Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising sodium-binding polymers and pharmaceutical compositions thereof. 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 hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.

Abstract: This invention discloses a process for making nanopanticles of amphiphilic copolymers by flash precipitation. Nanoparticles may be of amphiphilic copolymer alone or may contain an additive target molecule, preferably an organic active. The inclusion of additive target molecules in amphiphilic copolymer nanoparticles can alter their water solubility characteristics, fluid dynamics, and/or stability. Changing an additive target molecule's solubility and stability in an nanoparticle can make a water insoluble compound suitable for pharmaceutical administration as well as specifically target the molecule to a specific area of a patient's body. The process affords the production of nanoparticles at high absolute active content, at high yield, high productivity, and high processing rates while using unusually low amounts of amphiphilic copolymers. Furthermore, the resulting particles exhibit sufficient stability for post processing as desired.

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: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.

Abstract: A water soluble cosmetic or pharmaceutical or pharmaceutical actives in an electrolyte solution which, when impregnated with one or more retentive fillers (such as, for example, silica or hydrophobically modified silica, lamellar filler, crosspolymer, cellulosic, resins, or silicone elastomers) can form stable solid compositions with structurants. Such solid compositions do not require a higher buffer pH or leave residues upon application to the skin. Solid compositions according to the present invention are suitable for cosmetic and pharmaceutical purposes such as antiperspirants, deodorants, lip products, and other topical applications.

Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.

Abstract: The present invention relates to a pH-sensitive PIC (polyion complex) type polymeric micelle formed by electrostatic interaction between a dendritic block copolymer and another polymer of opposite charge. The presence of a dendritic block copolymer confers high stability to the micelles in physiological conditions, while in the acid medium of tumor tissues (pH 6.5) or cell compartments, such as the endosome/lysosome (pH 5.0-5.5), the micelles tend to become destabilized, being able to selectively release drugs or macromolecules encapsulated therein. The micelles are characterized by high stability against ionic strength, dilution and temperature. They can further be lyophilized and conserved in solid state.

Abstract: The present invention provides compositions comprising dicyclomine, or salts, and/or solvates and methods of making and using the compositions to treat intestinal hypermotility or Irritable Bowel Syndrome (IBS). The present invention also provides once-a-day orally disintegrating dosage forms comprising compositions of the present invention.

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, at least in part, to compositions comprising populations of synthetic nanocarriers that comprise different sets of antigens as well as related methods.

Abstract: The present invention provides a compositions and methods for the treatment of cancer, including pancreatic cancer, breast cancer and melanoma, in a human patient. The methods and compositions of the present invention employ curcumin or a curcumin analogue encapsulated in a colloidal drug delivery system, preferably a liposomal drug delivery system. Suitable colloidal drug delivery systems also include nanoparticles, nanocapsules, microparticles or block copolymer micelles. The colloidal drug delivery system encapsulating curcumin or a curcumin analogue is administered parenterally in a pharmaceutically acceptable carrier.

Abstract: The present invention relates to certain novel polymer powder compositions suitable for personal care and cosmetic compositions. The present invention also relates to cosmetic compositions comprising such novel polymer powders. The present invention also relates to processes for manufacturing the polymer powders, methods of making cosmetic and personal care compositions and the use of such cosmetic compositions in topical applications.

Abstract: A method for embolization treatment was developed in which microspheres with novel properties are administered in a mammal. The microspheres are made using a novel process that results in microspheres with new combined properties of high density, low fracture, high swell capacity, rapid swell, and deformability following swell. These microspheres form occlusions with high durability, withstanding over 100 mm Hg (13.3 kPa) of pressure.

Abstract: Immunogenic compositions are disclosed which comprise microparticles that comprise a biodegradable polymer, an immunological adjuvant and a tocol-family compound. Methods of making and using such microparticle compositions are also disclosed.

Abstract: The invention relates to soluble selenium compositions and methods of production, separation and purification thereof. In particular the present invention provides methods of preparing water soluble selenoglycoproteins (e.g., via extracting selenoglycoproteins from selenium enriched yeast), methods of supplementing a selenium deficient composition via admixing water soluble selenoglycoproteins with the selenium deficient composition, compositions comprising the water soluble selenoglycoproteins and methods of administering the same.

Abstract: A particle includes a ferromagnetic material, a radiopaque material, and/or an MRI-visible material.

Abstract: Compositions and methods of using the compositions to achieve a therapeutic effect are provided.

Abstract: Substantially non-porous polymeric microparticles comprising a hydrophobic polymer and a plasticizer, and containing therein a bioactive or bioinactive agent.

Abstract: The present invention relates to compositions comprising 4-(2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazol-3-ylthio)acetamido)-3-chlorobenzoic acid or pharmaceutically acceptable salts thereof, and to the preparation and use of such compositions, in particular for the treatment of diseases.

Abstract: Gel particles or beads can be prepared by forming a hot aqueous solution of a gelling agent, and discharging the hot gelling agent solution through a discharge orifice into a cold moving stream of hydrophobic liquid so that the gelling agent solution cools rapidly and good quality gel particles coalesce in the cold hydrophobic liquid stream. The cold hydrophobic liquid stream can be contained in a conduit so that the cold hydrophobic liquid stream moves past the discharge orifice and exerts a force on hot solution in the discharge orifice, the force acting to withdraw the hot solution from the discharge orifice. Optionally, the gel particles can be crushable gel beads 10 formed of an agar complex providing cosmetic, pharmaceutical, etc. delivery vehicles for topical delivery of biologically or cosmetically active agents. Preferred agar beads 10 are complexes of a continuous phase of agar gel 12 in a self-supporting solid or semi-solid form with a restraining polymer 14.

Abstract: A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration—time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.

Abstract: The present invention relates to method of targeting therapeutic agents for treating lung diseases.

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: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents such as AG1478 to induce nerve regeneration, specifically regeneration of the optic nerve useful for managing elevated intraocular pressure (TOP) in the eye.

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 disclosure generally relates to a method of producing a handleable wafer of medicament powder (for example, aspirin powder) by utilizing a restraining envelope of fine water-soluble fibers, which are, upon use, quickly dissolved by bodily fluids. Such wafer would quickly provide sublingual or buccal cavity medications without significant excipients. Additional applications for such a wafer is in the prompt provision of a variety of medicaments to selected moist areas, such as, surgery or trauma sites, such as, a wound dressing.

Abstract: The invention provides porous biomaterials and methods for forming porous biomaterials. The porous biomaterials of the invention comprise a biocompatible polymer scaffold defining an array of pores, wherein substantially all the pores have a similar diameter, wherein the mean diameter of the pores is between about 20 and about 90 micrometers, wherein substantially all the pores are each connected to at least 4 other pores, and wherein the diameter of substantially all the connections between the pores is between about 15% and about 40% of the mean diameter of the pores. The invention also provides implantable devices comprising a layer of a biomaterial, and methods for promoting angiogenesis in and around an implantable biomaterial.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: A method of stimulating an immune response in a subject including administering a micrometer-sized particle coupled with an antigen to the subject, wherein increasing the aspect ratio of the micrometer-sized particle increases the immune response. A method of stimulating an immune response in a subject including administering to the subject a plurality of particles, wherein each particle is coupled with an immuno stimulating agent and a protein. A vaccine particle composition including a plurality of particles configured to release a first protein at a first rate and a second protein at a second rate and configured to provide priming and boosting capability in a single dose.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: The present invention provides compositions and methods for the controlled release delivery of one or more biologically active compounds to a subject. Specifically, the invention provides for a pharmaceutical composition for the controlled release delivery of biologically active compounds to a subject comprising: a) a complex of a biologically active compound having at least one basic functional group and a polyanion derived from hexahydroxycyclohexane having at least two negatively charged functional groups; and b) a pharmaceutically acceptable carrier comprising a biodegradable, water-insoluble polymer. By complexing a biologically active compound with a polyanion, the tight, stable complex may be incorporated into a long-acting dosage system having a more desired drug release curve over time than that is found in the prior art. The invention also provides the methods of making such compositions and the methods of use thereof.

Abstract: The present invention discloses pharmaceutical composition comprising phosphate binding polymers such as Sevelamer carbonate substantially free of monovalent anion other than bicarbonate anion. Particularly, monovalent anion content is less than about 0.05% (w/w). Disclosed are compositions comprising wet granulated Sevelamer carbonate free of added metal ions and/or added monovalent anion source.

Abstract: Composition comprising a polymeric micelle and an associated polynucleotide.

Abstract: This invention relates to crosslinked amine-containing polymers for binding compounds or ions, and more specifically relates to pharmaceutically acceptable compositions for binding compounds or ions that include crosslinked amine-containing polymers. The pharmaceutically acceptable composition includes, for example, crosslinked polyamine particles, or pharmaceutically acceptable salts thereof, having a particle size distribution wherein greater than 10 vol. % of the particles have a particle size greater than 500 ?m.

Abstract: There are provided compositions and methods to disperse mucin and/or actin using nanoparticles wherein the average diameter of the nanoparticles is less than about 1000 nm.

Abstract: The invention relates to a novel suspension delivery system for the sustained and controlled release of pharmaceuticals. Methods of preparation and use are also disclosed.

Abstract: The present invention relates to a novel family of polymers of acrylic and/or methacrylic type, comprising alpha-tocopherol grafts, capable of forming nanoparticles in an aqueous medium at a neutral pH. It also relates to the use of such nanoparticles, non-covalently combined with an active ingredient, in particular an active ingredient of low or average aqueous solubility, for conveying, solubilizing and/or increasing the aqueous solubilization of said active ingredient.

Abstract: A drug delivery particle including a reservoir region having primarily large pores and a metering region. The particle can be highly spherical.

Abstract: The present invention is directed to the use of an agent selected from ethyl alcohol, isopropyl alcohol or a mixture thereof and a topically acceptable polymeric carrier in the preparation of a composition for the treatment of burns.

Abstract: Disclosed are cement products, methods of forming cement using the cement product, and methods of using the cement product in orthopedic and dental applications. Generally, the disclosed cement product includes a first component comprising a polymerizable resin comprising ethylenic unsaturated double bond, a second component comprising a compound comprising more than one type of amine selected from the group consisting of primary amines, secondary amines, tertiary amines and quaternary amines, and, optionally, the cement product includes a bioactive component to promote bone formation.

Abstract: A process of the present invention is directed toward conducting highly selective, high yield post-polymerization reactions on polypeptides to prepare functionalized polypeptides. In certain embodiments, the polypeptides can be prepared by ring opening polymerization of N-carboxyanhydrides. In certain embodiments, the post-polymerization reaction is a “click chemistry” reaction. In certain embodiment, the “click chemistry” reaction is a triazole-forming reaction involving an alkyne on the polypeptide and an azide.

Abstract: The present invention provides a Monodisperse Polymer Particles (MPP) adapted to release alkoxy groups by means of a hydrolyser, such that Monodisperse Bioactive Polymer Particles (MBPP) are obtained in vivo. The MBPP are characterized by (a) at least one naturally occurring or synthetic long molecular chain consisting of biologically stable backbones optionally crosslinked, further characterized by a molecular weight of at least 1 KD, comprising between 10 to 1,000,000 repeated covalently-linked small molecules with a functionality of at least one alkoxy releasing group per molecule; (b) a long dimension between 0.1 and 10 micrometers; and, (c) a zeta potential value of 30 to 130 mV at pH of about 7.0. The MBPP alter, inhibit, activate, induce or otherwise affect biological or chemical events in vivo.

Abstract: The present application discloses a sustained release composition in pellet form, wherein the core of the pellet comprises: (a) a therapeutically effective amount of a medicament; (b) 0.5 to 50% by weight of a water-soluble polymer; and (c) 25% by weight of a water-insoluble polymer applied as an aqueous latex dispersion and subsequently the water is removed, wherein the sum of the percentages of the medicament, the water-insoluble polymer and the water-soluble polymer is equal to or less than 100%. It also discloses methods of making this composition.

Abstract: The present invention comprises a plurality of injectable hollow particulate fillers suspended in a biocompatible fluid carrier to significantly improve the clumping resistance and injectability of the composition. The hollow particulate fillers have a lower effective density and are able to suspend in the carrier without precipitation. The loss of skin volume as a result of aging, diseases, weight loss, and injury can lead to uneven skin surface (e.g. wrinkle, etc.). The uneven skin can be repaired by injecting appropriate amount of hollow fillers underneath the skin. Some cases of urinary incontinence occur when the resistance to urine flow has decreased excessively. Continence is restored by injecting the present invention to the urethra tissue to increase resistance to urine outflow. Similarly, the present invention allows for the control of gastric fluid reflux by submucosal injections of the fillers to the esophageal-gastric and gastric-pyloric junction.

Abstract: The present invention discloses pharmaceutical composition comprising phosphate binding polymers such as Sevelamer carbonate substantially free of monovalent anion other than bicarbonate anion. Particularly, monovalent anion content is less than about 0.05% (w/w). Disclosed are compositions comprising wet granulated Sevelamer carbonate free of added metal ions and/or added monovalent anion source.

Abstract: Methods and compositions for providing long term pain relief in, for example, surgery recovery, including injecting a composition comprising a plurality of microparticles having different sizes and at least one local anesthetic loaded into the microparticles at different loading levels. Extended prolonged blockage of nerve action in sheep testing was confirmed. Some of the microparticles comprise a high loading of local anesthetic. Testing in sheep showed nerve blockage for at least six days.

Abstract: Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization.

Abstract: The invention discloses the bioactive nanoparticles composed of chitosan, poly-glutamic acid, and at least one bioactive agent characterized with a positive surface charge and enhanced permeability in oral drug delivery.

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.