with PC, but only a trend with non-significant differences was observed. An active agent release of 34.85 % + / - 2.93 % after 1 d was observed for the ISFI-composition with PLGA type RG 502H polymer and GF as solvent. In comparison, the ISFI-composition with PLGA type RG 502 polymer released 41.64 % + / - 2.66 % after the first day. This difference between the polymer types could not be observed for compositions with PC. A similarity between the two polymers in terms of release behavior of active agent was also evident from the curve in Fig. 4A.

[0272] 5. Influence of different polymer-load (see Fig. 5A to 5D)

[0273] Reducing the polymer content in ISFI-compositions according to the invention, regardless of the choice of polymer, had no significant effect on active agent release. However, a tendency of an increased active agent release could be observed by reducing the polymer content from 30 wt.% to 15 wt.% independent from the choice of polymer grade. Regarding the final measured amount of lactic acid released from the polymers, there was no significant increase or decrease from changing the polymer content notable.

[0274] 6. Release of solvent (see Fig. 6A and 6B)

[0275] The solvent release from ISFI-compositions for PC was initially high for all samples tested after 1 h and 1 d. After the first day, the content of released PC was almost 100 % for all DDSs formed from the compositions. There was no significant difference in solvent release with respect to PLGA type or active agent content. A correlation between solvent release and active agent release was not observed. Figure 6B showed that ISFI with 1.5 % active agent load and GF as solvent had a cumulative amount of solvent released of 27.80 % + / - 2.09 % (for PLAG type RG 502) and 42.60 % + / - 6.80 % (for PLGA type RG 502H) compared to the same formulations with PC as solvent that had a release of 80.42 % + / - 7.82 % (for PLGA type RG 502) and 64.39 % + / - 2.50 % (for PLGA type RG 502H) after 1 h. After 24 h, a GF contents of 72.76 % + / - 3.57 % (for PLGA type RG 502) and 78.05 % + / - 7.86 % (for PLGA type RG 502H) were found for the ISFI with an oxybutynin base content of 7.5 wt.%. At a lower active agent content of 1 .5 wt.% for PLGA polymer type RG 502, a lower amount of GF, 28.78 % + / - 2.60 % compared to 49.33 % + / - 2.82 % for PLGA polymer type 502H was detected in the release medium. After 7 d, a cumulative GF content of nearly 100 % was found for both formulations with 7.5 wt.% active agent content. In contrast, a release of 32.66 % + / - 3.16 % GF with PLGA polymer type RG 502 as polymer and 72.74 % + / - 0.71 % with PLGA polymer type 502H was observed for the ISFI with 1 .5 wt.% oxybutynin base. In addition, a higher amount of released active agent was observed in the formulations with a higher active agent content. In the two ISFI-formulations with a lower active agent content, a lower release of the active agent was observed in addition to the lower solvent released.

[0276] 7. Discussion of the obtained results

[0277] The drug release pattern of DDS, in particular SR-DDS, preferably ISFI, formed from compositions according to the invention is distinct, starting with a burst release, followed by zero-order release kinetics mainly due to API diffusion through the polymer matrix, concluded by an erosion process. The properties of the implant, by means of its configuration based on polymer variation, solvent, and API or polymer content, can significantly influence the drug release pattern. To show the feasibility of ISFI-use in the bladder, the polymer grade, active agent content, solvent, and polymer content was varied in the examples. Also, pH variation in the urinary bladder was mimicked by varying the pH between 4 and 8 in the release medium.

[0278] The behavior of ISFIs obtained from compositions according to the invention was tested for all formulations in a shaking bath setup. This setup was chosen since it is known that agitation conditions influence drug release. To assess the properties of the implants, the release of active agent, degradation of the polymer matrix, and release of the solvent were studied. These aspects have not been addressed before, specifically for a potential use of ISFI-compositions in a urinary bladder. DDS, in particular ISFI, can be characterized by several factors. One of these factors is the viscosity of the starting solutions. The viscosity affects the rate of implant formation and the release of drug and solvent. In the experiments, a higher viscosity resulted in a lower initial release of solvent as the implant structure solidified more quickly. In case of implants from PC-containing compositions according to the invention, there were no differences in viscosity when the concentration of the active agent or the type of polymer was changed. The viscosity changed in cases where the polymer content was reduced. For GF-containing compositions, oxybutynin as active agent was observed to have a plasticizing effect on respective implants. This effect is also observed for other drugs in polymer films. The effect ensures a high viscosity at low drug concentrations and, theoretically, a lower initial release. Accordingly, viscosity and mode of drug release can advantageously be adjusted by means of the solvent used as well as the amount of polymer present in compositions according to the present invention as well as ISFIs formed therefrom.

[0279] Oxybutynin, in its base form (i.e. molecular form as such), created an alkaline microclimate within the implant, which can catalyze the degradation of PLGA. Further, higher concentrations of the active substance in the implant resulted in an increased accumulation of the substance in the ISFI. The implant as a result degrades internally, leading to the formation of pores, voids or the like that increase the final release of the drug, regardless of the release medium. This occurred likewise for 1 .5 wt.% and 7.5 wt.% drug content. For these active agent loads, minor differences were observed for the initial drug release, wherein the differences were the result of differences in viscosity for the compositions and ISFI formed therefrom. The degradation reaction of PLGA to lactic acid and glycolic acid was catalyzed by the alkaline microclimate. Varying the pH of the release medium further accelerated the degradation reaction. There was no significant difference observed between pH 4 and pH 6, but an increase to pH 8 resulted in a further increase in implant degradation. At these pH values, which may also occur in human urine under extreme situations, degradation would be accelerated while release would be reduced. This is because the solubility of the active substance in the release medium is limited. Thus, it is an advantage of the present invention that by means of the choice of the active agent, in particular with regard to its molecular configuration, i.e. being present as the molecule as such, or as a pharmaceutically acceptable salt thereof, or being present comprising a chemical modification, e.g. as an ester or the like, the active agent release pattern of ISFI formed from compositions according to the invention can be influenced such that a faster or slower release of the active agent is achieved. Another factor for the formulation of an DDS, in particular an ISFI, for the treatment of e.g. overactive bladder is the chemical modification of the polymer. It was observed that ISFI with polymer Resomer RG 502 and GF as solvent showed a significant higher initial drug release rate compared to ISFI with Resomer RG 502H in GF. Further, it could generally be observed that drug release for the ISFI with PLGA polymer type 502H was significantly higher regardless of the solvent chosen. This indicated that polymer degradation does not determine the rate of drug released from the implant. Rather, it was concluded that the rate-determining step is a drug release through the polymer matrix by diffusion. Therefore, an increase in polymer degradation does not necessarily result in a significant increase in drug release. Hence, advantageously, the choice of the polymer can positively influence a high initial release of active agent, which may be favorable in cases where acute therapy, initiated by means of a comparably high stating dose of an active agent, is sought. Likewise, drug release can be adjusted such, that a balanced or continuous release of active agent is achieved which may in particular be advantageous in the treatment of chronic conditions or neurogenic disorders.

[0280] Altering the solvent resulted in a modification of both the active agent release and polymer degradation rates. PC is a polar solvent. In contrast to GF, which is also a polar solvent, PC does not comprise OH-groups that could for example form hydrogen bonds or interact with other OH-groups. PLGA and oxybutynin have chemical groups to undergo hydrogen bonding. It was observed that ISFI with PC had a higher initial amount of solvent released, independent of active agent load and polymer grade. In contrast, ISFI-compositions with GF initially released less solvent which further depended on the drug content of the ISFI-composition. An explanation for this behavior could be that PC does not form hydrogen bonds with PLGA and oxybutynin and therefore is released with a higher amount than GF, which could interact more with PLGA and the API, due the formation of hydrogen bonds.

[0281] In the experiments, a tendency could be seen that ISFI with PC released less API initially as well as after 7 days in total, compared to ISFI with GF as solvent. In addition to that the degradation of ISFI formed from compositions with PC was higher than for ISFI from compositions with GF. Without wishing to be bound to any specific theory, a reason for this could be that, due to the missing formation of hydrogen bonds and interaction between PC and oxybutynin, the active agent might have a lower tendency to diffuse with the solvent through the polymer matrix into the release medium. Instead, it remained in the ISFI, which decreased the initial release. The higher interaction between the polymer and GF could be a reason for the lower solvent release after 1 h compared to ISFI with PC. The higher initial release of the active agent on the other hand could be due to the fact that oxybutynin interacts with GF and thus a higher amount of API diffuses with the solvent through the polymer matrix into the artificial urine. An influence of the viscosity could also be observed in the rate of solvent release. Here, a higher viscosity should lead to a lower initial drug release, which is also connected to the time until the implant solidifies after injection into the aqueous phase. A significant difference between active agent loads of 7.5 wt.% and 1.5 wt.% for the GF release could be observed, but not for the PC release. That is due to the fact that for ISFI-compositions with PC no viscosity increase or decrease was measured after a change in active agent load. With a higher solvent release and a lower initial release, ISFI with PC also were characterized by a higher degradation rate than implants with GF.

[0282] Further, it was observed that a higher amount of oxybutynin (base) could be dissolved in GF compared to PC. This leads to the assumption that a high solvent release within a range of from 70 % to 80 % of PC within 1 h causes a supersaturation of the implant with the active agent, which results in the precipitation of the active agent in the implant. In addition, a diffusion of the release medium through the created pores in the polymer matrix of the ISFI would result in creation of an alkaline microclimate inside the ISFI. This accelerated and increased degradation of ISFI based on compositions with PC compared to ISFI with GF. With an increase in drug load, the amount of precipitated drug rises, which leads to more possible areas with an alkaline microclimate.

[0283] On the other hand, ISFIs with GF are characterized by a higher initial release of the API but a lower solvent release and degradation rate. As before described, the higher viscosity leads to a lower solvent and drug release, resulting in a higher amount of API being dissolved in the solvent inside the polymer matrix. The dissolved active agent has a higher affinity for the solvent than for the release medium penetrating into the ISFI, such that the active agent does not precipitate as fast as in ISFI with PC, resulting in a slower degradation rate and lower final amount of measured lactic acid in the artificial urine.

[0284] ISFI-compositions based on PC with a higher active agent content had a lower viscosity, resulting in a higher initial drug release and solvent release, compared to the ISFI with GF and 1 .5 wt.% active agent. A consequence is the oversaturation and later precipitation of the API in the ISFI, which is another reason for a higher polymer degradation with increasing drug content. The impact of the higher initial release of the API in ISFI with GF could be another reason for the lower degradation of the implants, compared to ISFI with PC, because in total more active agent is released, which thus is no longer available for accelerating the degradation process. The reduction in polymer content affects the release and degradation rates to a less significant but noticeable extent, although it did cause a decrease in viscosity and a tendency of an increased initial release was visible. In contrast, the degradation was not influenced by the polymer content reduction. It is important to note that the degradation of PLGA is not solely determined by basic catalysis, but also by autocatalysis, which is dependent on the amount of lactic acid and glycolic acid present. The presence of these components on site accelerates the degradation process. The results show that the amount of lactic acid per gram of PLGA is consistent across all tested ISFI solutions. This indicates that the degradation and release of the active agent is influenced not only by viscosity, concentration of active agent, solvent, pH value of the release medium, choice of polymer, and interaction between the solvent and the API of polymer, but also by the amount of lactic acid present.

[0285] Accordingly, by means of the solvent in combination with the active agent and the polymer used, degradation of ISFI formed from inventive compositions can be adjusted and tuned, in particular vis-a-vis specific needs or requirements. For example, if an ISFI with a particular long-term stability and a pronounced initial drug release, followed by flattened continuous drug release, is envisioned, a combination of polar, hydrogen bond-forming solvent, chemically modified and thus stabilized polymer and moderate amounts of active agent could be chosen. On the other hand, if an ISFI with a rather short-termed lifespan is envisioned, a combination of polar, aprotic solvent, unmodified or acid modified polymer and comparably high amounts of active agent would be advantageous. Accordingly, be means of the present invention, DDSs which can be tailored to specific need in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder can advantageously be presented.

[0286] Comparable studies were carried out using poly(lactic-co-glycolide acid) copolymers with the tradenames Resomer® RG 503H and Resomer® RG 504H. Further comparable studies were carried out with compositions comprising meglumine as adjuvant. The studies gave similar results to those discussed above. Specifically, it was again confirmed that viscosity and drug release rate as well as the drug release profile can be tailored and further controlled by means of the polymer, in particular by means of the molecular weight and / or viscosity of the polymer, as well as by means of the addition of adjuvants. Specifically, the adjuvant meglumine allowed for an increase of the drug release rate, such that the use of adjuvants proved as a suited means for demand-oriented tailoring of the properties of DDS, SR-DDS or ISFI, respectively, according to the invention. Herein, it is believed, without wishing to be bound to this theory, that adjuvants like meglumine contribute to a local alkaline environment that assists in accelerated decomposition of the polymer matrix of the DDS, SR-DDS or ISFI, respectively. Overall, the inventive concept is thus characterized by a great flexibility and adaptability in orientation with specific or individual disease- or disfunction-related needs.

[0287] 8. Conclusions

[0288] Inventive DDSs or ISFIs, respectively, that contain the biodegradable polymer PLGA were proven as method of drug delivery over a sustained period of time, in particular due to their low release and degradation rate, especially wherein the properties of ISFI can be adjusted based on the components of compositions according to the invention. The investigated ISFIs and respective compositions, from which the ISFI are obtained, constitute an alternative to the current treatment of e.g. NDO, which at the moment involves a single catheterization per day with the possibility of up to five applications per day. Advantageous drug release rates and polymer degradation rates were observed by adding oxybutynin as such to the studied compositions. The solvent PC promoted formation of an alkaline microclimate due to drug precipitation in the implant. When combined with a polymer such as PLGA type Resomer RG 502H, which has a free acid as an end group, the polymer degradation rate could be further increased without affecting drug release, in particular by means of chemical modification of the polymer. The pH value of the artificial urine as a release medium had a minor influence on drug release at pH values of 4 and 6. Higher urine pH values are likely to lead to lower drug release at a higher degradation rate.

[0289] Overall, a preferred formulation for the treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder can for example consist of a high content of active agent, PC as solvent and PLGA type Resomer RG 502H, due to a low burst release and enhanced polymer degradation rate. ISFI-compositions with PLGA constitute a beneficial alternative to current medications of e.g. NDO therapy. Specifically, it becomes apparent from the examples above, that the drug and / or active agent release pattern as well as the polymer degradation mechanism can be adjusted by the choice of solvent, polymer and active agent in the compositions according to the invention.

Claims

Claims:

1. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine;wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time (i.e. especially if compared to a drug delivery without polymer and / or if compared to the application of the active agent as such) and / or by diffusion-controlled release.

2. Composition according to claim 1 , wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

3. Composition according to claim 1 or 2, wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, at least 35 %, in particular at least 45 %, preferably at least 55 %, more preferably at least 60 %, of the active agent contained in the composition; and / orwherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, up to 100 %, in particular up to 98 %, preferably up to 95 %, more preferably up 93 %, of the active agent contained in the composition; and / or wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, 35 % to 100 %, in particular 45 % to 98 %, preferably 55 % to 95 %, more preferably 60 % to 93 %, of the active agent contained in the composition; in particular wherein the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, is determined by means of injecting the composition into artificial urine, taking a sample of the composition immediately after injection, analyzing the proportion of free and / or non-entrapped and / or non-embedded, especially non-encapsulated, active agent, especially by means of HPLC with adequate detection, in particular UV- detection, against a respective active agent-standard, and calculating the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three- dimensional aggregates and / or agglomerates, based on the proportion of free and / or non-entrapped and / or non-embedded, especially non-encapsulated, active agent.

4. Composition according to one of the preceding claims, wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent is formed within a time period of at most 45 minutes, in particular of at most 35 minutes, preferably of at most 25 minutes, more preferably of at most 20 minutes, after the composition has been contacted with urine present in the urinary bladder; and / or wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent is formed within a timeperiod of from 0.01 seconds to 45 minutes, in particular within a time period of from 0.05 seconds to 35 minutes, preferably within a time period of from 0.1 seconds to 25 minutes, more preferably within a time period of from 0.2 seconds to 20 minutes, after the composition has been contacted with urine present in the urinary bladder.

5. Composition according to one of the preceding claims, wherein the composition undergoing in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI ), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, releases the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

6. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, whereby the composition undergoes in situ- formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / tu-forming implant (ISFI), configured for and / or capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours;in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

7. Composition according to one of the preceding claims, wherein the composition comprises one (single) continuous phase and / or is monophasic and / or is composed of a single phase; and / or wherein the composition is not multiphasic, in particular is not biphasic, and / or is not composed of more than one phase.

8. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution, in particular continuously phased and / or monophasic and / or single phased solution, containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting ofmatrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, whereby the composition undergoes in situ- formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / tu-forming implant (ISFI), configured for and / or capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, in particular UV-detection, against a respective active agent-standard, andcalculating the proportion of released active agent vis-a-vis the standard; and / or wherein the three-dimensional matrix, in particular the three-dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, at least 35 %, in particular at least 45 %, preferably at least 55 %, more preferably at least 60 %, of the active agent contained in the composition, and / or comprises and / or entraps and / or embeds, especially encapsulates, up to 100 %, in particular up to 98 %, preferably up to 95 %, more preferably up 93 %, of the active agent contained in the composition; in particular wherein the three-dimensional matrix, in particular the three- dimensional aggregates and / or agglomerates, comprises and / or entraps and / or embeds, especially encapsulates, 35 % to 100 %, in particular 45 % to 98 %, preferably 55 % to 95 %, more preferably 60 % to 93 %, of the active agent contained in the composition; preferably wherein the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, is determined by means of injecting the composition into artificial urine, taking a sample of the composition immediately after injection, analyzing the proportion of free and / or non-entrapped and / or non-embedded, especially non-encapsulated, active agent, especially by means of HPLC with adequate detection, in particular UV- detection, against a respective active agent-standard, and calculating the proportion of active agent comprised and / or entrapped and / or embedded, especially encapsulated, in the three-dimensional matrix, in particular three- dimensional aggregates and / or agglomerates, based on the proportion of free and / or non-entrapped and / or non-embedded, especially non-encapsulated, active agent.

9. Composition according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin,solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof.10 Composition according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

11. Composition according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

12. Composition according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, andwherein the active agent is selected from oxybutynin as well as salts and esters thereof.

13. Composition according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is selected oxybutynin as well as salts and esters thereof.

14. Composition according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is present and / or used in neutral and / or uncharged molecular form and / or in form of the active agent as such or in the form of a pharmaceutically acceptable salt or ester or mixtures or combinations thereof.

15. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof, in particular wherein the active agent, particularly the pharmaceutical active ingredient (API), is present and / or used in neutral and / oruncharged molecular form and / or in form of the active agent as such or in the form of a pharmaceutically acceptable salt or ester or mixtures or combinations thereof;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

16. Composition according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient(API), is net-positively charged; or wherein the active agent, particularly the pharmaceutical active ingredient (API), is net-neutral; or wherein the active agent, particularly the pharmaceutical active ingredient (API), is net-negatively charged; or wherein the active agent, particularly the pharmaceutical active ingredient(API), is a mixture of net-positively charged, net-negatively charged and net- neutral active agents; in particular wherein net-positive, net-negative or net-neutral charge of the active agent is induced by means of modification of the agent, in particular by means of chemical reaction, in particular derivatization or masking of charged functional groups; neutralizing treatment or alkalizing treatment, in particular by means of salt formation, ion-exchange, esterification and / or precipitation.

17. Composition according to one of the preceding claims, wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at least 0.05 wt.%, in particular in amounts of at least 0.1 wt.%, preferably in amounts of at least 0.2 wt.%, more preferably in amounts of at least 0.3 wt.%, based on the total composition; and / or wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at most 50 wt.%, in particular in amounts of at most 35 wt.%, preferably in amounts of at most 25 wt.%, more preferably in amounts of at most 20 wt.%, based on the total composition; and / or wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts in a range of from 0.05 wt.% to 50 wt.%, in particular in amounts in a range of from 0.1 wt.% to 35 wt.%, preferably in amounts in a range of from 0.2 wt.% to 25 wt.%, more preferably in amounts in a range of from 0.3 wt.% to 20 wt.%, based on the total composition.

18. Composition according to one of the preceding claims, wherein the composition comprises a mixture of biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymers selected from the group consisting of matrix-forming polymers, preferably selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer; or wherein the composition comprises one single type of biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, preferably selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co- caprolactone) copolymer, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); in particular wherein the mixture of biodegradable and / or biocompatible polymers or the single type of biodegradable and / or biocompatible polymer is composed of one or more polymer fractions of a / the single polymer, in particular wherein the polymer fractions differ in one or more aspects selected form the group consisting of molecular weight, chemical modification, end- group configuration and / or end-group modification, net-charge, molecular shape, in particular branching, monomer ratio, in particular in case of copolymers.

19. Composition according to one of the preceding claims, wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at least 500 g / mol, in particular of at least 750 g / mol, preferably of at least 1 ,500 g / mol, preferably of at least 3,000 g / mol, preferably of at least 5,000 g / mol, preferably of at least 6,000 g / mol, more preferably of at least 7,000 g / mol; and / or wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at most 200,000 g / mol, in particular of at most 100,000 g / mol, preferably of at most 75,000 g / mol, more preferably of at most 50,000 g / mol; and / or wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwin a range of from 500 g / mol to 200,000 g / mol, in particular in a range of from 750 g / mol to 200,000 g / mol, preferably in a range of from 1 ,500 g / mol to 200,000 g / mol, preferably in a range of from 3,000 g / mol to 200,00 g / mol, preferably in a range of from 5,000 g / mol to 100,000 g / mol, preferably in a range of from 6,000 g / mol to 75,000 g / mol, more preferably in a range of from 7,000 g / mol to 50,000 g / mol; in particular wherein the weight average molecular weight Mwis determined by means of size-exclusion chromatography, preferably in accordance with standard ISO 16014 of 2019.

20. Composition according to one of the preceding claims, wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer comprises a chemical modification, in particular an end-group modification and / or capping; in particular wherein the chemical modification, in particular end-group modification and / or capping, is selected from branching, in particular graft copolymerization, esterification, in particular by means of short-chain alcohols, etherization, PEGylation, salt formation, in particular ion exchange to physiologically compatible and / or physiologically tolerable counter ions, and / or acid-functionalization, in particular by means of carboxylic acids, preferably by means of acrylic acid and / or methacrylic acid-modification.

21. Composition according to one of the preceding claims, wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is net-negatively charged; or wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is net-neutral; or wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is a mixture of net- negatively charged and net-neutral polymers; in particular wherein net-negative or net-neutral charge of the polymer is induced by means of chemical modification, in particular end-group modification and / or capping, of the polymer, preferably wherein the chemical modification, in particular end-group modification and / or capping, is selected from branching, in particular graft copolymerization, esterification, in particular by means of short-chain alcohols, etherization, PEGylation, salt formation, in particular ion exchange to physiologically compatible and / or physiologically tolerable counter ions, and / or acid-functionalization, in particular by means of carboxylic acids, preferably by means of acrylic acid and / or methacrylic acidmodification.

22. Composition according to one of the preceding claims, wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is a copolymer selected from the group consisting of matrix-forming polymers, preferably wherein the copolymer is selected from the group consisting of (poly(lactide-co- polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co- polyethylene glycol) copolymer (PLA-PEG), poly(lactic-co-glycolide acid) copolymer (PLGA), poly(lactide-co-caprolactone) copolymer; in particular wherein the copolymer has a ratio of first monomer : second monomer in a range of from 99 : 1 to 1 : 99, in particular in a range of from 85 : 15 to 15 : 85, preferably in a range of from 60 : 30 to 30 : 60, more preferably in a range of from 55 : 45 to 45 : 55.

23. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is a copolymer selected from the group consisting of matrixforming polymers, preferably wherein the copolymer is selected from the group consisting of (poly(lactide-co-polyalkylene glycol) copolymer (PLA- PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA- PEG), poly(lactic-co-glycolide acid) copolymer (PLGA), poly(lactide-co- caprolactone) copolymer; in particular wherein the copolymer has a ratio of first monomer : second monomer in a range of from 99 : 1 to 1 : 99, in particular in a range of from 85 : 15 to 15 : 85, preferably in a range of from 60 : 30 to 30 : 60, more preferably in a range of from 55 : 45 to 45 : 55; and / orin particular wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer has a weight average molecular weight Mwof at least 500 g / mol, in particular of at least 750 g / mol, preferably of at least 1 ,500 g / mol, preferably of at least 3,000 g / mol, preferably of at least 5,000 g / mol, preferably of at least 6,000 g / mol, more preferably of at least 7,000 g / mol, and / or has a weight average molecular weight Mwof at most 200,000 g / mol, in particular of at most 100,000 g / mol, preferably of at most 75,000 g / mol, more preferably of at most 50,000 g / mol, preferably wherein the weight average molecular weight Mwis determined by means of size-exclusion chromatography, preferably in accordance with ISO 16014 of 2019;(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release.

24. Composition according to one of the preceding claims, wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is linear; or wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is branched, in particular graft-copolymerized, comb-like or in a dendrimeric manner.

25. Composition according to one of the preceding claims, wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at least 5 wt.%, in particular in amounts of at least 10 wt.%, preferably in amounts of at least 12.5 wt.%, more preferably in amounts of at least 15 wt.%, based on the total composition; and / or wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at most 50 wt.%, in particular in amounts of at most 40 wt.%, preferably in amounts of at most 35 wt.%, more preferably in amounts of at most 30 wt.%, based on the total composition; and / or wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts in a range of from 5 wt.% to 50 wt.%, in particular in a range of from 10 wt.% to 40 wt.%, preferably in a range of from 12.5 wt.% to 35 wt.%, more preferably in a range of from 15 wt.% to 30 wt.%, based on the total composition.

26. Composition according to one of the preceding claims, wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1.5 to 1 : 500, preferably in a range of from 1 : 1 .75 to 1 : 200, more preferably in a range of from 1 : 2 to 1 : 50, particularly based on the weight percentage of the respective components (i.e. active agent and polymer).

27. Composition according to one of the preceding claims, wherein the solvent is selected from protic or aprotic solvents having a polarity lesser than the polarity of water and / or lesser than the polarity of urine; in particular wherein the solvent has a relative polarity value E? of less than 1 and / or more than 0.1 ; and / orin particular wherein the solvent has a relative polarity value E of at most 0.95, in particular of at most 0.9, preferably at most 0.85, more preferably of at most 0.8; and / or in particular wherein the solvent has a relative polarity value E of at least 0.15, in particular of at most 0.2, preferably at most 0.25, more preferably of at most 0.3; and / or in particular wherein the solvent has a relative polarity value E? in a range of from 0.15 to 0.95, in particular in a range of from 0.2 to 0.9, preferably in a range of from 0.25 to 0.85, more preferably in a range of from 0.3 to 0.8; preferably wherein the relative polarity value E? is obtained from the £r(30)- value normalized to the polarity extremes tetramethylsilane set as zero (= 0) and water set as 1 (= 1 ), wherein the £r(30)-value is defined as the transition energy of the long-wavelength VIS / NIR absorption band in a solution comprising the negative solvatochromic Reichardt dye (Betaine 30) at standard conditions (20 °C, 1.013 bar) indicated in the unit kcal / mol.

28. Composition according to one of the preceding claims, wherein the solvent is selected from the group consisting of A / -Methyl-2- pyrrolidon (NMP); dimethyl sulfoxide (DMSO); alkylene carbonates, in particular ethylene carbonate (EC), propylene carbonate (PC) and mixtures thereof, preferably propylene carbonate (PC); dihydrolevoglucosenone (Cyrene™); dimethyl sulfone (DMSO2); glycofurol (GF); ethanol (EtOH), isopropanol (I PA) and mixtures thereof; in particular propylene carbonate (PC), glycofurol (GF) and mixtures thereof.

29. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine, wherein the solvent is selected from protic or aprotic solvents having a polarity lesser than the polarity of water and / or lesser than the polarity of urine; in particular wherein the solvent has a relative polarity value E? of less than 1 and / or more than 0.1 ; and / or in particular wherein the solvent has a relative polarity value E? in a range of from 0.15 to 0.95, in particular in a range of from 0.2 to 0.9, preferably in a range of from 0.25 to 0.85, more preferably in a range of from 0.3 to 0.8 (wherein the relative polarity value E? is obtained from the £r(30)-value normalized to the polarity extremes tetramethylsilane set as zero (= 0) and water set as 1 (= 1 ), wherein the £r(30)-value is defined as the transition energy of the long-wavelength VIS / NIR absorption band in a solution comprising the negative solvatochromicReichardt dye (Betaine 30) at standard conditions (20 °C, 1.013 bar) indicated in the unit kcal / mol), in particular wherein the solvent is selected from the group consisting of A / -Methyl-2-pyrrolidon (NMP); dimethyl sulfoxide (DMSO); alkylene carbonates, in particular ethylene carbonate (EC), propylene carbonate (PC) and mixtures thereof, preferably propylene carbonate (PC); dihydrolevoglucosenone (Cyrene™); dimethyl sulfone (DMSO2); glycofurol (GF); ethanol (EtOH), isopropanol (IPA) and mixtures thereof; in particular propylene carbonate (PC), glycofurol (GF) and mixtures thereof; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release.

30. Composition according to one of the preceding claims, wherein the composition comprises the solvent in amounts of at least 40 wt.%, in particular in amounts of at least 50 wt.%, preferably in amounts of at least 55 wt.%, more preferably in amounts of at least 60 wt.%, based on the total composition; and / or wherein the composition comprises the solvent in amounts of at most 90 wt.%, in particular in amounts of at most 80 wt.%, preferably in amounts of at most 75 wt.%, more preferably in amounts of at most 70 wt.%, based on the total composition; and / or wherein the composition comprises solvent in amounts in a range of from 40 wt.% to 90 wt.%, in particular in a range of from 50 wt.% to 80 wt.%, preferably in a range of from 55 wt.% to 75 wt.%, more preferably in a range of from 60 wt.% to 70 wt.%, based on the total composition.

31. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release; and wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), in amounts of at least 0.05 wt.%, in particular in amounts of at least 0.1 wt.%, preferably in amounts of at least 0.2 wt.%, more preferably in amounts of at least 0.3 wt.%, based on the total composition, and / or in amounts of at most 50 wt.%, in particular in amounts of at most 35 wt.%, preferably in amounts of at most 25 wt.%, more preferably in amounts of at most 20 wt.%, based on the total composition; and / or wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in amounts of at least 5 wt.%, in particular in amounts of at least 10 wt.%, preferably in amounts of at least 12.5 wt.%, more preferably in amounts of at least 15 wt.%, based on the total composition, and / or in amounts of at most 50 wt.%, in particular in amounts of at most 40 wt.%, preferably in amounts of at most 35 wt.%, more preferably in amounts of at most 30 wt.%, based on the total composition; and / or wherein the composition comprises the solvent in amounts of at least 40 wt.%, in particular in amounts of at least 50 wt.%, preferably in amounts of at least 55 wt.%, more preferably in amounts of at least 60 wt.%, based on the total composition, and / or in amounts of at most 90 wt.%, in particular in amounts ofat most 80 wt.%, preferably in amounts of at most 75 wt.%, more preferably in amounts of at most 70 wt.%, based on the total composition.

32. Composition according to one of the preceding claims, wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the solvent in an active agent : solvent (weight) ratio in a range of from 1 : 1 to 1 : 10,000, in particular in a range of from 1 : 2 to 1 : 5,000, preferably in a range of from 1 : 3,5 to 1 : 1 ,000, more preferably in a range of from 1 : 5 to 1 : 500, in particular based on the weight percentage of components.

33. Composition according to one of the preceding claims, wherein the composition comprises the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer and the solvent in an polymer : solvent (weight) ratio in a range of from 1.5 : 1 to 1 :100, in particular in a range of from 1 : 1 to 1 : 75, preferably in a range of from 1 : 1.5 to 1 : 50, more preferably in a range of from 1 : 1.2 to 1 : 25, in particular based on the weight percentage of components.

34. Composition according to one of the preceding claims, wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer, and the solvent in an active agent + polymer : solvent (weight) ratio in a range of from 2 : 1 to 1 :50, in particular in a range of from 1.5 : 1 to 1 : 25, preferably in a range of from 1 : 1 to 1 : 15, more preferably in a range of from 1 : 1.2 to 1 : 10, in particular based on the weight percentage of components.

35. Composition, especially pharmaceutical composition, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular composition according to one of the preceding claims,wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer selected from the group consisting of matrix-forming polymers, wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine;wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release, and wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1.5 to 1 : 500, preferably in a range of from 1 : 1 .75 to 1 : 200, more preferably in a range of from 1 : 2 to 1 : 50, particularly based on the weight percentage of the respective components; and / or wherein the composition comprises the active agent, particularly the pharmaceutical active ingredient (API), the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer, and the solvent in an active agent + polymer : solvent (weight) ratio in a range of from 2 : 1 to 1 :50, in particular in a range of from 1.5 : 1 to 1 : 25, preferably in a range of from 1 : 1 to 1 : 15, more preferably in a range of from 1 : 1.2 to 1 : 10, in particular based on the weight percentage of components.

36. Composition according to one of the preceding claims, wherein the composition has a viscosity of at least 10 mPas, in particular of at least 15 mPas, preferably of at least 20 mPas, more preferably of at least 25 mPas, more preferably of at least 100 mPas, preferably of at least 150 mPas, preferably of at least 175 mPas, more preferably of at least 190 mPas; and / orwherein the composition has a viscosity of at most 15,000 mPas, in particular of at most 10,000 mPas, preferably of at most 7,500 mPas, preferably of at most 6,000 mPas, preferably of at most 5,000 mPas, more preferably of at most 1 ,500 mPas, preferably of at most 1 ,250 mPas, preferably of at most 1 ,100 mPas, more preferably of at most 1 ,000 mPas; and / or wherein the composition has a viscosity in a range of from 10 mPas to 15,000 mPas, in particular in a range of from 15 mPas to 15,000 mPas, preferably in a range of from 20 mPas to 15,000 mPas, more preferably in a range of from 25 mPas to 15,000 mPas, more preferably wherein the composition has a viscosity in a range of from 100 mPas to 15,000 mPas, in particular in a range of from 150 mPas to 7,500 mPas, preferably in a range of from 175 mPas to 6,000 mPas, preferably in a range of from 190 mPas to 5,000 mPas, more preferably wherein the composition has a viscosity in a range of from 100 mPas to 1 ,500 mPas, in particular in a range of from 150 mPas to 1 ,250 mPas, preferably in a range of from 175 mPas to 1 ,100 mPas, more preferably in a range of from 190 mPas to 1 ,000 mPas, in particular wherein the viscosity is measured by means of rotational viscometry, preferably in accordance with ISO 3219 of 2021.

37. Composition according to one of the preceding claims, wherein the composition comprises or at least essentially consists of a solution containing in addition to the components (a), (b) and (c)(d) at least one, particularly physiologically compatible and / or physiologically tolerable, adjuvant, in particular selected from the group consisting of pH- adjusting agents, surfactants, coagulants, wetting agents, excipients and mixtures thereof, preferably selected from pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids and / or acidic amino acids, amine sugars, in particular derived from aldohexoses, physiologically compatible and / or physiologically tolerable organic and / or inorganic acids and / or basis, and mixtures thereof; in particular wherein pH-adjusting agents and / or excipients selected from the group consisting of amino acids, in particular alkaline amino acids, are selected from the group consisting of lysine, arginine, histidine or mixtures thereof, in particular lysine, and / or wherein pH-adjusting agents and / or excipientsselected from the group consisting of amine sugars, in particular derived from aldohexoses, are selected from the group consisting of meglumine, dimethyl meglumine, glucosamine, galactosamine, mannosamine and mixtures thereof, preferably meglumine, dimethyl meglumine and mixtures thereof; and / or wherein a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts sufficient for the composition to be pharmaceutically effective over an extended and / or prolonged period of time and / or by diffusion-controlled release; in particular wherein a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts of at least 0.5 mg, in particular in amounts of at least 1 mg, preferably in amounts of at least 2 mg, more preferable in amounts of at least 5 mg; and / or in particular wherein a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts of at most 500 mg, in particular in amounts of at most 375 mg, preferably in amounts of at most 250 mg, more preferable in amounts of at most 200 mg; and / or preferably wherein a single dosage of the composition comprises the active agent (active ingredient), particularly the pharmaceutical active ingredient (API), in amounts in a range of from 0.5 mg to 500 mg, in particular in a range of from 1 mg to 375 mg, preferably in a range of from 2 mg to 250 mg, more preferable in a range of from 5 mg to 200 mg.

38. Use of a composition according to the preceding claims for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitialcystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

39. Use of a composition according to the respective preceding claims for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

40. Method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder,wherein a composition according to the respective preceding claims is intravesically, preferably via instillation by means of a catheterizing device (catheter), applied into the urinary bladder of a subject in need thereof, wherein the composition after intravesical application is contacted with urine present in the urinary bladder, and forms, in particular by means of the polymer, a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

41. Use of a composition according to the respective preceding claims for forming a drug delivery system (DDS), particularly a sustained-release drug delivery system (SR-DDS), preferably an in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the drug delivery system is formed from the composition being contacted after intravesical application with urine present in the urinary bladder, in particular by means of a polymer, as a three-dimensional matrix, in particular as three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / Yu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in s / Yu-forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release.

42. Drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the drug delivery system comprises or at least essentially consists of(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; especially wherein the drug delivery system is formed in situ in a urinary bladder to be treated.

43. Drug delivery system according to the preceding claim, wherein the drug delivery system is formed in situ in a urinary bladder to be treated when a composition according to one of the respective preceding claims is contacted after intravesical application with urine present in the urinary bladder.

44. Drug delivery system according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

45. Drug delivery system according to one of the preceding claims, wherein the drug delivery system (DDS), particularly the sustained-release drug delivery system (SR-DDS), preferably the in s / tu-forming implant (ISFI ), is configured for and / or is capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, inparticular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

46. Drug delivery system according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof.

47. Drug delivery system according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

48. Drug delivery system according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, andwherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

49. Drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular drug delivery system according to one of the preceding claims, wherein the drug delivery system comprises or at least essentially consists of(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures andcombinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); wherein the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; especially wherein the drug delivery system is formed in situ in a urinary bladder to be treated.

50. Drug delivery system according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is oxybutynin as well as salts and esters thereof.

51. Drug delivery system according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is oxybutynin as well as salts and esters thereof.

52. Drug delivery system according to one of the preceding claims, wherein the drug delivery system comprises the active agent, particularly the pharmaceutical active ingredient (API), and the biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer in an active agent : polymer (weight) ratio in a range of from 1 : 1 to 1 : 1000, in particular in a range of from 1 : 1.5 to 1 : 500, preferably in a range of from 1 : 1 .75 to 1 : 200, more preferably in a range of from 1 : 2 to1 : 50, particularly based on the weight percentage of the respective components (i.e. active agent and polymer).

53. Drug delivery system (DDS), particularly sustained-release drug delivery system (SR-DDS), preferably in s / Yu-forming implant (ISFI), for releasing at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), over an extended and / or prolonged period of time and / or by diffusion-controlled release, particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular drug delivery system according to the respective preceding claims, wherein the drug delivery system is obtained from a composition according to one of the respective preceding claims, in particular wherein the drug delivery system is obtained from the composition according to one of the respective preceding claims via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated.

54. Use of a drug delivery system according to the preceding claims for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

55. Use of a drug delivery system according to the respective preceding claims for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseasesand / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

56. Method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder, wherein a drug delivery system according to the respective preceding claims is intravesically, preferably via instillation by means of a catheterizing device (catheter), formed in the urinary bladder of a subject in need thereof.

57. Application device, in particular syringe, preferably ready-to-use piston syringe, comprising a composition, especially pharmaceutical composition, according to the respective preceding claims.

58. Application device, in particular syringe, preferably ready-to-use piston syringe, comprising a composition, especially pharmaceutical composition, in particular a composition according to the preceding claims, for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the composition comprises or at least essentially consists of a solution containing(a) at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder;(b) at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA));(c) at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine;wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release.

59. Application device according to the preceding claim, wherein the application device is a syringe, preferably a ready-to-use piston syringe, and / or wherein the application device has a volume in a range of from 2 ml to 25 ml; and / or wherein the application device comprises the composition in an amount in a range of from 2 ml to 25 ml.

60. Packaging unit comprising at least one pack and at least one application device according to the respective preceding claims, wherein the application device is inserted into the pack and / or is present in the pack.

61. Kit-of-parts comprising an instillation system, wherein the instillation system comprises(i) at least one composition for intravesical application into the urinary bladder according to the respective preceding claims, present in an application device as according to the respective preceding claims;(ii) at least one catheterizing device (catheter) connectable to the application device; and(iii) at least one instillation manual comprising application instructions.

62. Active agent (active ingredient), particularly pharmaceutical active ingredient (API), for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder; and wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is applied to a urinary bladder to be treated via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in s / Yu-formed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion-controlled release, wherein the in s / Yu-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; and wherein the at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is not miscible with urine and / or is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide- co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)).

63. Active agent according to the preceding claim, wherein the drug delivery system is obtained from a composition according to one of the respective preceding claims, in particular wherein the drug delivery system is obtained from the composition according to one of the respective preceding claims via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated.

64. Active agent according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

65. Active agent according to one of the preceding claims, wherein the drug delivery system (DDS), particularly the sustained-release drug delivery system (SR-DDS), preferably the in s / tu-forming implant (ISFI ), is configured for and / or is capable of releasing the active agent over a period of time of at least 12 hours, in particular at least 24 hours, preferably at least 36 hours, more preferably at least 48 hours, most preferably at least 72 hours; in particular wherein a proportion of the active agent contained in the composition of at least 40 %, in particular at least 50 %, preferably at least 60 %, more preferably at least 65 %, is released over the extended and / or prolonged period of time and / or by diffusion-controlled release; preferably wherein the proportion of active agent released is determined by means of injecting the composition into artificial urine, taking a sample of the composition at the periods of time as defined above, analyzing the proportion of released active agent, especially by means of HPLC with adequate detection, inparticular UV-detection, against a respective active agent-standard, and calculating the proportion of released active agent vis-a-vis the standard.

66. Active agent according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, and more preferably is selected from the group consisting of (i) agents promoting wound healing, in particular hyaluronan, panthenol, chondroitin sulphate, heparin, pentosan sulphate; (ii) antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine, preferably oxybutynin as well as salts and esters thereof; (iii) anticholinergic agents, especially fesoteridine as well as salts and esters thereof; (iv) antiphlogistics and / or anti-inflammatory agents, in particular from the group consisting of non-steroidal anti-inflammatory drugs or agents (NSAIDs) and corticosteroids; (v) anti-infectives, in particular virustatics and / or antibiotics and / or fungistatics, in particular Clorpactin; (vi) antitumor and anticancer agents and oncologically active substances, in particular cytostatics; (vii) beta-3 agonists, in particular Mirabegron; and mixtures thereof.

67. Active agent according to one of the preceding claims, wherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

68. Active agent according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, andwherein the active agent, particularly the pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof.

69. Active agent (active ingredient), particularly pharmaceutical active ingredient (API), for intravesical application into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, in particular active agent according to one of the preceding claims, wherein the at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), is selected from antimuscarinergic agents, in particular oxybutynin, solifenacin, darifenacin, atropine and mixtures thereof as well as salts and esters thereof, preferably oxybutynin as well as salts and esters thereof, and is applied to a urinary bladder to be treated via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in situ- ormed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release, wherein the in situ-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three- dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent; wherein the at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer is not miscible with urine and / or is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA), (ii) poly(lactide-co-polyalkylene glycol)copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG) (iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide- co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)).

70. Active agent according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is oxybutynin as well as salts and esters thereof.

71. Active agent according to one of the preceding claims, wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of neurogenic detrusor overactivity and overactive bladder syndrome, and wherein the active agent is oxybutynin as well as salts and esters thereof.

72. Active agent according to one of the preceding claims, wherein the active agent is contained in a composition according to the respective preceding claims, and / or wherein the active agent is contained in a drug delivery system obtained from a composition according to one of the respective preceding claims, in particular wherein the drug delivery system is obtained from the composition according to one of the respective preceding claims via in situ formation when contacted after intravesical application with urine present in a urinary bladder to be treated; and / orwherein the active agent is contained in a drug delivery system according to the respective preceding claims.

73. Use of an active agent according to the preceding claims for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis,(iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

74. Use of an active agent according to the respective preceding claims for producing a drug or medicament for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis,(v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder.

75. Method for the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder, in particular wherein the diseases and / or dysfunctions of the urogenital tract, preferably the diseases and / or dysfunctions of the urinary bladder, are selected from the group consisting of (i) neurogenic lower urinary tract dysfunctions, especially neurogenic bladder dysfunctions (nBFS), neurogenic bladder emptying disorders, neurogenic detrusor overactivity and overactive bladder syndrome, (ii) infections and inflammations of the urogenital tract, especially of the bladder, particularly bacterial, abacterial, viral or fungicidal infections and inflammations of the urogenital tract, (iii) cystitis, especially acute or chronic cystitis, interstitial cystitis, bacterial or abacterial cystitis, urocystitis, pancystitis, (iv) urethritis, (v) urinary tract obstruction, especially bladder outlet obstruction and ureteral obstruction, (vi) tumor and cancer disease of the urogenital tract, especially of the bladder, wherein an active agent according to the respective preceding claims is intravesically, preferably via instillation by means of a catheterizing device (catheter), applied into the urinary bladder of a subject in need thereof via an in s / Yu-formed drug delivery system (DDS), particularly via an in s / Yu-formed sustained-release drug delivery system (SR-DDS), preferably via an in situ- ormed implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release, wherein the in situ-formed drug delivery system comprises at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer forming a three- dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, the active agent.

76. Use of a composition, especially pharmaceutical composition, for intravesical application of at least one active agent (active ingredient), particularly at least one pharmaceutical active ingredient (API), selected from the group consisting of active agents being topically effective against diseases and / or dysfunctions of the urogenital tract, preferably against diseases and / or dysfunctions of the urinary bladder, into the urinary bladder, preferably via instillation by means of a catheterizing device (catheter), particularly for use in the prophylactic and / or curative treatment of diseases and / or dysfunctions of the urogenital tract, preferably diseases and / or dysfunctions of the urinary bladder,wherein the composition comprises or at least essentially consists of a solution containing at least one biodegradable and / or biocompatible, particularly physiologically compatible and / or physiologically tolerable, polymer which is not miscible with urine and / or which is not soluble in urine, particularly wherein the polymer is selected from the group consisting of matrix-forming polymers, preferably wherein the polymer is selected from the group consisting of (i) polylactide (polylactic acid, PLA),(ii) poly(lactide-co-polyalkylene glycol) copolymer (PLA-PAG), especially poly(lactide-co-polyethylene glycol) copolymer (PLA-PEG)(iii) polyglycolic acid (PGA), (iv) poly(lactic-co-glycolide acid) copolymer (PLGA), (v) poly(lactic-co-glycolide acid) / (polyalkylene glycol) copolymer (PLGA-PAG), especially poly(lactic-co-glycolide acid) / (polyethylene glycol) copolymer (PLGA-PEG), (vi) polycaprolactone (PCL), (vii) poly(lactide-co-caprolactone) copolymer, and mixtures and combinations thereof, preferably poly(lactic-co-glycolide acid) copolymer (PLGA)); and at least one solvent in which both the active agent and the polymer are soluble and / or which dissolves both the active agent and the polymer, and which is miscible with and / or soluble in urine and / or dissipates in urine; wherein, when the composition is contacted after intravesical application with urine present in the urinary bladder, the composition, in particular by means of the polymer, forms a three-dimensional matrix, in particular three-dimensional aggregates and / or agglomerates, comprising and / or entrapping and / or embedding, especially encapsulating, at least part of the active agent, preferably most of the active agent, preferably whereby the composition undergoes in s / tu-formation of a drug delivery system (DDS), particularly of a sustained-release drug delivery system (SR-DDS), preferably of an in situ- forming implant (ISFI), configured for and / or capable of releasing the active agent over an extended and / or prolonged period of time and / or by diffusion- controlled release.

77. Methods according to claims 40, 56 and 75, and uses according to claims 38, 39, 41 , 54, 55, 73, 74 and 76, characterized each by one or more of the features of any of claims 1 to 37.

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