52 results about "Macromolecular drug" patented technology

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 5 kDa or more, the polymer matrix containing a hydrophobic polymer. The membrane polymer matrix includes from about 70 wt. % to about 99 wt. % of an ethylene vinyl acetate copolymer.

The present disclosure relates to a porous self-healing polymer matrix for encapsulation of active macromolecules and a method of manufacturing said porous self-healing polymer matrix for a drug delivery system for a macromolecule.

The invention belongs to the technical field of nano-drugs, and particularly relates to an artificially evolved protein cage nano-drug as well as a preparation method and application thereof. The artificial evolution protein cage nano-drug provided by the invention comprises an artificial evolution protein cage and a nucleic acid biomacromolecular drug, the artificial evolution protein cage is obtained by artificially obtaining a 240 polymer nano-protein cage C27-A with a PDB number of 6NJ8 by an artificial evolution system, and the amino acid sequence of a protein subunit of the artificial evolution protein cage is as shown in SEQ ID NO.1; the artificially evolved protein cage can be used for efficiently packaging nucleic acid type biological macromolecular drugs inside, has the advantages of high protein yield, good stability, good tumor treatment effect, excellent safety and the like, and can solve the technical problem of low drug packaging efficiency of protein cage nano drugs in the prior art.

Methods, systems and apparatus are described for classifying one or more candidate molecule drugs in relation to one or more desired target conditions for use in downstream processing of drug optimization. A candidate molecule drug inference dataset is received for one or more molecule drugs, the candidate molecule drug dataset comprising data representative of a set of physiochemical values for each candidate molecule drug and a set of pharmacokinetic (PK) values associated with a dosage regimen and target in relation to each candidate molecule drug, and where each candidate molecule drug of the candidate molecule drug dataset is classified as a large molecule drug. For each candidate molecule drug of the candidate molecule drug inference dataset, the corresponding set of physiochemical values and set of PK values for the dosage regimen and target are applied to a machine learning (ML) model configured for classifying whether each candidate molecule drug meets one or more desired conditions associated with pharmacological or pharmacodynamic effects. The ML model is trained using an ML algorithm to train model parameters defining the ML model for classifying whether each candidate molecule drug meets the one or more desired conditions based on a training dataset comprising data representative of a plurality of molecule drugs, each molecule drug represented by a corresponding set of physiochemical values and a set of PK values associated with the dosage regimen and the target, and annotated in relation to corresponding pharmacological or pharmacodynamic effects, responses and / or values in relation to the desired conditions. A set of candidate molecule drugs satisfying the desired conditions is output for downstream processing of drug optimization.

The invention discloses a drug delivery device in a human body cavity, which comprises an inflatable balloon, at least one part of the outer wall of the balloon is provided with a protective shell, the balloon is provided with an inner cavity, and the protective shell can be dissolved by specific body fluid in the human body cavity; the triggering part is arranged in an inner cavity of the balloon, and the triggering part can react with body fluid to generate fluid to inflate the balloon when making contact with the body fluid, so that the inflated balloon is tightly attached to the wall of a body cavity; the propelling part is arranged in the inner cavity of the balloon and comprises a tissue penetrating component, and the triggering part can generate power to propel the tissue penetrating component; and the containing part is used for containing a medicine preparation, and the triggering part can push and press the liquid medicine preparation contained in the containing part into the pushing part after the balloon is inflated, and injects the liquid medicine preparation into the inner wall tissue of the human body cavity through the tissue penetrating component. By means of the device, macromolecular drugs or preparations can be injected into the inner wall of the human body cavity, such as the tissue of the intestinal wall.

According to the invention, IN10018 and a macromolecular drug are combined to treat tumors, and the macromolecular drug is a monoclonal antibody, a bispecific antibody or an antibody conjugate.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 0.5 kDa or more, the polymer matrix containing a hydrophobic polymer. Further, the membrane layer comprises a plurality of water-soluble particles distributed within a membrane polymer matrix containing an ethylene vinyl acetate copolymer, wherein the water-soluble particles have a D50 particle size of about 150 micrometers or less and contain a non-polymeric, hydroxy-functional compound.

The invention discloses a method for preparing a biomacromolecular drug delivery carrier based on a simple and efficient interface cross-linking system. An amphiphilic polymer monomer containing an epoxy group is prepared through RAFT polymerization so that the amphiphilic polymer monomer can exist on an oil-water interface, meanwhile, a three-arm cross-linking agent which has environmental sensitivity and is terminated by an amino group is prepared, and the amino group on the cross-linking agent and the epoxy group on the amphiphilic monomer are subjected to a cross-linking reaction on the oil-water interface; a drug delivery vehicle is formed. The carrier can entrap biomacromolecules and accurately target tumors through a high-permeability long-retention effect, and glutathione rich in a tumor microenvironment can break disulfide bonds in the carrier and release drugs entrapped in the carrier, so that the aim of treating the tumors is fulfilled. Therefore, the invention provides a drug delivery carrier which is simple, convenient, efficient in entrapment of biomacromolecules and high in stability, and the prepared carrier can be efficiently taken by tumor cells so as to regulate and control apoptosis of the tumor cells and is high in safety.

To provide a method for treating a subject in need of treatment, the method comprising administering a large agent (for example, a biologically active large agent, such as a biologic therapeutic, for example, botulinum toxin) to the subject.SOLUTION: A method of treating a subject in need of treatment is provided, the method comprising a step of administering, in combination with microneedle skin conditioning (MSC), a plurality of doses of a composition that delivers a large agent having a molecular weight of 100,000 Da or greater to a site on skin of the subject according to a dosing regimen in which at least two successive doses are separated from one another by a time period of at least one month.SELECTED DRAWING: None

This disclosure relates to the treatment of tumors using IN10018 in combination with a macromolecular drug, wherein the macromolecular drug is a monoclonal antibody, a bispecific antibody, or an antibody-drug conjugate.

The invention discloses an ionic liquid transmucosal delivery system based on polyphenol modification. A preparation method comprises the following steps: S1, preparing polyphenol modified ionic liquid by adopting aromatic folic acid, polyphenol A and choline bicarbonate; the polyphenol A is gallic acid or caffeic acid; s2, polyphenol B is dissolved in ultrapure water, a biomacromolecule medicine is added, freeze drying is performed after ultrasonic treatment, and polyphenol-biomacromolecule nanoparticles are obtained; the polyphenol A is epigallocatechin-3-gallate, and the polyphenol B is epigallocatechin-3-gallate or tannic acid; s3, adding the polyphenol-biomacromolecule nanoparticles into the ionic liquid, and performing ultrasonic treatment to obtain the ionic liquid transmucosal delivery system based on polyphenol modification. According to the drug delivery system, polyphenol participates in ionic liquid construction, more intermolecular interaction force sites are provided for the ionic liquid, the charge property of the ionic liquid is reduced, and meanwhile, polyphenol-biomacromolecule nanoparticles are constructed to prolong the in-vivo action time of the drug.

The invention discloses a drug delivery device in a human body cavity, which comprises an inflatable balloon, at least one part of the outer wall of the balloon is provided with a protective shell, the balloon is provided with an inner cavity, and the protective shell can be dissolved by specific body fluid in the human body cavity; the triggering part is arranged in an inner cavity of the balloon, and the triggering part can react with body fluid to generate fluid to inflate the balloon when making contact with the body fluid, so that the inflated balloon is tightly attached to the wall of a body cavity; the propelling part is arranged in the inner cavity of the balloon and comprises a tissue penetrating component, and the triggering part can generate power to propel the tissue penetrating component; and the containing part is used for containing a medicine preparation, and the triggering part can push and press the liquid medicine preparation contained in the containing part into the pushing part after the balloon is inflated, and injects the liquid medicine preparation into the inner wall tissue of the human body cavity through the tissue penetrating component. By means of the device, macromolecular drugs or preparations can be injected into the inner wall of the human body cavity, such as the tissue of the intestinal wall.

An amphiphilic drug carrier and the use thereof in the ocular delivery of a biomacromolecular drug. The amphiphilic drug carrier is capable of penetrating the ocular mucus barrier, loading a biomacromolecular drug by means of non-covalent interaction, and delivering the biomacromolecular drug for the treatment of fundus diseases.

The present invention discloses an α-difluoromethylstyrene derivative and a preparation method thereof. The structure of the α-difluoromethylstyrene derivative of the present invention is as shown in formula (I), and the α-difluoromethylstyrene derivative is formed by reacting 3,3-difluoroallyl hydrazine, a transition metal salt and an additive in a solvent. The α-difluoromethylstyrene derivative of the present invention contains both gem-difluoromethylene and double bond structural units, and can be used as a potential pharmaceutical lead compound or a synthetic intermediate of a drug active molecule, providing an opportunity for the synthesis of macromolecular drugs. At the same time, the present invention provides a preparation method of the compound. The method is direct, simple, efficient, has a wide range of substrate applicability, and the raw materials are economically available and easy to obtain, and is suitable for large-scale production of α-difluoromethylstyrene derivatives.

The invention discloses a drug delivery device in a human body cavity, which comprises an inflatable balloon, at least one part of the outer wall of the balloon is provided with a protective shell, the balloon is provided with an inner cavity, and the protective shell can be dissolved by specific body fluid in the human body cavity; the triggering part is arranged in an inner cavity of the balloon, and the triggering part can react with body fluid to generate fluid to inflate the balloon when making contact with the body fluid, so that the inflated balloon is tightly attached to the wall of a body cavity; the propelling part is arranged in the inner cavity of the balloon and comprises a tissue penetrating component, and the triggering part can generate power to propel the tissue penetrating component; and the containing part is used for containing a medicine preparation, and the triggering part can push and press the liquid medicine preparation contained in the containing part into the pushing part after the balloon is inflated, and injects the liquid medicine preparation into the inner wall tissue of the human body cavity through the tissue penetrating component. By means of the device, macromolecular drugs or preparations can be injected into the inner wall of the human body cavity, such as the tissue of the intestinal wall.

The application discloses a swallowable drug device combination device for promoting intestinal absorption of macromolecular drugs, and belongs to the technical field of drug delivery and medical devices, and the structure comprises an intestinal built-in vibration component and an external alternating magnetic field driving component; the intestinal built-in vibration component comprises a soft magnetic layer and an adhesive hydrogel layer, the soft magnetic layer is prepared by magnetizing after curing of an elastomer material doped with magnetic particles, and the adhesive hydrogel layer is a sodium alginate-acrylamide double-network hydrogel loaded with macromolecular drugs; the external alternating magnetic field driving component comprises a power module, a current driving module, an electromagnetic module, a control module and an interactive terminal; in the working state, the alternating magnetic field generated by the external alternating magnetic field driving component penetrates the body surface tissue and acts on the soft magnetic layer of the intestinal built-in vibration component, so that mechanical vibration is generated to exert physical stimulation on the local tissue in the intestine. The device can accelerate the release rate of macromolecular drugs and enhance the absorption efficiency of the macromolecular drugs in the intestine.

This application belongs to the field of nanomedicine technology, and particularly relates to an artificially evolved protein cage nanomedicine, its preparation method, and its application. The artificially evolved protein cage nanomedicine provided by this application includes an artificially evolved protein cage and a nucleic acid-based biomolecular drug. The artificially evolved protein cage is artificially obtained by an artificial evolution system from a 240-polymer nanoprotein cage C27-A with PDB number 6NJ8. The amino acid sequence of the protein subunit of the artificially evolved protein cage is shown in SEQ ID NO.1. The artificially evolved protein cage can efficiently encapsulate nucleic acid-based biomolecular drugs and has advantages such as high protein yield, good stability, good tumor efficacy, and excellent safety. It can solve the technical problem of low drug encapsulation efficiency in existing protein cage nanomedicines.

The present application relates to the field of pharmaceutical wastewater treatment technology, and discloses a system for treating pharmaceutical wastewater derived from Citrus aurantium, comprising a pretreatment unit, wherein wastewater enters the pretreatment unit, and colloidal proteins in the wastewater are removed by flocculation, and the generated flocculated impurities are formed into agglomerates, and the impurities in the wastewater are filtered by the agglomerates; a molecular imprinting treatment unit, which receives the wastewater output by the pretreatment unit, and adopts Fe3O4@SiO2 core-shell adsorption material with hesperidin as a template as an adsorbent, and cooperates with magnetic field fluidization to carry out targeted absorption of flavonoids in the wastewater, and cooperates with magnet assistance and regeneration process to complete the recovery of flavonoids and regeneration of adsorbent; and a bioelectrochemical reaction unit. Through the synergistic action of multiple mechanisms, the system realizes the step-by-step decomposition and mineralization of complex organic matter, especially showing excellent removal effect on pollutants such as macromolecular drug residues and pigments that are difficult to treat by traditional processes, ensuring that the effluent water quality is stable and meets the standards.

An implantable device for delivery of a macromolecular drug compound is provided. The device comprises a core having an outer surface and a membrane layer positioned adjacent to the outer surface of the core. The core comprises a core polymer matrix within which is dispersed a drug compound having a molecular weight of about 0.5 kDa or more, the polymer matrix containing a hydrophobic polymer. Further, the membrane layer comprises a membrane polymer matrix within which the macromolecular drug compound is optionally dispersed. The membrane polymer matrix contains a hydrophobic polymer in combination with a hydrophilic compound, and the weight ratio of the hydrophobic polymer to the hydrophilic compound within the membrane polymer matrix ranges from about 0.25 to about 200.

According to the application of the sodium taurocholate in preparing the medicine for coordinating the metabolic balance of the bone fat, the sodium taurocholate is used for coordinating the metabolic balance of the bone fat by inhibiting the accumulation of bone marrow adipose tissues. According to the application, the bone marrow adipose tissue can be accurately targeted to inhibit abnormal accumulation of the bone marrow adipose tissue, and normal bone marrow adipose tissue is not influenced. And moreover, by inhibiting abnormal accumulation of bone marrow adipose tissues, the bone fat metabolism balance is synergistically regulated and controlled, and particularly, adipogenesis inhibition and continuous osteogenesis promotion are combined. Sodium taurocholate is an endogenous bile acid derivative, so that the safety is higher, and sodium taurocholate is a micromolecular drug, so that sodium taurocholate can be orally taken compared with the current macromolecular drug injection administration route. In the application of the sodium taurocholate in preparing the medicine for coordinating the metabolism balance of the bone fat, the volume reduction amount of bone marrow adipose tissue is not less than 40%, and the bone mass increase amount is not less than 30%.

The present application relates to the field of biological materials, in particular to a high-efficiency transdermal recombinant humanized elastin as well as a preparation method and application thereof. In view of the problem that macromolecular drugs and proteins are difficult to be effectively absorbed through skin in the prior art, the present application discloses a high-efficiency transdermal recombinant humanized elastin, a coding gene, a recombinant vector, a recombinant genetically engineered bacterium, and a preparation method and application thereof. The protein has cell penetration ability and transdermal ability, and is obtained by protease cleavage from a precursor elastin. The nucleotide sequence of the coding gene of the precursor elastin is a sequence shown in SEQ ID NO. 3 or an equivalent sequence. The recombinant humanized elastin of the present application can be applied to skin care products, dressings, implants, artificial skin, artificial blood vessels, medical devices, biological materials or functional foods, and is particularly suitable for external preparations for anti-wrinkle, anti-aging or skin barrier repair.

The invention discloses a deep eutectic solvent which is an organic molten salt consisting of an anion component and a cation component, the anion component is selected from organic acid, polyhydric alcohol or sugar which can be used as a hydrogen bond donor; the cationic component is selected from quaternary ammonium salts and zwitterionic surfactants which can be used as hydrogen bond acceptors; and the molar ratio of the cation component to the anion component is 1: 4-1: 0.5. The invention further discloses a macromolecular pharmaceutical composition prepared on the basis of the deep eutectic solvent technology. The macromolecular pharmaceutical composition comprises an external enteric-coated protective layer and drug-loaded composite particles or drug-loaded composite pellets packaged in the enteric-coated protective layer, the drug-loaded composite particles or drug-loaded composite pellets are prepared from a deep eutectic solvent-macromolecular drug delivery system and other auxiliary materials; the deep eutectic solvent-macromolecular drug delivery system is prepared from a biological macromolecular drug and a deep eutectic solvent. According to the drug delivery system, the intestinal permeability of macromolecular drugs can be enhanced, and the oral bioavailability of the macromolecular drugs is improved.

The disclosure provides a branched structure polypeptide peptide carrier and its variations. The branched structure peptide has the following sequence formula:The technical solution of the disclosure enables efficient delivery of nucleic acids to tissues and organs in vivo for targeted therapy. The polypeptides have several times more conformational flexibility and affinity than macromolecular drugs (proteins and antibodies). The branched structure polypeptides possess long-lasting in vivo stability while maintaining strong affinity and minimal toxicity. By forming stable nanocomplexes or nanoparticles through electrostatic interactions with nucleic acid molecules, they can facilitate the delivery of nucleic acid drugs and their stable release inside cells, thereby enhancing the activity of nucleic acid-based therapeutics.

The invention relates to a Jinhuang powder drug-loaded microneedle for improving gouty arthritis and a preparation method thereof. The preparation method comprises the following steps: step 1, researching the action mechanism of the Jinhuang powder for treating the gouty arthritis; 2, according to the research result, increasing the proportion of cortex phellodendri, cortex magnoliae officinalis and liquorice in the original golden-huang powder prescription, and reducing the proportion of other medicinal materials to obtain a new golden-huang powder prescription; and step 3, preparing the Jinhuang powder drug-loaded microneedle on the basis of the new prescription of the Jinhuang powder. A golden yellow powder medicinal material is loaded through a microneedle, painless drug delivery of the microneedle is utilized, the delivery efficiency is higher than that of traditional transdermal drug delivery, good biocompatibility is achieved for delivery of protein and nucleic acid macromolecular drugs, the drug delivery efficiency can be improved, the drugs are delivered to specific parts in a targeted mode, adverse reactions of the drugs are reduced, and the utilization rate of the drugs is increased; the proportion of the golden cypress, the mangnolia officinalis and the liquorice in an original golden-yellow powder prescription is increased, and the treatment effect of the golden-yellow powder drug-loaded microelement on gouty arthritis is further enhanced.

This invention belongs to the field of biomedical technology, specifically relating to a biodegradable hyaluronic acid gel microsphere with synergistic effects of physical embolization and macromolecular drug loading, its preparation method, and its application in arterial chemoembolization. This embolic microsphere can load not only small molecule drugs but also ADC drugs, achieving long-term release, and is completely degradable, meeting the needs of long-term clinical application.

The invention discloses application of rhizoma atractylodis macrocephalae polysaccharide in preparation of a medicine for treating sepsis. The sepsis is a systemic infection complication with extremely high morbidity and death rate, and a specific treatment medicine is lacked at present. In-vivo experiments prove that the rhizoma atractylodis macrocephalae polysaccharide (the preferable administration dosage is 50 mg / kg) has remarkable immunoregulation and anti-inflammatory effects, and can effectively improve the survival rate of sepsis model mice, improve multi-organ injury, inhibit inflammatory factor storm and regulate blood coagulation dysfunction. In addition, the atractylodes macrocephala polysaccharide can enhance the defense capability of a host in an immunosuppression state and reduce the risk of secondary bacterial infection. The rhizoma atractylodis macrocephalae polysaccharide has a wide application prospect in sepsis treatment as a macromolecular medicine with a natural source.

This application provides a flexible hollow electrostimulation electrode array device and its preparation method, belonging to the field of medical device technology. Specifically, it includes a flexible substrate and a microneedle array; the microneedle array includes multiple microneedles, at least some of which have different heights; the leads of the microneedles are used for electrical connection to a detection device and an electrical pulse generator. When it is necessary to use electroporation to allow macromolecular drugs to enter the intracellular fluid, the flexible hollow electrostimulation electrode array device is implanted into human tissue. Microneedles of different heights penetrate into different depths within the tissue. The leads of the microneedles are first connected to a detection device to detect the neurophysiological signals of the target brain region to determine the location and type of the disease. Then, an electrical pulse generator is connected to provide pulsed current to the microneedles, enabling macromolecular drugs to enter the intracellular fluid through the nanopores of the cell membrane via electroporation for treatment of the lesion. After a period of treatment, the detection device is connected again to assess the treatment effect.

This invention discloses a macromolecular JAK inhibitor, its preparation method, and its applications. This macromolecular JAK inhibitor is an anti-inflammatory amphiphilic polymer of hexachlorocyclotriphosphazene or cyanuric chloride coupled with different functional groups. The anti-inflammatory amphiphilic polymer is synthesized with hexachlorocyclotriphosphazene or cyanuric chloride as the backbone structure, linked by a stepwise nucleophilic substitution reaction with different proportions of hydrophilic modules polyethylene glycol and 3-aminobenzoyl hydrazide (i.e., luminol). The preparation method of this type of anti-inflammatory macromolecular drug is simple, its structure and function are controllable, and it is easy to synthesize on a large scale. Furthermore, this type of amphiphilic anti-inflammatory macromolecular drug can self-assemble into nanomicelles in aqueous solution through intermolecular interactions. It can be applied to the treatment of various acute and chronic inflammations or diseases related to the JAK signaling pathway, and can be administered via intravenous injection, subcutaneous injection, nebulized inhalation, intramuscular injection, and any combination of the above methods. This anti-inflammatory macromolecular drug has significant therapeutic effects in acute lung injury, acute kidney injury, acute liver failure, sepsis, and asthma.

The invention discloses a drug delivery device in a human body cavity, which comprises an inflatable balloon, at least one part of the outer wall of the balloon is provided with a protective shell, the balloon is provided with an inner cavity, and the protective shell can be dissolved by specific body fluid in the human body cavity; the triggering part is arranged in an inner cavity of the balloon, and the triggering part can react with body fluid to generate fluid to inflate the balloon when making contact with the body fluid, so that the inflated balloon is tightly attached to the wall of a body cavity; the propelling part is arranged in the inner cavity of the balloon and comprises a tissue penetrating component, and the triggering part can generate power to propel the tissue penetrating component; and the containing part is used for containing a medicine preparation, and the triggering part can push and press the liquid medicine preparation contained in the containing part into the pushing part after the balloon is inflated, and injects the liquid medicine preparation into the inner wall tissue of the human body cavity through the tissue penetrating component. By means of the device, macromolecular drugs or preparations can be injected into the inner wall of the human body cavity, such as the tissue of the intestinal wall.

The present application provides a novel series of small molecular immune agonists of Toll-like receptor 7, having a structure represented by Formula I. The present application further provides use of the immune agonist for activating and amplifying immune cells and lymphocytes, and for preparing an immunomodulatory drug, an immune anti-tumor small molecule drug, and an immune anti-tumor macromolecular drug.