Abstract: Described herein are polymer-agent conjugates and particles, which can be used, for example, in the treatment of cancer. Also described herein are mixtures, compositions and dosage forms containing the particles, methods of using the particles (e.g., to treat a disorder), kits including the polymer-agent conjugates and particles, methods of making the polymer-agent conjugates and particles, methods of storing the particles and methods of analyzing the particles.

Abstract: Described herein are polymer-agent conjugates and particles, which can be used, for example, in the treatment of cancer. Also described herein are mixtures, compositions and dosage forms containing the particles, methods of using the particles (e.g., to treat a disorder), kits including the polymer-agent conjugates and particles, methods of making the polymer-agent conjugates and particles, methods of storing the particles and methods of analyzing the particles.

Abstract: Provided is a naphthoquinone-based compound represented by Formula 1 or 2 having therapeutic effect on the treatment and/or prevention of prostate and/or testicle (seminal glands)-related diseases, and to a pharmaceutical composition of intestinal delivery system containing the same.

Abstract: It is believed that the abnormal absorption of endotoxin present in the gastrointestinal tract relates to the pathogenesis of autoimmune diseases such as rheumatoid arthritis. In an animal model for rheumatoid arthritis, it is observed that arthritis is improved by removing endotoxin. The present invention provides an endotoxin-adsorbent, which is capable of removing endotoxin in the gastrointestinal tract and can be administered to humans safely. By using a non-digestible and non-absorbable, and therefore, safe endotoxin-adsorbent, which has a high endotoxin-binding capacity for removing large amounts of endotoxin present in the gastrointestinal tract, it is possible to prevent and treat autoimmune diseases such as rheumatoid arthritis.

Abstract: The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20%, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface.

Abstract: An object of the present invention is to provide highly safe nanoparticles which can be used simultaneously for imaging, hyperthermia and DDS and have high drug incorporation ratio. The present invention provides a nanoparticle which comprises an inorganic nanoparticle of 1 to 500 nm in average particle size having an active substance immobilized on the surface and a polymer.

Abstract: A process for producing microspheres was developed that provides microspheres with new combined properties of high density, low fracture, high swell capacity, rapid swell, and deformability following swell. The process is reliable and high yielding, and makes use of a low temperature azo initiator and a small molecule chlorinated solvent as the organic phase. The microsphere preparation made using the process is particularly useful in medical treatments such as embolization.

Abstract: An ophthalmically acceptable vehicle includes an aqueous suspension having a first viscosity. The suspension includes about 0.1% to about 6.5% by weight of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less than about 5% by weight of a cross-linking agent. The polymer has average particle size of not more than about 50 ?m in equivalent spherical diameter. The vehicle includes a second polymer that allows the carboxyl-containing polymer to remain suspended. Upon contact with tear fluid, the vehicle gels to a second viscosity which is greater than the first viscosity. A method of administering a medicament to the eye of a subject includes applying a composition that includes this ophthalmically acceptable vehicle and a medicament contained for treatment of a disease or disorder for which ophthalmic delivery is indicated. The medicament is released from the vehicle in a sustained release manner.

Abstract: There is disclosed a novel sustained release granular resin-pharmaceutical composition comprising an ion exchange resin complexed with a pharmaceutical material wherein said complex is embedded into and on the surface of a diffusion barrier material. There is also disclosed a novel process for preparing the granulated complex wherein an aqueous granulating vehicle is employed to form the complex and the granulated product, thereby avoiding the use of coatings and large amounts of organic solvents in the process.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The invention relates to a process for preparing PCL-comprising microparticles, to microparticles obtainable by said process, to gel hence obtained and to several uses of the gel such as for the preparation of a medicament for treating a skin abnormality or disfigurement, and/or for controlling bladder function and/or controlling gastric reflux and/or for treating erectile dysfunction and/or for treating vocal cords. The gel may also be used for cosmetic applications.

Abstract: A method of delivering embolic particles to an aneurysm includes inserting a delivery catheter into the vasculature of a patient and directing the distal end of the delivery catheter to a pre-selected deployment site. Embolic particles are loaded into the delivery catheter, and hydraulic pressure is applied to move the embolic particles through the delivery catheter. The hydraulic pressure is adjusted to control the velocity of the embolic particles and to reduce jetting.

Abstract: Embolization, as well as related particles, compositions, and methods, are disclosed.

Abstract: The present invention describes methods and tools for preparing a population of monodisperse polymer microparticles, which are of particular interest in the field of drug delivery.

Abstract: A powder•particle dosage form obtained by granulating an excipient and/or a disintegrating agent with a liquid in which a bitter taste masking base is dissolved and/or suspended, and a drug having solubility in water (20° C.) of not higher than 1 g/mL is dissolved or suspended, or a tablet obtained by compressing the powder•particle dosage form could mask bitter taste of a drug.

Abstract: The present invention is a composition composed of a therapeutic agent encapsulated in a copolymer of an N-alkylacrylamide, a vinyl monomer, and a polyethylene glycol (PEG) conjugate and a method for using the same in the treatment or prevention of a disease or condition.

Abstract: The present invention provides a medical device, and methods of preparing and using a medical device. The medical device has a surface including a biologically active agent therein. The methods are particularly useful for preparing, for example, coated stents having a biologically active agent within the coating.

Abstract: The present invention describes polymer nanoparticles with a cationic surface potential, in which both hydrophobic and hydrophilic pharmaceutically active substances can be encapsulated. The hydrophilic and thus water-soluble substances are encapsulated in the particle core by co-precipitation through ionic complexing with a charged polymer. Both therapeutic agents and diagnostic agents can be used as pharmaceutically active substances for encapsulation. The cationic particle surface permits stable, electrostatic surface modification with partially oppositely charged compounds, which can contain target-specific ligands for improving passive and active targeting.

Abstract: The present invention features dual network hydrogels that possess the structural, mechanical, and biological properties required of load bearing three-dimensional support structures.

Abstract: The present invention relates to a novel one step process for preparing cross-linked poly(allylamine) polymers or salts thereof using the novel cross-linking agent of Formula (IV). This invention also relates to the compound of Formula (IV) as well as to a process to obtain it. The cross-linked poly(allylamine) polymers of the invention are useful in medicine as substrate-binding polymers.

Abstract: It is intended to provide a remedy for diseases caused by macrophages with dysfunction or mediated by macrophages. Namely, a remedy which activates the phagocytic capacity of macrophages and thus is efficiently incorporated into the macrophages due to the vigorous phagocytosis. As a result, the macrophages with dysfunction are normalized, macrophages infected with a pathogen are exterminated or a pathogen in the infected macrophages is exterminated.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides polymeric and pharmaceutical compositions comprising crosslinked amine polymers. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of renal diseases and hyperphosphatemia.

Abstract: Improved compositions for tissue augmentation are provided. These compositions comprise an amount of crosslinked material sufficient to provide a melt temperature (Tm) greater than 37 C, wherein microparticles can be substantially uniformly dispersed and maintained at ambient room temperature as well as body temperature. Said compositions also provide high shear moduli, sufficient to effectively deliver microparticles into dense tissue and narrow intersticial spaces without significant disruption to the homogeneous distribution of microparticles within the solution. The provided compositions can be stored and shipped at room temperature without significant detriment to the material composition. Additional embodiments include a system for delivery of tissue augmentation materials and methods of manufacture thereof.

Abstract: A dispensing device having a polymer which is combined with a therapeutic agent in the form of a microparticle or nanoparticle which is “hyper-compressed” to form a controlled release dispensing device and methods of locally administering a therapeutic agent using said microparticles.

Abstract: A process is described for loading hydrophilic polymer particles with a water-insoluble solvent-soluble drug. The particles are preferably embolic agents. The method provides particles having little or no drug at the surface and in a surface layer, whereby the burst effect is minimised. The drug is precipitated in the core of the particle, leading to extended release. The drug is, for instance, paclitaxel, rapamycin, dexamethasone or ibuprofen.

Abstract: The present invention relates to novel and improved compositions of anticancer drugs, preferably taxanes, such as paclitaxel and docetaxel, their derivatives or their analogues, methods of manufacturing these compositions and methods of fractionating the particles in particular size range and methods of treating cancer patients with these compositions, which provide reduced chemotherapy-induced side-effects especially reduced chemotherapy-induced-alopecia. The composition is such that there is substantially no free drug in the said composition.

Abstract: Provided herein are compositions and methods for treating cancer by increasing the pro-apototic actions of small molecule ligands of integrin RGD recognition sites such as polyphenols by administering such compounds in conjunction with anti-angiogenic thyroid hormone analogs such as tetrac or triac.

Abstract: An active agent composition includes particles containing a water-insoluble active agent or an active agent with a significant food effect; and a ternary amine polymer having both hydrophobic (meth)acrylate units and acid-soluble (meth)acrylate units, and an acidifying agent; wherein upon ingestion by a human subject, the acidifying agent facilitates the dissolution of the ternary amine polymer in the gastrointestinal tract.

Abstract: A process for preparing particles of a substance comprising contacting a first formulation including a first substance with a first solvent stream and a second solvent stream, thereby causing formation of particles of the first substance, wherein both the first and second solvent streams are in a non-supercritical state, and subjecting the resultant mixture to a separation process which causes separation of the first substance from the first and second solvent streams.

Abstract: The present application relates to a method for preparing nanoparticles containing a poorly water-soluble pharmaceutically acceptable compound and compositions containing such nanoparticulates.

Abstract: A two-phase drug delivery medium comprising a discontinuous phase and a solid continuous phase, the discontinuous phase comprising a plurality of droplets, each of which comprises a fluid and at least one drug dissolved or suspended within the fluid, and the continuous phase surrounding and encapsulating the discontinuous phase.

Abstract: Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof.

Abstract: The present invention relates to a medical product that can be implanted or introduced into a vascular system of a human or animal organism, having an active substance coating according to the invention on the surface of the medical product, to a method for the production of a medical product that can be implanted or introduced into a vascular system of a human or animal organism, having an active substance coating according to the invention, to an active substance coating according to the invention for a medical product that can be implanted or introduced into a vascular system of a human or animal organism, to uses of the active substance coating according to the invention for the production of a medical product that can be implanted or introduced into a vascular system of a human or animal organism, and to a method for treatment of a stenosis, etc., in the vascular system of a human or animal organism.

Abstract: The present invention relates to a preparation comprising at least one encapsulation material and at least one bioactive natural substance, which bioactive natural substance can be released from the preparation in a controlled manner, wherein the encapsulation material comprises at least one glyceride with a melting point of at least 35° C. and additionally at least one polymer with polyester units, which has a melting temperature of at least 30° C. and a viscosity in the range from 50 mPa*s to 250 Pa*s, measured by means of rotational viscometry at 110° C. The present invention further describes processes for producing the preparation of the invention, as well as preferred uses.

Abstract: Particles and related methods are disclosed. In some embodiments, a method of making particles can include forming a stream of a mixture including first and second materials, exposing the stream to a vibration, and treating the stream to form particles. The vibration can have, for example, a sinusoidal, triangular, and/or sawtooth waveform.

Abstract: Polymeric delivery agents, delivery agent compounds and compositions comprising them which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: A pharmaceutical composition comprises nanoparticles comprising a cholesteryl ester transfer protein inhibitor and a poorly aqueous soluble non-ionizable polymer.

Abstract: The present invention provides a vaccine composition comprising an effective amount of antigen or a nucleic acid encoding antigen, encapsulated in polymeric particles, wherein said polymeric particles comprises nanoparticles, microparticles or combinations thereof, wherein surprisingly the nanoparticle induces cellular response and the microparticle induces humoral response. The invention further provides a method of inducing cellular and/or humoral immune response.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The present invention relates to a material having osteoinductive and osteoconductive properties in vivo comprising a ceramic carrier, preferably containing calcium phosphate, and an active agent, preferably an osteoinductive protein/peptide or a drug, and a polymer, wherein the active agent is homogeneously coated on the carrier and within the polymer, which is preferably a degradable polymer. Said polymer modulates the release kinetic of the active agent and protects same from degradation to prolong the half-life in vivo. Moreover, the present invention relates to a method for the production of a material having osteoinductive and osteoconductive properties in vivo.

Abstract: A composition which comprises (A) a plurality of cross-linked polymer particles, said polymer being the polymerization product of at least two monomer units selected from the group consisting of monoalkenyl aromatic compounds, alkyl esters derived from a saturated alcohol and acrylic or methacrylic acid, and vinyl esters of an aliphatic carboxylic acid; and said cross-line polymer particles being loaded with (B) an active ingredient, the weight ratio of the active ingredient (B) to the polymer particles (A) being from 0.05 to 50:1, is useful to release the active ingredient over an extended period of time while controlling sebum on skin and hair.

Abstract: A low melting binder composition for preparation of pharmaceutical tablets and/or granules which comprises a polymer and a hydrophobic meltable binder.

Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a vinca alkaloid; and about 50 to about 99 weight percent biocompatible polymer.

Abstract: Biocompatible, bioerodible implants and microspheres include latanoprost and a biodegradable polymer effective, when placed intraocular (such as into the subtenon space) to treat glaucoma.

Abstract: Anti-angiogenesis compositions, and methods of using such compositions, useful for intraocular to treat neovascularization. The compositions can have viscosities at about 25° C. of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity at 25° C. is in the range of from about 80,000 cps to about 300,000 cps.

Abstract: Provided are polymer vesicles comprising polymersomes, a radiofrequency absorbing moiety, a protein or a polysaccharide associated with the inner leaflet of the membrane and a therapeutic or diagnostic cargo. The invention also concerns the use of these polymer vesicles for selective electromagnetic energy-induced delivery of therapeutic or diagnostic agents.

Abstract: Techniques are provided to produce and use non-spherical colloidal particles with independently tuned size, shape, flexibility, and chemical properties. A pre-polymer mixture for forming hydrogel particles includes a percentage of PEGDA selected to impart a target stiffness to the particles and includes, a percentage of acrylic acid selected to impart an independent target chemical function to the particles. The mixture also includes a percentage of photo-initiator to polymerize PEGDA upon exposure to a light source to impart an independently selected target size or shape or both to the particles.

Abstract: Disclosed are in vitro methods for evaluating the in vivo redispersibility of dosage forms of poorly water-soluble active agents. The methods utilize media representative of in vivo human physiological conditions.