Abstract: A method of forming particles, comprises accelerating a first stream comprising a first liquid, applying a charging voltage of at most 1.5 kV to the first stream, and vibrating the first stream, to form particles.

Abstract: Disclosed is a method of stimulating bone growth at a site in a subject in need of osteoinduction. The method comprises the step of administering a therapeutically effective amount of an agonist of the non-proteolytically activated thrombin receptor to the site.

Abstract: The invention relates to a preparation comprising a carrier phase and at least one further phase which cannot be mixed with the carrier phase or only partially mixed therewith, wherein the change in ambient conditions alters the viscosity of the carrier phase. The invention also relates to a method for the production thereof and to particles and implants containing said preparations. The inventive preparations can contain various active substances with a delayed release action.

Abstract: Bioadhesive nanoparticulate compositions, comprising active agent particles and one or more cationic surface stabilizers, are described. The cationic surface stabilizers prevent aggregation of the nanoparticles and increase bioadhesion of the nanoparticles to biological substrates, such as an insect, teeth, bone, nails, chitin, feathers, scales, mucous, skin, hair, plant tissue, etc. The particles may consist of pharmacologically active compounds (e.g., drug compounds for human or veterinary use), agricultural chemicals (pesticides, herbicides, fertilizers, and the like), cosmetic agents, consumer products (coloring agents, flavors, or fragrances), or other materials which function by interacting with biological substrates. In addition, the invention relates to methods of preparing and using such bioadhesive nanoparticulate compositions.

Abstract: One of the most prominent amino acids found in biological proteins is aspartic acid. In the present invention L-aspartic acid was heated at 150 deg C for up to 100 hrs to form thermal polyaspartylimide which when heated in boiling water without addition of base hydrolyzed to form thermal polyaspartic acid which upon cooling formed protective biocompatible microcapsules.

Abstract: This invention provides methods and compositions to preserve bioactive materials in a matrix of powder particles. Methods provide high-pressure gas spraying and/or near supercritical spraying of formulations followed by drying in a stream of conditioned gas to form stable powder particles containing bioactive materials.

Abstract: The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

Abstract: The invention provides proteinoid microsphere made up of a mixture of thermally condensed amino acids that are crosslinked with a bis dithiol crosslinker reagent. The proteinoid microspheres of the invention may be used to encapsulate a material or a compound and to provide slow, sustained or timed release of the material or compound. The proteinoid microspheres are stable in solution until exposed to a reducing agent. However, the in vivo environment provides a sufficient reduction potential to provide slow, sustained release of materials contained therein from the proteinoid microspheres of the present invention.

Abstract: A suspension of vector particles (PV) based on polyamino acids and have a mean hydrodynamic diameter between 30 and 120 nm, and an insulin load factor of from 5 to 25% of associated insulin volume relative to the polyamino acid volume forming the vector particles. The polyamino acids are double-block polymers containing hydrophilic and hydrophobic monomers. The suspension may be prepared by copolymerizing N-carboxy anhydrides of hydrophobic monomers and precursors of hydrophilic monomers, in the presence of N-methyl pyrrolidone and methanol. The copolymer is optionally neutralized, subjected to dialysis, concentrated and water is eliminated to produce a solid powder, which can be suspended in a liquid to produce the colloidal suspension. Active principles such as insulin or vaccines are associated with the carrier particles to prepare special pharmaceutical products.

Abstract: Provided is a method of isolating a bio-molecule from a water-borne mixture, the method comprising: contacting the water-borne mixture with dimethyl ether to form solid particles of the bio-molecule.

Abstract: UEA-1 Mimetics, pharmaceutical formulations comprising them, and their uses as targeting agents for therapeutic and diagnostic purposes.

Abstract: Methods and reagents for improved treatment and diagnostic imaging, particularly of cancer. The methods and reagents utilize specific targeting of treatment and imaging ligands to the targeted tumor, or specific organ or tissue, in association with extracorporeal affinity adsorption of the targeting ligand. The targeted species include antibodies as well as other peptides with specific affinity to the targeted tumor organ or tissue. Included are hybrid targeting molecules, such as hybrid F(ab?)2, with one binding site specific for the target and the other binding site specific for the targeted treatment or visualization ligand. The affinity adsorption devices may include adsorbents specific to one or more of the components of the targeting molecule-targeted ligand moiety.

Abstract: The present inventive subject matter relates to amorphous drug beads comprising an amorphous active drug and an organic surfactant having improved solubility, absorption and wettability characteristics. The present inventive subject matter further relates to methods of preparing the amorphous drug beads, wherein molten drug beads are subject to a cooling step with or without shear.

Abstract: NGF microencapsulation compositions having controlled release characteristics, preferably with increased stability, for the NGF component, particularly human recombinant NGF (“rhNGF”) are provided that yield enhanced stability of NGF for use in promoting nerve cell growth, repair, survival, differentiation, maturation or function. Methods for making and using such compositions are also provided.

Abstract: Methods and compositions for delivering macromolecules to or via the respiratory tract, such that the macromolecules exhibit improved local and/or systemic bioavailability are provided. Such methods utilize lipid-based microstructures formed in combination with at least one bioactive macromolecule, which have a superior ability to rapidly release the bioactive macromolecule(s) thereby resulting in improved local and/or systemic bioavailability of the bioactive macromolecule(s). Such improved bioavailability is believed to be due, in part, to reduction of scavenging by bronchoalveolar macrophages and/or mucociliary clearance.

Abstract: Disclosed is an oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof, the preparation comprising at least one sustained-release coated particle comprising a core having a surface and a coating formed on the surface of the core, wherein the core contains the active ingredient and the coating comprises a coating base material and a specific insoluble auxiliary material, and wherein the preparation exhibits, with respect to the active ingredient, a specific dissolution rate, as measured by the dissolution test. By using the oral sustained-release preparation of the present invention, it becomes possible to surely control the release of fasudil hydrochloride from the preparation, so that the effect of the active ingredient is maintained for a long period of time.

Abstract: The present invention teaches an improved process for preparing a population of microcapsules having a substantially uniform size distribution, especially useful for manufacture of carbonless paper. The improved process teaches use of membrane material having a pre-selected pore size in the capsule manufacture process. A core material is provided along with a receiving solution for receiving the core material. The receiving solution is a nonsolvent for the core material. The core material is passed under pressure through the membrane into a moving or turbulent receiving solution forming uniform droplets of core material dispersed in the receiving solution. Wall-forming material is added to the receiving solution for coating the core material droplets. The coating on the droplets is polymerized forming microcapsules. This novel process also lends itself to microcapsule formation in a continuous process.

Abstract: An effective prophylactic mucosal gene expression vaccine (GXV), made up of a cocktail of at least 4 different plasmid DNAs encoding corresponding RSV antigens, coacervated with chitosan to formulate nanospheres. In a murine model of RSV infection, intranasal administration with GXV results in significant induction of RSV-specific antibodies, nasal IgA antibodies, cytotoxic T lymphocytes, and IFN-? production in the lung and splenocytes. A single dose of GXV induces a drastic reduction of viral titers.

Abstract: The present invention relates to an improved controlled release system that can be incorporated into anhydrous cosmetic formulations and can encapsulate different types of fragrances, flavors, active ingredients, or combinations of fragrances, flavors, and various active ingredients. The controlled delivery system of the present invention is substantially free-flowing powder formed of solid hydrophobic nano-spheres that are encapsulated in a moisture sensitive micro-spheres. The fragrances, flavors, and active ingredients encapsulated in the nano-spheres can be the same or different from those encapsulated in the micro-sphere. The encapsulation of one or more fragrances, flavors or active agents in the various components of the system, such as nano-spheres and micro-spheres, provides odor or flavor transition (change in odor character or change in flavor character) during the use of the product, in response to moisture, such as wetting the lips, perspiration, and the like.

Abstract: A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

Abstract: Compositions useful in treating immune modulated disease comprising an anticytokine antibody or immune active drug capable of modifying cytokine activity or modulating the immune system microencapsulated with a biodegradable nonantigenic material, such as albumin or PLGA. When the composition is introduced into a subject, it is phagocytosed by the target organ, the target organ digests the microsphere, releasing the drug or an active form or fragment thereof intracellularly. The drug then modifies the target organ function, thereby modulating it's activity. A method is disclosed for preparation of the microencapsulated composition.

Abstract: The present invention is directed to sustained release microparticle formulation for parenteral administration of biologically active substances, especially drugs. More specifically it relates to coated drug containing microparticles, wherein the coating is a synthetic, bioabsorbable, biocompatible polymeric wax that is the reaction product of a polybasic acid or derivative thereof, a polyol and a fatty acid, the polymeric wax having a melting point less than about 70° C., as determined by differential scanning calorimetry.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: The present invention relates to a sustained release composition for the targeted delivery of biologically active agents to specific tissues and cells. The composition comprises microparticles containing a biocompatible polymer, a water-soluble polymer and a biologically active agent. In one embodiment, the biologically active agent is an antigen or an immunomodulator. In another embodiment, the biologically is a labile agent. The microparticles have a number median diameter of greater than 20 microns upon administration. The water-soluble polymer is present in the sustained released composition in at least about 20% of the dry weight of the microparticle. The sustained release composition provides for the dissolution of the water-soluble polymer of the composition upon hydration, at a much greater rate than the degradation of the biocompatible polymer.

Abstract: A medicinal preparation capable of lowering the threshold of cavitation and generating active oxygen species via acoustic cavitation caused by an ultrasound is provided. The preparation, which is to be used in combination with ultrasonic irradiation, comprises a shell within the internal space of which a gas is enclosed and which contains or retains a substance capable of generating active oxygen species upon ultrasonic irradiation of the shell.

Abstract: The invention relates to a process for producing dry powders of one or more carotenoids by a) dispersing one or more carotenoids in an aqueous molecular or colloidal solution of a mixture of lactose and a protective colloid and b) converting the dispersion which has formed into a dry powder by removing the water and, where appropriate, additionally used solvents and drying, where appropriate in the presence of a coating material, wherein at least one soybean protein is used as protective colloid in process step a).

Abstract: The present invention relates to cosmetic formulations comprising a multi component controlled release system that imparts long lasting cooling sensation and/or provides high odor or flavor intensity (i.e., high impact fragrance or flavor burst) in response to moisture. The controlled delivery system of the present invention is substantially free-flowing powder formed of solid hydrophobic nano-spheres that are encapsulated in a moisture sensitive micro-spheres.

Abstract: Disclosed herein are biodegradable microparticle compositions, and methods for the generation of biodegradable and biocompatible microparticles that stabilize proteins and also control the kinetics of release of proteins over a period of several weeks to several months under physiological conditions.

Abstract: The invention provides proteinoid microsphere made up of a mixture of thermally condensed amino acids that are crosslinked with a bis dithiol crosslinker reagent. The proteinoid microspheres of the invention may be used to encapsulate a material or a compound and to provide slow, sustained or timed release of the material or compound. The proteinoid microspheres are stable in solution until exposed to a reducing agent. However, the in vivo environment provides a sufficient reduction potential to provide slow, sustained release of materials contained therein from the proteinoid microspheres of the present invention.

Abstract: Novel burst-free, sustained release biocompatible and biodegrable microcapsules which can be programmed to release their active core for variable durations ranging from 1–100 days in an aqueous physiological environment. The microcapsules are comprised of a core of polypeptide or other biologically active agent encapsulated in a matrix of poly(lactide/glycolide) copolymer as a blend of uncapped (free carboxyl end group) and end-capped forms ranging in ratios from 100/0 to 1/99.

Abstract: Pharmaceutical compositions useful for treating autoimmune diseases in a mammal comprising as an active ingredient a therapeutically effective amount of Copolymer 1, and microcrystalline cellulose are disclosed. Processes for the manufacture of such compositions are also disclosed.

Abstract: The present invention relates to protein-coated micro-crystals and their method of preparation. The protein-coated micro-crystals may find particular application in preparing enzymes for use as biocatalysts; preparation of therapeutic proteins for use in pharmaceutical formulations; production of cleansing agents comprising enzymes; production of paints, varnishes, coatings, films and the like comprising proteins which impart protective and/or antifouling properties; production of films, polymers, inks, coatings, electrodes and/or optical materials comprising proteins for diagnostic kits and/or biosensor applications; use of proteins for studies of molecular recognition, molecular binding and inhibitor binding in non-aqueous media; and preparation of protein based food additives.

Abstract: The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form drug containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: A particle is disclosed that comprises a first volume of hydrophobe-rich material with tunable dissolution and solubilization characteristics and a distinct second volume of nanostructured nonlamellar liquid crystalline material, said second volume containing said first domain and being capable of being in equilibrium with said first volume. Preferably, the nanostructured nonlamellar liquid crystalline material is capable of being in equilibrium with a polar solvent or a water-immiscible solvent or both.

Abstract: Microencapsulation methods and products are provided. The method includes forming, at a first temperature, a emulsion which comprises aqueous microdroplets, including the agent (e.g., a magnetic material or drug) and a cross-linkable matrix material (e.g., a protein such as albumin), dispersed in a hydrophobic continuous phase comprising an oil and an oil-soluble surfactant, the first temperature being below the temperature effective to initiate cross-linking of the matrix material, and then heating the emulsion to a temperature and for a time effective to cause the matrix material to self-crosslink, to form microparticles comprising the agent encapsulated by the crosslinked matrix material.

Abstract: Once daily pharmaceutical compositions containing lithium carbonate in the form of coated granules.

Abstract: The present invention relates generally to methods and compositions for targeting and delivering solid-phase platelet-dependent vascular occlusion agents. In particular, particles or coils or stents coated with platelet binding agents are directed to target vasculature, such as the vasculature of solid tumor masses or AV-malformations or aneurysms or endoleaks; the solid-phase agent then binds and activates platelets, which in turn bind and activate other platelets. This process results in the rapid formation of a platelet-mediated thrombus about the solid-phase agent causing vessel occlusion.

Abstract: Disclosed is a process for producing sustained-release powders that is fast, efficient, and economical. The process involves melting an animal or vegetable oil with a melting point above 110 degrees F. in specially designed mixer through either the work energy input of the mixer shaft itself, or a specially fitted plow type mixer equipped with a heating tank, cooling unit, jacket for hot water circulation, and heated lines with nozzles for atomizing the hot oil to be sprayed on. The entire manufacturing process can be completed in about 5-30 minutes, and results in small, sustained-release particles that are free flowing and solid at room temperature. The preferred oil is a hydrogenated soy oil with a melting point range of 145-160 degrees F. which is applied at about a 5% level by weight in a high shear mixer. Also included are sustained-release compositions for therapeutic agents such as drugs, botanicals, biological agents, fungicides, and fertilizers.

Abstract: The present invention is directed to a coating composition for coating a solid dosage form of a medicament, where the coating composition controls the release of the medicament, said coating composition comprising (a) at least 50% (w/w) by dry weight of a water insoluble polymer insoluble in both acidic, basic and neutral pH, present in the form of an aqueous latex dispersion, (b) a water soluble non-polymeric component present in a weight ratio of about 5 to about 50% (w/w) by dry weight of the coating, having a molecular weight of less than about 15,000 daltons and water solubility in excess of 5 grams per 100 grams of water at room temperature at 1 atm pressure, said water soluble non-polymeric component being organic and either solid or liquid; said ratio of water insoluble polymer to water soluble non-polymeric component ranging from about 95:5 to about 1:1, the solid content in the coating composition ranges from about 5% to about 25%, said water soluble component being completely dissolved in the aqueo

Abstract: A microbubble preparation formed of a plurality of microbubbles comprising a first gas and second gas surrounded by a membrane such as a surfactant, wherein the first gas and the second gas are present in a molar ration of from about 1:100 to abut 1000:1, and wherein the first gas has a vapor pressure of at least about (760?X) mm Hg at 37° C., where x is the vapor pressure of the second gas at 37° C., and wherein the vapor pressure of each of the first and second gases is greater than about 75 mm Hg at 37° C.; also disclosed are methods for preparing microbubble compositions, including compositions that rapidly shrink from a first average diameter to a second average diameter less than about 75% of the first average diameter and are stabilized at the second average diameter; methods and kits for preparing microbubbles; and methods for using such microbubbles as contrast agents.

Abstract: Zeaxanthin (ZX) or other medically or commercially important carotenoids can be prepared in microcrystalline form, in an oily carrier liquid, to increase their bioavailability following oral ingestion. Initial processing is carried out to prepare a “rough” or “coarse-grained” carotenoid preparation containing relatively large particles of the ZX or other carotenoid, in a suitable form such as a lyophilized stable powder. The coarse-grain preparation is dissolved in a suitable solvent such as tetrahydrofuran, and mixed with a carrier liquid comprising a digestible oil (such as a vegetable oil) and an emulsifying agent. The resulting oil-and-solvent mixture is injected, along with inert gas such as nitrogen, into a vacuum chamber, where a suitable vacuum and temperature combination is used to remove the solvent in a rapid “flash” manner which does not give the carotenoid crystals time to grow larger through accretion or aggregation.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety.

Abstract: Methods and compositions are provided for the encapsulation of antigens in PLGA microspheres for use as vaccines. Such microspheres can also contain adjuvants. Mixtures of microspheres are provided which release antigen at desired intervals to provide boosts with antigen.

Abstract: Disclosed is a method of stimulating bone growth at a site in a subject in need of osteoinduction. The method comprises the step of administering a therapeutically effective amount of an agonist of the non-proteolytically activated thrombin receptor to the site.

Abstract: Disclosed is a method of stimulating bone growth at a site in a subject in need of osteoinduction. The method comprises the step of administering a therapeutically effective amount of an agonist of the non-proteolytically activated thrombin receptor to the site.

Abstract: A method is provided for in vivo or ex vivo delivery of a preparation of powdered nucleic acid molecules into vertebrate tissue for transformation of cells in the tissue using needleless injection techniques. The method can be used to deliver therapeutically relevant nucleotide sequences to cells in mammalian tissue to provide gene therapy, elicit immunity or to provide antisense or ribozyme functions. A method for providing densified processed pharmaceutical compositions is also described. The method is used to convert non-dense pharmaceutical powders or particulate formulations into densified particles optimally suited for transdermal delivery using a needleless syringe. The method is also used to optimize the density and particle size of powders and particulate formulations for subsequent transdermal delivery thereof. Densified pharmaceutical compositions formed by the present methods are also provided.

Abstract: The present invention teaches an improved process for preparing a population of microcapsules having a substantially uniform size distribution, especially useful for manufacture of carbonless paper. The improved process teaches use of membrane material having a pre-selected pore size in the capsule manufacture process. A core material is provided along with a receiving solution for receiving the core material. The receiving solution is a nonsolvent for the core material. The core material is passed under pressure through the membrane into a moving or turbulent receiving solution forming uniform droplets of core material dispersed in the receiving solution. Wall-forming material is added to the receiving solution for coating the core material droplets. The coating on the droplets is polymerized forming microcapsules. This novel process also lends itself to microcapsule formation in a continuous process.

Abstract: The present invention relates to an improved controlled release system that can encapsulate different flavors, sensory markers, and active ingredients, or combinations of flavors, sensory markers and various active ingredients and release multiple active ingredients in a consecutive manner, one after the other. The controlled delivery system of the present invention is substantially free-flowing powder formed of solid hydrophobic nanospheres that are encapsulated in a moisture sensitive microspheres. The flavors, and active ingredients encapsulated in the hydrophobic nanospheres, in the water sensitive microsphere, or in both the nano and the microsphere. The flavors and active ingredients encapsulated in the nanospheres can be the same or different from those encapsulated in the microspheres.