114 results about "Site of action" patented technology

This invention discloses methods for preparing compositions of cyclodextrin polymers for carrying drugs and other active agents. Methods are also disclosed for preparing cyclodextrin polymer carriers that release drugs under controlled conditions. The invention also discloses methods for preparing compositions of cyclodextrin polymer carriers that are coupled to biorecognition molecules for targeting the delivery of drugs to their site of action. The advantages of the water soluble (or colloidal) cyclodextrin polymer carrier are: (1) Drugs can be used that are designed for efficacy without conjugation requirements. (2) It will allow the use of drugs designed solely for efficacy without regard for solubility. (3) Unmodified drugs can be delivered as macromolecules and released within the cell. (4) Drugs can be targeted by coupling the carrier to biorecognition molecules. (5) Synthesis methods are independent of the drug to facilitate multiple drug therapies.

This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)_k—(X)_l—A—Z, wherein: V is a specifier; (W)_k—(X)_l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)_m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)_m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.

This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.

Antimicrobial peptides enable an alternate approach to developing antimicrobial coatings due to their targeting of the membranes of the bacteria. High specific activity is achieved by orienting the peptides so that the antimicrobial ends of the peptides maximally contact the bacteria. In one embodiment, one end of the peptide is covalently attached directly to the substrate. In another embodiment, the peptides are immobilized on the substrate using a coupling agent or tether. Non-covalent methods include coating the peptide onto the substrate or physiochemically immobilizing the peptides on the substrate using highly specific interactions, such as the biotin/avidin or streptavidin system. The compositions are substantially non-leaching, antifouling, and non-hemolytic. The immobilized peptides retain sufficient flexibility and mobility to interact with and de endocytosed by the bacteria, viruses, and/or fungi upon exposure. Immobilizing the peptides to the substrate reduces concerns regarding toxicity of the peptides and the development of antimicrobial resistance, while presenting substantially all of the peptide at the site of action at the surface of the substrate.

The present application generally discloses delivery of an agent which can be therapeutic or prophylactic and, more particularly, the preparation and use of attenuated bacteria, such as Salmonella, containing a bacteriophage in which the genome of the bacteriophage has been modified to encode for a gene product of interest, e.g., an antigen or an anti-tumor protein. The bacteria functions as a vector for delivering the bacteriophage encoded gene product of interest to an appropriate site of action, e.g., the site of a solid tumor.

This invention discloses compositions and methods for preparing pharmaceutical nucleic acid carriers. The compositions comprise a carrier substance coupled to a nucleic acid intercalator whereby the intercalator is coupled by intercalation to the nucleic acid. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

A problem to be solved of the present invention is to provide a drug formulation and a method of administering an active ingredient which allow the active ingredient to be delivered evenly into the site of action in the skin with high efficiency while ensuring stability of the active ingredient over a long time, and which are easily handled and are less stressful for patients. Mean for solving the problem is a microneedle assembly formulation for skin treatment comprising a platform and a plurality of conical or pyramidal microneedles formed on the platform containing a base composed of a bio-soluble and thread-forming polymer substance and an objective substance retained in the base, wherein the objective substance is a substance effective for prevention or treatment of skin senescence, or treatment of skin scar.

An anesthesia device has a device (4, 5) for the supply of at least one first anesthetic and a second anesthetic in a quantitatively settable, controlled manner. A data processing unit (6) with a corresponding display (8) is set up for determining the current concentrations in the plasma or at the site of action from continuously supplied data on the quantities of the anesthetics administered with a module (10) for a pharmacokinetic compartment model calculation and for storing these concentration values. Concentration data is predicted for at least one point in time in the future and this is also calculated. An action module (20) keeps ready the curve of at least one anesthesia action parameter as a function of the concentrations of the anesthetics in a stored manner. A display module (30) displays on the display (8) at least one action diagram, in which the concentration of the first or second anesthetic as well as the sequence of the concentration data of the anesthesia curve obtained up to that point in time are displayed and the predicted concentration data are displayed with a separate symbol. In case of comparison with concentration set points, it is also possible to act automatically on the feed of the anesthetics in a controlled manner with the predicted concentrations.

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The present invention relates to the use of compounds such as compounds of the xanthenone acetic acid class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) for the treatment of cancer, wherein the compounds are administered gastrointestinally, preferably orally. More particularly, the invention is concerned with the use of such compounds, wherein the compound is delivered to the site of action in the patient to be treated in two or more doses.

The disclosure relates to a solid glass matrix of polysaccharides, monossaccharides or disaccharides in combination with polyols as delivery vehicles for preservation and post gastric administration of a probiotic. The delivery vehicle is capable of releasing the probiotic at their site of action. The present invention further includes methods of making and using the solid glass matrix delivery vehicle of the invention.

Identification of the molecular targets of a drug or toxin is the first step in understanding how the drug or toxin works, an important advance in learning how to improve a drug or assess the risks due to a toxin. The primary action of a drug usually involves binding to a protein; secondary actions may express themselves in the form of side effects and in some cases may be due to binding to other proteins. Consequently, it is useful to identify all physiologically relevant sites of action of a drug or toxin. A simple method for obtaining a list of the potential targets of a drug, toxin or other biologically active substance (referred to collectively as ligands) involves a multistep process. The first step is screening a protein or peptide library to identify library members that exhibit high affinity for a particular ligand. The second step involves searching of sequence data bases for proteins that contain the sequences of the library members shown to have high affinity for the ligand. The proteins thus identified constitute a list of potential targets for the ligand. If random peptide libraries have been used, the position of identified consensus sequences within the identified protein constitutes an identification of the potential ligand binding site on the target.

Disclosed herein are compositions and methods for the delivery and targeting of therapeutics using nanometer sized polysaccharide structures. The methods and compositions described herein afford improved efficacy for pharmaceuticals such as anti-tumor drugs on metastatic tumor. The methods described herein are applicable to all chemotherapeutic agents and are especially useful for poorly soluble (hydrophobic) drugs which when formulated with the present compositions render them deliverable in physiological fluids. The methods and compositions described herein also improve the efficacy of pharmaceutical agents by targeting carbohydrate receptors specific to tumors that mediate endocytosis or enhance delivery of the drug to the ultimate site of action.

PCT No. PCT/JP94/00237 Sec. 371 Date Oct. 23, 1995 Sec. 102(e) Date Oct. 23, 1995 PCT Filed Feb. 17, 1994 PCT Pub. No. WO94/19314 PCT Pub. Date Sep. 1, 1994The object of the invention is to provide a lipid device functionally equivalent to the so-called cationic liposome and of lesser toxicity and a lipid or the like as a component of the device. The compound of the invention includes but is not limited to 3-O-(4-dimethylaminobutanoyl)-1,2-O-dioleylglycerol, 3-O-(2-dimethylaminoethyl)carbamoyl-1,2-O-dioleylglycerol, 3-O-(2-diethylaminoethyl) carbamoyl-1,2-O-dioleylglycerol and 2-O-(2-diethylaminoethyl) carbamoyl-1,3-O-dioleoylglycerol. The device of the invention comprises such a lipid and a phospholipid. By administering a double-stranded RNA, for instance, together with the device of the invention, the double-stranded RNA can be safely delivered to the site of action.

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of peptides and peptide-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

It is intended to provide a novel therapeutic method for a disease with apoptotic degeneration in eye tissue cells such as retinal pigment degeneration. Attention was paid on the concomitant administration of two neurotrophic factors: pigment epithelium-derived factor (PEDF) and fibroblast growth factor 2 (FGF2). The sites of actions are considered to be different between PEDF and FGF2. An SIV-PEDF vector and an SIV-FGF2 vector were constructed and administered to the subretinal space of an RCS rat, which is a disease model of retinal pigment degeneration, and their effects were evaluated. At 4 weeks, 8 weeks and 12 weeks after the administration of the vectors, a significantly higher visual cell protection effect was obtained in a group with concomitant administration than in a group with sole administration. Further, the functional evaluation of retina was carried out by electroretinogram and an effect in the group with concomitant administration was significantly higher than in the group with sole administration. From the above results, it was found for the first time that the concomitant administration of PEDF and FGF2 has higher effects in the treatment of retinal pigment degeneration than conventional methods.

The invention relates to an externally-used gel-type lotion containing sophora alopecuroides of alkaloid. The externally-used gel-type lotion comprises the sophora alopecuroides of alkaloid, a gel substrate, a permeability accelerant, a surface active agent, a humectant, a pH modifier, fragrance, coloring matter and the balance purified water, wherein every 1000 ml externally-used gel-type lotion comprises 1 to 5 percent of the sophora alopecuroides of alkaloid, 1 to 15 percent of the gel substrate, 0 to 0.5 percent of the permeability accelerant, 0.5 to 5 percent of the surface active agent, 0 to 10 percent of the humectant, 0.1 to 2 percent of the pH modifier, 0 to 1 percent of the fragrance and 0 to 1 percent of the coloring matter. The good antibacterial effect of the extract of pure natural plant sophora alopecuroides and the advantages of gels are used, and the gel-type lotion obvious in antibacterial effect and long in residence time of medicine on the site of action is prepared. Natural ingredients serve as the permeability accelerant, the dual effects of permeability acceleration and sterilization are achieved, and the externally-used gel-type lotion has the advantages of the broad spectrum, the strong bactericidal ability and the good nursing effect.