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: Disclosed are biodegradable microspheres between 40 ?m and 200 ?m in diameter that are effectively retained in the anterior chamber of the eye without producing hyperemia. The microspheres generally contain a drug effective for the treatment of an ocular condition and include a biodegradable polymer matrix that can provide for the sustained (>7 day) release of the drug following administration to the anterior chamber of the eye. Methods for making and using the microspheres to treat an ocular condition are also 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: 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, 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 methods for extending the period of filtering bleb survival and/or providing for long term bleb survival following Glaucoma Filtration Surgery by delivering an ALK-5 inhibitor to a wound area (the surgical site) of a patient's eye. More particularly, the present invention relates to a method for the controlled delivery of an ALK-5 inhibitor to patient's eye using a thermo-sensitive polymer formulation, wherein the ALK-5 inhibitor is first contained in the polymer formulation at a temperature sufficient to maintain the formulation as a liquid and then applied to the eye wound opening, wherein the formulation turns to a gel. The use of the thermo-sensitive gel with ALK-5 inhibitor contained therein, provides for longer term bleb survival following Glaucoma Filtration Surgery (GFS) on a patient's eye. Thus, the present invention is particularly effective in inhibiting ocular fibrotic wound response following GFS.

Abstract: A bioactive PMMA (polymethylmethacrylate) bone cement contains a powder component and a reactive monomer liquid, wherein the powder component and the reactive monomer liquid when mixed with one another react with one another and form a polymer-based solid material. The powder component contains particulate polymer powder of polymethylmethacrylates; a radical starter; and anionic copolymer nanoparticles. The anionic copolymer nanoparticles are distributed in nano-particulate form within the particulate powder component or coated as a film on particles of the particulate polymer powder.

Abstract: The present invention relates to a method for preparing nano-particles, and more particularly, to a method for preparing nano-particles containing active materials in a simple and highly efficient manner through a grinding process.

Abstract: A powdery composition C1 contains for 100% of the mass: 5 to 70 mass % and more particularly 10 to 50 mass % of at least one compound of formula (I): R—O-(G)x-H, wherein R is a linear saturated aliphatic radical including 12 to 22 carbon atoms, G is the remainder of a reducing sugar selected from the group including glucose, xylose and arabinose, and x is a decimal number greater than or equal to 1 and lower than or equal to 10; 95 to 30 mass % and more particularly 90 to 50 mass % of one or more alcohols of formula (II): R?—OH, wherein R? is a linear saturated aliphatic radical including 12 to 22 carbon atoms identical to or different from R as defined in formula (I), wherein at least 90 vol % of the particles have a diameter lower than or equal to 250 micrometers, more particularly a diameter lower than or equal to 150 micrometers.

Abstract: The described invention provides a biodegradable, biocompatible delivery system of flowable sustained release microparticulate composition of a substantially pure crystalline form of a bioactive agent such as, for example, nimodipine, a process of preparing a therapeutic form of a substantially pure crystalline form of the bioactive agent and a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury.

Abstract: Compositions and methods for treating dry age related macular degeneration (dry AMD) by administration to an intraocular location of an anti-neovascular agent (such as bevacizumab) in either a liquid or solid polymeric vehicle (or both), such as a biodegradable hyaluronic acid or PLGA (or PLA).

Abstract: The present invention relates to a granular pharmaceutical composition obtained by coating a nucleus with: (1) a layer containing a material having a damp-proofing function, and (2) a drug layer containing linaclotide, a pharmaceutically acceptable salt, or a hydrate thereof, and (3) a layer containing a material having a damp-proofing function. Also, the present invention relates to a method for manufacturing the granular pharmaceutical composition obtained by coating the nucleus with (1) the layer containing the material having a damp-proofing function, (2) the drug layer containing the linaclotide, the pharmaceutically acceptable salt, or the hydrate thereof, and (3) the layer containing the material having a damp-proofing function.

Abstract: The invention provides a method of preventing or reducing the growth of crystals in a substance which is susceptible to crystal growth in which colloidal particles having an amphiphilic structure, e.g. Janus particles, are contacted with the substance. Colloidal particles suitable for use in the invention include cross-linked, colloidal materials formed from hydrophobic monomers such as acrylates or methacrylates and hydrophilic monomers such as those derived from acrylic and/or methacrylic acid. The colloidal particles find particular use in methods of cryopreservation of biological samples (e.g. cells, tissues or organs), as a texture modifier in frozen food products, in the inhibition of gas hydrate formation, and as scale inhibitors.

Abstract: Benzonatate resinates of weak acid ion exchange resins having the same distribution of butyl 4-aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210. These resinates, in simulated gastrointestinal dissolution, release essentially the same distribution of butyl-4 aminobenzoate homologs as exist in the benzonatate listed in the F.D.A. Orange Book as Application No. N011210.

Abstract: Controlled release particles are obtained by dissolving a hydrophobic antibiotic compound in a hydrophobic polymerizable vinyl monomer without the presence of a solvent, thereby preparing a hydrophobic solution, the hydrophobic antibiotic compound having a melting point of 100° C. or less, a polar term ?p,compound of 2 to 8 [(J/cm3)1/2] of a solubility parameter (?) and a hydrogen bonding term ?h,compound of 5.5 to 9.5 [(J/cm3)1/2] of the solubility parameter (?), the solubility parameter (?) defined by Hansen and calculated by van Klevelen and Hoftyzer method; dispersing the hydrophobic solution in water; and polymerizing the polymerizable vinyl monomer in the presence of an oil-soluble initiator by radical polymerization, thereby producing a polymer having a polar term ?p,polymer of 5 to 7 [(J/cm3)1/2] and a hydrogen bonding term ?h,polymer of 8 to 10 [(J/cm3)1/2] of the solubility parameter (?).

Abstract: A delivery vehicle including a mixture of: a) an effective amount of an expander activatable by a wetting agent and, b) a treatment agent. The expander and treatment agent intermingled and compressed so as to form a substantially solid delivery vehicle. The solid delivery vehicle, on exposure to a volume of wetting agent forms a predetermined volume of a paste containing the treatment agent; and the volume of paste is adapted for delivery of the treatment agent.

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: The process for manufacturing porous nanoparticles disclosed herein includes feeding a dry-blended mixture of at least one resin and a neutralizing agent into a feed section of a screw extruder, injecting a surfactant solution downstream of the hopper, and adding an aqueous composition both directly after the surfactant solution as well as further downstream. Porous nanoparticles having a particle size of from about 50 nm to about 2 ?m and a pore diameter of from about 20 nm to about 400 nm may be continuously recovered from the extruder following this process.

Abstract: The present invention relates to injectable compositions comprising biocompatible, hydrophilic, non-toxic and substantially spherical microspheres associated with stem cells useful for tissue construction and generation. The invention also relates to methods of tissue construction and generation, for the treatment of various tissue damage and defects, using the injectable compositions.

Abstract: Microparticles and nanoparticles and compositions thereof are provided. The microparticles and nanoparticles and compositions may be used for the treatment of musculoskeletal disease, such as osteoarthritis and injury.

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: Colloidal suspensions comprising a therapeutic agent and squalene. Squalene binds to certain compounds, such as gacyclidine, much more tightly than other drug carriers, such as polylactic glycolic acid. Including squalene in the particulate phase sequesters the therapeutic agent and provides superior stability at room or body temperature.

Abstract: The present disclosure generally relates to a process for preparing therapeutic nanoparticles, where the process includes combining a therapeutic agent with an organic acid. The therapeutic nanoparticles may have, for example, improved drug loading and/or drug release properties.

Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a mTOR inhibitor; and about 70 to about 99 weight percent biocompatible polymer.

Abstract: Disclosed herein are process for preparing cyclic esters comprising unsaturated functional groups. Also disclosed are copolymers prepared from the cyclic esters. The copolymers can be used to form microparticles, polymer micelles, etc., which are useful in drug delivery applications.

Abstract: A local system for the release of active principle is described which consists of approximately spherical or rotation symmetrical bodies which are composed essentially of polymethyl methacrylate or polymethyl methacrylate co-methyl acrylate, zirconium dioxide or barium sulphate and one or more pharmaceutical active principles, in particular antibiotics, and which are produced by radical polymerization, radical polymerization activators effective in the temperature range of 10-80° C. or residues of these polymerization activators from the groups of aromatic amines, heavy metal salts and barbiturates not being contained therein.

Abstract: Biodegradable polymeric nanoparticles comprising an inner core formed of a photodynamic agent capable of being activated to generate cytotoxic singlet oxygen are prepared. These nanoparticles have anti-cell proliferation activity and are useful in treating both cancerous and non-cancerous conditions including actinic keratosis, psoriasis and acne vulgaris. Preferably, the photodynamic agent is a hypocrellin B derivative while the polymeric nanoparticle comprises polyglycolic acid, polylactic acid or poly(lactide-co-glycolide). Hypocrellin-comprising nanoparticles are demonstrated to be activated by light or hydrogen peroxide.

Abstract: The present invention relates to injectable compositions comprising biocompatible, swellable, substantially hydrophilic, non-toxic and substantially spherical polymeric material carriers which are capable of efficiently delivering bioactive therapeutic factor(s) for use in embolization drug therapy. The present invention further relates to methods of embolization gene therapy, particularly for the treatment of angiogenic and non-angiogenic-dependent diseases, using the injectable compositions.

Abstract: Provided herein are methods of making and controlling multiphasic polymeric micro-components capable of shape-shifting. Such a multiphasic micro-component comprises a first phase (that can include a first polymer) and at least one additional phase distinct from said first phase (that can include a second polymer). One or more of the first phase and additional phase comprises a component that is responsive to an external stimulus. Thus, the micro-component exhibits a substantial physical deformation in response to: (i) the presence of the external stimulus or (ii) a change in the external stimulus. Exemplary external stimuli include temperature, pressure, light, pH, ionic strength, hydrophobicity/hydrophilicity, solvent, concentration, a stimulator chemical, sonic energy, electric energy, pressure, magnetic fields, and combinations thereof.

Abstract: The invention relates to an oral, multiparticle pharmaceutical dosage form containing pellets, the size of which ranges from 50 to 2500 ?m and which essentially consist of: a) an inner matrix layer containing an active substance which is a peptide or a protein, including the derivatives or conjugates thereof, and which is embedded in a matrix consisting of a polymer with mucoadhesive effect, and b) an outer film coating essentially consisting of an anionic polymer or copolymer, which can be optionally formulated with pharmaceutically conventional adjuvants, more particularly softening agents.

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: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: A multiparticulate dosage form formulated to make misuse more difficult containing least one active substance with potential for misuse (A), at least one synthetic or natural polymer (C), optionally at least one natural, semi-synthetic or synthetic wax (D), at least one disintegrant (E) and optionally one or more additional physiologically compatible excipients (B), wherein the individual particles of the dosage form display a breaking strength of at least 500 N and a release of active substance of at least 75% after 45 minutes measured according to Ph.Eur. in the paddle mixer with sinker in 600 ml of aqueous buffer solution with a pH value of 1.2 at 37° C. and 75 rpm.

Abstract: Biocompatible microparticles include an ophthalmically active cyclic lipid component and a biodegradable polymer that is effective, when placed into the subconjunctival space, in facilitating release of the cyclic lipid component into the anterior and posterior segments of an eye for an extended period of time. The cyclic lipid component can be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the cyclic lipid component can be encapsulated by the polymeric component. The present microparticles include oil-in-water emulsified microparticles. The subconjunctivally administered microparticles can be used to treat or to reduce at least one symptom of an ocular condition, such as glaucoma or age related macular degeneration.

Abstract: The present invention provides biocompatible nano-polymer particles which are composed of a biocompatible polymer, a stabilizer and an active agent for the treatment of pulmonary hypertension or erectile dysfunction and which can be used to produce a pharmaceutical preparation for the treatment of pulmonary hypertension or erectile dysfunction. Biocompatible nano-polymer particles of this invention have a diameter ranging from 10 nm to 10 ?m auf, a stabilizing layer thickness between 0 and 50 nm, contain between 0 and 50% of an active agent for the treatment of pulmonary hypertension or erectile dysfunction, are nebulizable and continuously release the active agent over a period of up to 48 hours. Biocompatible nano-polymer particles of this invention can be synthesized for example using the emulsion technique known to the expert with subsequent solvent evaporation or via spray drying.

Abstract: Polymeric nanoparticles with a hydrophobic core and a hydrophilic shell are formed from: 1) N-isopropylacrylamide (NIPAAM), at a molar ratio of about 50% to about 90%, and preferably 60% for specific delivery routes such as oral or parenteral; either water-soluble vinyl derivatives like vinylpryolidone (VP) or vinyl acetate (VA), or water insoluble vinyl derivatives like methyl methacrylate (MMA) or styrene (ST), at a molar ratio of about 10% to about 30%; and acrylic acid (AA), at a molar ration of about 10% to about 30%.

Abstract: Methods for preparing uniformly sized micropanicles, with an optional polymeric coating generally include: 1) providing nanoparticles, preferably having a size of between 1 nm and 100 nm; 2) adding a hydrophobic surface layer to the nanoparticles; 3) making a suspension of the hydrophobic nanoparticles and a polymerization initiator in an hydrophobic solvent; 4) dissolving a monomer in the hydrophobic solvent; 5) making an emulsion by dispersing droplets of the hydrophobic solvent in a continuous aqueous phase with an emulsifier; 6) sizing the first emulsion to provide a second emulsion of the same components in which the droplets are substantially uniform and between 2 and 20 um in size; 7) evaporating at least a substantial portion of the dispersed hydrophobic droplets to assemble nanoparticles to form micropanicles suspended now in the aqueous phase; 8) replacing the first surfactant with a second surfactant, which is preferably a polymerizable surfactant; 9) adding a polymerizable monomer to the aqueous p

Abstract: A process for preparing polymeric composite particles includes the steps of preparing an oil phase containing a biodegradable polymer and a water phase containing a hydrophilic compound or nanoparticle and emulsifying the oil phase in the water phase to form emulsions. Then solvent is removed from the emulsions to prepare the particles in the form of capsules and spheres in sizes from 0.01 ?m (10 nm) to 50 ?m.

Abstract: The present invention relates to micro- or nanoparticles comprising a polyesteramide (PEA) having a chemical formula described by structural formula (IV), Formula (IV) wherein —m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9 —m+p+q=1 whereby m or p could be 0-n is about 5 to about 300; (pref 50-200) —R1 is independently selected from the group consisting of (C2-C20) alkylene, (C2-C20) alkenylene, —(R9—CO—O—R10—O—CO—R9)—, —CHR11—O—CO—R12—COOCR11— and combinations thereof; —R3 and R4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C1C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C10)aryl, (C1-C6)alkyl, —(CH2)SH, —(CH2)2S(CH3), —CH2OH, —CH(OH)CH3, —(CH2)4NH3+, —(CH2)3NHC(?NH2+)NH2, —CH2COOH, —(CH2)COOH, —CH2—CO—NH2, —CH2CH2—CO—NH2, —CH2CH2COOH, CH3—CH2—CH(CH3)—, (CH3)2—CH—CH2—, H2N—(CH2)4—, Ph-CH2—, CH?C—CH2—, HO-p-Ph-CH2—, (CH3)2—CH—, Ph-NH—, NH—(CH2)3—C—, NH—CH?N—CH?C—CH2—.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. In a particular embodiment, the drug dosage form comprises a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: The organic polymer particles comprise a carboxyl group and 2,3-dihydroxypropyl group, and the magnetic particles for diagnostics comprise fine magnetic material particles and a polymer part containing a hydrophilic polymer part and a crosslinked polymer part, a dry coating film obtained from a water dispersion thereof having a contact angle with water of 5° to 60°. The process for producing the carboxyl group-containing particles comprises a step of producing an ester bond by reacting a hydroxyl group in organic polymer particles having the hydroxyl group with a carboxylic anhydride. The organic polymer particles comprise a hydroxyl group originating from a 2,3-dihydroxypropyl group and a polyoxyethylene group.

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

Abstract: A method for treating a surface with a therapeutic agent is disclosed. The method comprises precipitating a therapeutic agent from a hydrophilic polymeric base layer with which the therapeutic agent has been complexed, to form a layer comprising microparticles of the therapeutic agent on the hydrophilic polymeric base layer, the hydrophilic polymeric base layer being grafted to the surface. Devices comprising a surface having a hydrophilic polymeric base layer comprising a hydrophilic polymer grafted to the surface and a layer comprising microparticles of a therapeutic agent disposed on and complexed with the hydrophilic polymeric base layer are also disclosed.

Abstract: The present invention relates to injectable compositions comprising biocompatible, swellable, substantially hydrophilic, non-toxic and substantially spherical polymeric material carriers which are capable of efficiently delivering bioactive therapeutic factor(s) for use in embolization drug therapy. The present invention further relates to methods of embolization gene therapy, particularly for the treatment of angiogenic and non-angiogenic-dependent diseases, using the injectable compositions.

Abstract: A method for protection of tissues subject to ischemic and/or reperfusion damage is provided. The method includes administering to the tissue a composition comprising nanodevices. The nanodevices can take the form of, for example, polymeric nanoparticles or lipidic nanoparticles. The nanodevices also find use in methods for reducing ischemic injury in tissue at risk of such injury, such as heart and brain tissue.

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 are low-volume, safe for injection formulations of dantrolene yielding significant advantages over the currently approved and marketed dantrolene for malignant hyperthermia (MH) threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. The low volume, safe for injection formulations of dantrolene have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.

Abstract: A process for preparing the drug-loaded cyanoacrylate nanoparticles is described. The cyanoacrylate nanoparticles which effectively deliver biological and therapeutic agents are synthesized by miniemulsion polymerization with surfactant, pluronic F127 or F68. Before initiation of polymerization, active agents with particularly highly hydrophobicity are dissolved in cyanoacrylate monomer. Compared with the drug-loaded polyalkylcyanoacrylate nanoparticles produced by emulsion polymerization, those produced by miniemulsion polymerization possess higher loading and encapsulation efficiencies. While the content of dissolved agents increases, furthermore, the loading and encapsulation efficiencies increase concurrently.

Abstract: The present invention relates generally to vesicles such as liposomes, colloidosomes, and polymersomes, as well as techniques for making and using such vesicles. In some cases, the vesicles may be at least partially biocompatible and/or biodegradable. The vesicles may be formed, according to one aspect, by forming a multiple emulsion comprising a first droplet surrounded by a second droplet, which in turn is surrounded by a third fluid, where the second droplet comprises lipids and/or polymers, and removing fluid from the second droplet, e.g., through evaporation or diffusion, until a vesicle is formed. In certain aspects, the size of the vesicle may be controlled, e.g., through osmolarity, and in certain embodiments, the vesicle may be ruptured through a change in osmolarity. In some cases, the vesicle may contain other species, such as fluorescent molecules, microparticles, pharmaceutical agents, etc., which may be released upon rupture.

Abstract: The present invention relates to elastic, hydrophilic and substantially spherical microspheres useful for dermal augmentation and tissue bulking. The invention provides injectable compositions comprising the microspheres and a biocompatible carrier for use in dermal augmentation. The present invention further provides methods of dermal augmentation and tissue bulking, particularly for the treatment of skin contour deficiencies, Gastro-esophageal reflux disease, urinary incontinence, and urinary reflux disease, using the injectable compositions.

Abstract: The present invention relates to elastic, hydrophilic and substantially spherical microspheres useful for dermal augmentation and tissue bulking. The invention provides injectable compositions comprising the microspheres and a biocompatible carrier for use in dermal augmentation. The present invention further provides methods of dermal augmentation and tissue bulking, particularly for the treatment of skin contour deficiencies, Gastro-esophageal reflux disease, urinary incontinence, and urinary reflux disease, using the injectable compositions.