Abstract: The present invention relates to a nanoparticulated anaesthetic composition for topical use in which at least one local anaesthetic agent is encapsulated in polymeric nanoparticles. The present invention also relates to the use of such polymeric nanoparticles comprising at least one local anaesthetic agent in the preparation of an anaesthetic composition for topical application to the skin or mucosa.

Abstract: To provide a pulmonary disease therapeutic drug exhibiting high efficacy and reduced side effects. The pulmonary disease therapeutic drug of the invention for intratracheal administration contains biocompatible polymer nanoparticles including an HMG-CoA reductase inhibitor.

Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug and a poorly aqueous soluble non-ionizable polymer, and casein.

Abstract: Nanoparticulate preparations of pharmaceutical and cosmetic active substances with a core-shell structure, whereby the active substance is present in an X-ray amorphous form, together with a polymer matrix and the shell consists of a stabilizing sheathing matrix.

Abstract: Biodegradable therapeutic agent incorporating microspheres formulated in a high viscosity carrier suitable for intraocular administration to treat an ocular condition. The formulation can also be used to treat non-ocular conditions such as articular pathologies.

Abstract: The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.

Abstract: The invention provides a cosmetic product which has a good texture and allows full expression of the inherent functions of ceramide as an intercellular lipid, such as skin barrier function and hair protection effect, as well as nanoparticles for cosmetics and powder for cosmetics which may be used in the above cosmetic product, exhibit good skin barrier function and hair protection effect, and are easy to incorporate into the above cosmetic product. The cosmetic product, the nanoparticles, and the powder for cosmetics according to the present invention contain a polymer obtained by polymerization of a monomer material containing a glycerol (meth)acrylate monomer represented by the formula (1): (R1: —H, —CH3; R2: —(CH2)n-; n is an integer of 1 to 4).

Abstract: The invention relates generally to an odor-absorbing superabsorbing composition, a process for production of an odor-absorbing superabsorbing composition, a composite comprising an odor-absorbing superabsorbing composition, a hygiene article comprising a composite, chemical products comprising or based on an odor-absorbing superabsorbing composition or a composite, as well as the use of an odor-absorbing superabsorbing composition or of a composite in chemical products.

Abstract: A method for preventing or treating a blood clotting disorder is disclosed. The method includes administering a therapeutic effective amount of at least one nanoparticle-based anticoagulant to a subject afflicted with blood clotting disorder or potentially afflicted with a blood clotting disorder, wherein the at least one nanoparticle-based anticoagulant is a substituted fullerene, polyamidoamine (PAMAM) dendrimer or combination thereof.

Abstract: The present invention relates to compositions devices and methods for treating bone and/or cartilage defects, and a method for manufacturing such a composition or device. In a certain embodiment, the invention provides a device and/or composition for treating bone and/or cartilage defects, having at least one collagen, for example of animal origin, and further containing at least one substance having an osteo-inductive or chondro-inductive activity, at least one differentiation and/or growth factor having osteo-stimulative and/or chondro-stimulative effect, and at least one filling material, in which the composition is in the form of a lyophil.

Abstract: The disclosure provides a method to form sustained release drug-containing microparticles with a biodegradable polymer. The method involves forming a polymer-drug-organic solvent phase, and dispersing the polymer-drug-organic solvent phase in an aqueous suspension of an inorganic gel, which may be hydroxyapatite. The hydroxyapatite appears to coat the polymer-drug-solvent droplets to prevent them coalescing. The solvent then evaporates with stirring of the dispersion, at which time the droplets solidify to drug-containing microparticles. The inorganic gel allows suitably small microparticles to form without use of an organic emulsifier.

Abstract: The present disclosure relates to processes for preparing microparticles comprising peptides and to microparticles prepared by such processes. Also disclosed are methods for delivering a bioactive peptide to a subject in need of treatment by the bioactive peptide.

Abstract: The present invention provides a pharmaceutical preparation to be dispersed before administration which has an adequate viscosity and a suitable flowability even when dispersed in a small amount of water and can be easily administered through an NG tube is provided. Specifically, the pharmaceutical preparation to be dispersed before administration contains active granules containing a pharmaceutically active substance having an average particle diameter of 5 mm or less and a thickening agent, and can be administered through an NG tube by dispersing in water before administration.

Abstract: The present application is directed to biodegradable polymers, compositions, including microspheres and nanospheres, formed of such polymers, and methods of using such polymers and compositions. In certain embodiments, the subject polymer compositions include therapeutic agents, optionally providing sustained release of the encapsulated agent after administration to a patient.

Abstract: Embodiments include a vehicle for delivery of nitric oxide comprising: a collection of micelles having an internal micelle core that comprises a polymer with N-diazeniumdiolate comprising NO complexed with secondary amines of the polymer. Embodiments include a method of making a nitric oxide vehicle comprising dissolving a polymer that comprises secondary amines in an aqueous solution and combining the polymer with nitric oxide in the solution to form a N-diazeniumdiolate comprising the nitric oxide complexed with the secondary amines, with the formation of the N-diazeniumdiolate causing the polymer to be at least partially insoluble in the solution and to form a collection of micelles that have an internal core that comprises N-diazeniumdiolate.

Abstract: Drug-containing nanoparticles are provided that enable effective targeting and sustained-release of a water-soluble, non-peptide, low-molecular weight drug and cause reduced accumulation of the drug in the liver. The nanoparticles containing a water-soluble, non-peptide, low-molecular weight drug are obtained by hydrophobicizing the water-soluble, non-peptide, low-molecular weight drug by a metal ion, and reacting the hydrophobicized drug with a poly(lactic acid)-polyethylene glycol block copolymer or a poly(lactic-co-glycolic acid)-polyethylene glycol block copolymer. The nanoparticles have favorable targeting and sustained-release properties and cause reduced accumulation of the drug in the liver.

Abstract: The invention provides immunomodulatory compounds and methods for immunomodulation of individuals using the immunomodulatory compounds.

Abstract: The invention provides an oral pharmaceutical composition comprising modafinil particles, wherein at least about 5% of said modafinil particles have a diameter greater than 200 microns.

Abstract: Topical compositions are provided in which active compounds for topical delivery through the stratum corneum are complexed with nanospheres of a triblock copolymer having an A-B-A structure wherein each A end block is a water-soluble, hydrophilic and non-toxic polymer or oligomer; and the hydrophobic middle B block is a hydrophobic polymer or oligomer with the same or different repeating units having the structure according to formula:(I) wherein X is —C —R—C— or —C—; Z is between 2 and about 100, inclusive; R1 is CH?CH or (CH2), wherein n is from 0 to 18, inclusive; R2 is selected from hydrogen and straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms; and R is selected from a bond or straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms.

Abstract: A process for the production of a composition comprising a water-insoluble sartan which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble sartan, ii) a water soluble carrier, iii) a solvent for each of the sartan and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the sartan in the carrier.

Abstract: Microparticle-bioactive agent based treatments for local treatment of diseased tissues/organs are disclosed.

Abstract: The present invention provides a composition comprising a platelet aggregation inhibitor, for example, cilostazol, or a salt or derivative thereof, useful in the treatment and prevention of ischemic symptoms. The invention provides a composition which comprises nanoparticulate particles comprising the platelet aggregation inhibitor and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a platelet aggregation inhibitor, or nanoparticles comprising the same, in a pulsatile or continuous manner.

Abstract: A composition for delivery of a therapeutic agent is provided. The composition comprises: (a) a biocompatible block copolymer comprising one or more elastomeric blocks and one or more thermoplastic blocks and (b) a therapeutic agent, wherein the block copolymer is loaded with the therapeutic agent. The block copolymer is preferably of the formula X-(AB)n, where A is an elastomeric block, B is a thermoplastic block, n is a positive whole number and X is a seed molecule. The elastomeric blocks are preferably polyolefin blocks, and the thermoplastic blocks are preferably selected from vinyl aromatic blocks and methacrylate blocks. According to another aspect of the invention, a medical device is provided, at least a portion of which is insertable or implantable into the body of a patient. The medical device comprises (a) the above biocompatible block copolymer and (b) a therapeutic agent, wherein the block copolymer is loaded with the therapeutic agent.

Abstract: Methods for preparing dry powders having hydrophobic and hydrophilic components comprise combining solutions of the components and spray drying them simultaneously in a spray dryer. The hydrophilic and hydrophobic component are separately dissolved in separate solvents and directed simultaneously through a nozzle, usually a coaxial nozzle, into the spray dryer. The method provides dry powders having relatively uniform characteristics.

Abstract: A nanostructure includes a nanoparticle core (110) and a ligand (120) bonded to the nanoparticle core (110). The ligand includes a linking group (130) having a first end bonded to a polyethylene imine (PEI) polymer (140) and a second end bonded to the nanoparticle core (110) and a polyethylene glycol (PEG) polymer (150) grafted to the PEI polymer (140). Methods for making these nanostructures and their use in magnetic resonance imaging and management of inflammatory conditions are provided.

Abstract: A method of treating tissue includes placing substantially spherical polymer particles in the tissue. The particles include an interior region having relatively large pores and a first region substantially surrounding the interior having fewer relatively large pores than the interior region.

Abstract: Disclosed is a process of preparing sustained release microspheres, containing a biodegradable polymer as a carrier and a drug, using spray drying. The process comprises preparing a solution, suspension or emulsion containing a biodegradable polymer, a drug and a solvent; spray drying the solution, suspension or emulsion; and suspending spray-dried microspheres in an aqueous solution containing polyvinyl alcohol to remove the residual solvent and increase the hydrophilicity of the microsphere surface. The process enables the preparation of microspheres having high drug encapsulation efficiency, almost not having a toxicity problem due to the residual solvent, and having good syringeability. The microspheres prepared according to the present invention release an effective concentration of a drug in a sustained manner for a predetermined period when administered to the body, and are thus useful in the treatment of diseases.

Abstract: The invention provides an article comprising, a mesoporous silicate matrix, such as a particle, having one or more pores; and one or more releasable caps obstructing one or more of the pores. The articles are useful as delivery vehicles for encapsulated agents such as therapeutic agents, polynucleotides, polypeptides and the like.

Abstract: The disclosure relates to novel microencapsulation processes based on the use of high viscosity fluids (e.g., gelatinized starch and alginate), which are mixed and then sprayed using a much gentler hydraulic pressure and, preferably gas-based atomization into a crosslinking solution (e.g. of calcium chloride). To improve the efficiency of the system, the process can be performed in a continuous mode rather than by a conventional batch process. This involves continuous or intermittent harvest of the microparticles collected in the capture vessel followed by amendment and recycling of the CaCl2 solution and its redeployment into the capture vessel. The process allows production of microencapsulated probiotic bacteria without major losses in viability, thereby providing a useful and efficient new manufacturing method for the stabilization of probiotic bacteria prior to their introduction into functional foods.

Abstract: Degradable polymeric compositions containing water-insoluble drugs blended with copolymers of biocompatible diphenol compound monomer units with pendant carboxylic acid groups polymerized with biocompatible diphenol com-pound monomer units with pendant carboxylic acid ester groups and poly(alkylene oxide) blocks, wherein the molar fraction in the copolymer of biocompatible diphenol compound monomer units with pendant carboxylic acid groups and poly(alkylene oxide) blocks relative to the weight percentage of the drug in the composition is effective to provide pseudo-zero order release of the drug from the composition during the sustained-release phase of drug delivery under physiological conditions. Ocular treatment methods and manufacturing methods are also disclosed.

Abstract: The present invention provides a nano-micellar preparation of anthracycline antitumor antibiotics for intravenous injection, which comprises a therapeutically effective amount of anthracycline antitumor antibiotics, a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants. The preparation is prepared by encapsulating the medicament with a nano-micelle to obtain the nano-micellar preparation of anthracycline antitumor antibiotics for injection. The anthracycline antitumor antibiotics and the phosphatide derivatized with polyethylene glycol form a nano-micelle with a highly homogeneous particle size.

Abstract: The invention features core-shell microsphere compositions, hollow polymeric microspheres, and methods for making the microspheres. The microspheres are characterized as having a polymeric shell with consistent shell thickness.

Abstract: A nanocomposite delivery system uses chitosan as a mucoadhesive material encapsulated in a surface modified network of colloidal nanoporous nanoparticles, such as silica, or other colloid-forming materials, especially metal oxides. Drug delivery systems may be provided by binding a drug to the chitosan/silica nanocomposite, typically by adding a drug or other active agent during in-situ gellation of colloidal silica. When the active agent is, for example, amoxicillin or other antibiotic agent, the drug delivery system may be used in the treatment of stomach ulcers, for example.

Abstract: Embolic polymer particles are described.

Abstract: The invention discloses a pharmaceutical composition for the controlled release of relatively toxic active compounds, in particular for bioactive proteins from the class of interferons. The composition comprises a biodegradable block copolymer constructed from poly(ethylene glycol) terephthalate (PEGT) and poly(butylene terephthalate) (PBT). The composition is provided in the form of injectable microparticles, of an injectable liquid which may have self-gelling properties, or of a solid implant. The invention further provides a pharmaceutical kit comprising the composition, methods for preparing the composition, and the pharmaceutical uses relating thereto.

Abstract: Biocompatible intraocular drug delivery systems include nanoparticles that encapsulate siRNA molecules. The drug delivery systems may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others.

Abstract: Controlled release ceramic particles, processes for their preparation, controlled release ceramic particles prepared by such processes, compositions comprising such controlled release ceramic particles and methods of using controlled release ceramic particles are described. In one form each of the controlled release ceramic particles has an active material(s) substantially homogeneously dispersed throughout the particles, wherein the active material(s) is capable of being released from said particles, and the active material(s) in said particles is substantially protected from degradation until release of the active material(s) from the particles.

Abstract: Novel main chain acid degradable polymer backbones and drug delivery systems comprised of materials capable of delivering bioactive materials to cells for use as vaccines or other therapeutic agents are described. The polymers are synthesized using monomers that contain acid-degradable linkages cleavable under mild acidic conditions. The main chain of the resulting polymers readily degrade into many small molecules at low pH, but remain relatively stable and intact at physiological pH. The new materials have the common characteristic of being able to degrade by acid hydrolysis under conditions commonly found within the endosomal or lysosomal compartments of cells thereby releasing their payload within the cell. The materials can also be used for the delivery of therapeutics to the acidic regions of tumors and other sites of inflammation.

Abstract: Provided are thermo-responsive polymersomes, which display cold-controlled encapsulation near the physiological temperatures, and have a PDI less than 1.2. Morphology of the thermo-responsive polymersomes is a function of the weight fraction of the hydrophilic block in the block copolymer and the number average molecular weight (Mn) of the block copolymer. When the lower critical solution temperature (LCST) is at, or slightly above physiological temperature, the thermo-responsive block displays hydrophobic properties, such that the block copolymer self-assembles in aqueous solution to form a polymersome with the thermo-responsive block occupying the core of the polymersome and the hydrophilic block occupying the corona of the polymersome. Below the LCST, the thermo-responsive block displays hydrophilic properties, such that the polymersome dissociates, providing fast release of an active agent encapsulated therein.

Abstract: The present invention relates to a delayed release pharmaceutical oral dosage form and method of making same. The delayed release dosage form comprises one or more active ingredients within a granulated composition, which further comprises one or more excipients selected from the group of solid aliphatic alcohols, fatty acid esters, mixtures of esters of saturated fatty alcohols and saturated fatty acids, natural waxes, synthetic waxes, hydrogenated castor oil, hydrogenated vegetable oil, gums, and mixtures thereof; and one or more polymers or copolymers exhibiting a pH-dependent solubility. The present invention also related to method of making these delayed release dosage form.

Abstract: A medicotechnical product for adhesion prophylaxis for the post-operative prevention of accretions in the body comprises at least one PVA (polyvinyl alcohol) selected from the group comprising uncrosslinked PVA with a molecular weight of 15,000 to 400,000, crosslinked PVA and mixtures thereof. The molecular weight of the PVA or the mixture is selected in such a way that it can be excreted via the kidneys substantially with no degradation of the PVA molecules.

Abstract: [Problems] To provide a thin film-shaped porous bioabsorbable material that is a dense structure in which the pore size average is small and the pore size is uniform and which further has a large maximum stress, in particular, a porous bioabsorbable material extremely useful as an adhesion preventing material.

Abstract: The present invention relates to a process of preparing a biocompatible temperature-sensitive nano-carrier, which comprises the steps of (a) preparing a polymer dispersion comprising a water-soluble biocompatible polymer with photo-crosslinkable functional group(s), (b) preparing a polymer-initiator solution by adding an initiator to the polymer dispersion, and (c) preparing the nano-carrier by irradiating light onto the polymer-initiator solution, wherein the average diameter of the nano-carrier changes depending on temperature, and also relates to a temperature-sensitive nano-carrier. Nano-carriers of the present invention are temperature-sensitive, and their average diameter and pore size reversibly change in response to temperature change. In an embodiment of the present invention, nano-carriers can be prepared via a one-pot single-phase synthesis.

Abstract: The present invention relates to a method of forming shape-retentive and shape-conforming aggregate wound dressings and biomaterials composed of gel nanoparticles and wound or bodily fluid in which the aggregates are held together by non-covalent bond physical forces such as, without limitation, hydrophobic-hydrophilic interactions and hydrogen bonds. The method comprises introducing a dry powder of gel nanoparticles to a wound site in which the nanoparticles absorb some of the blood or wound exudate and coalesce in situ into the claimed shape-retentive aggregate dressing. The method also comprises introducing the dry nanoparticle powder in or on a wet bodily tissue in vivo to form the claimed shape-retentive biomaterial. In addition, the method also comprises incorporating biomedical agents to produce medicated aggregate dressings or biomaterials for a variety of medical applications. This invention also relates to uses of the method of formation of the shape-retentive aggregates of gel nanoparticles.

Abstract: The present invention relates to an injectable composition which comprises polymeric, water-insoluble, non-biodegradable, anionic particles, these particles having an irregular shape and a biocompatible carrier with a lubricated surface, a method for preparing the same, a method for treating a tissue in a patient which comprises injecting into the tissue site the injectable composition as a permanent implant and the use of the injectable composition as a medicament, particularly for bulking a tissue site.

Abstract: The present invention relates to injectable compositions comprising biocompatible, swellable, hydrophilic, non-toxic and substantially spherical microspheres useful for tissue bulking. The invention also relates to methods of tissue bulking, particularly for the treatment of Gastro-esophageal reflux disease, urinary incontinence, or urinary reflux disease, using the injectable compositions.

Abstract: Disclosed herein are methods that include providing a first particle having pores, the first particle having a first compression test value, and partially cross-linking the first particle to form a second particle having pores, the second particle having a second compression test value that is larger than the first compression test value by 25% or more, where a maximum dimension of the first particle is 5,000 microns or less, and a maximum dimension of the second particle is 5,000 microns or less.

Abstract: In accordance with one aspect of the invention, injectable particles are provided which comprise (a) a first group of injectable particles comprising first polymeric particles loaded with a first therapeutic agent and (b) a second group of injectable particles comprising second polymeric particles loaded with a second therapeutic agent. The first and second polymeric particles may be the same or different, and the first and second therapeutic agents may be the same or different. Other aspects of the invention pertain to methods of making such particles, to kits that comprise such particles, and to methods of treatment that employ such injectable particles.

Abstract: The disclosed processes for forming microparticles utilize low volumes of processing water while still providing microparticles having low residual solvent levels. The processes are adaptable to both continuous and batch processes using oil/water or water/oil or water/oil/water or oil/water/oil emulsions.

Abstract: In a solvent extraction process for preparing microspheres of a biodegradable polymer, the improvement comprising: preparing a homogenized antigen-sucrose matrix and adding a solvent to the sucrose-antigen matrix to form a solution; preparing a solution of a biodegradable polymer by adding a solvent to the polymer; adding the biodegradable polymer solution to the antigen-sucrose solution; adding an oil to the polymer-sucrose-antigen solution to form an emulsion having a controlled viscosity that corresponds to a predetermined average particle size of distributions of microspheres of biodegradable polymers; centrifuging the emulsion of controlled viscosity and removing the supernatant to obtain microspheres of a predetermined range of particle size distributions of from about 0.5 to about 7.0 micrometers.