Abstract: An edible dry-powder formulation of a film coating for pharmaceuticals and confectioneries using gum acacia as a low-cost film former is provided. A cellulosic polymer such as hydroxypropyl methylcellulose is used in addition to the gum acacia. A plasticizer such as propylene glycol is also added. The resulting formulation is a dry, free flowing powder that can be put into solution and applied to a tablet or other substrate without an extended waiting period. The resulting film coating is clear, shiny, durable and extremely economical. Because the formulation is a dry powder, it has along shelf life and low shipping costs.

Abstract: A hematopoietic growth factor delivery composition includes a hematopoietic growth factor, a liquid vehicle, a first biocompatible polymer and a second biocompatible polymer. The composition exhibits reverse-thermal viscosity behavior, due to interaction between the first biocompatible polymer and the liquid vehicle. The second biocompatible polymer helps to protect the first biocompatible polymer from being dissolved in vivo following administration to a host.

Abstract: The present invention relates to a process for preparing silica microcapsules and more particularly, to a process for preparing silica microcapsules comprising the steps of dissolving tetraethyl orthosilicate (TEOS) into an aqueous solution containing a hydrolysis catalyst to control a degree of hydrolysis and contribute hydrophilicity or lipophilicity, adding a core material and an appropriate amount of aminopropyltrialkoxysilane(APS) as a gelling agent into the solution, and emulsifying and dispersing the resulting solution to a solution having a polarity opposite to that of the core material to microcapsulate by coating the core material with silica shell via a sol-gel reaction. The process for preparing microcapsules of the present invention reduces environmental pollution compared to conventional processes using an alkali gelling agent such as an ammonia solution, and are suitable for both organic or inorganic core materials having hydrophilic or lipophilic property.

Abstract: The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse of dispose of. In one aspect, the present invention provides endosomolytic agents capable of effecting the lysis of an endosome in response to a change in pH, and methods for effecting the lysis of an endosome. These inventive endosomolytic agents obviate the need for known agents (i.e., chloroquine, fusogenic peptides, inactivated adenoviruses and polyethyleneimine) that can burst endosomes and have negative effects on cells.

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, which may contain a pharmaceutically-acceptable adjuvant, as a blend of upcapped free carboxyl end group, and end-capped forms ranging in ratios from 100/0 to 1/99.

Abstract: The present invention relates to the use of calcium phosphate particles in formulation with allergens for allergic desensitization. Particularly, the invention relates to novel calcium phosphate core particles, particularly nano- and micron-sized particles, as allergen adjuvants and in compositions for inducing allergic desensitization. Methods of making such particles and to methods of inducing a specific immune response using the particles of this invention are also provided.

Abstract: A microparticle contains a cross-linked protein shell, and a surface coating.

Abstract: Provided are a composition for preparing a lyophilized preparation, comprising a drug-encapsulating polymer micelle and saccharides and/or polyethylene glycol as a stabilizing agent, a lyophilized preparation and a process for producing them. The lyophilized preparation thus provided is easily restructured to an aqueous preparation using an aqueous medium.

Abstract: The present invention provides fibrin microbeads that are biologically active and comprise extensively cross-linked fibrin(ogen), and a method for preparing the fibrin microbeads. The present invention also provides a composition comprising cells bound to the fibrin microbeads, and methods for culturing and separating cells using the fibrin microbeads of the present invention. Finally, the present invention provides methods for transplanting cells and engineering tissue using the fibrin microbeads of the present invention.

Abstract: Compositions are provided which include hyaluronic acid derivatives in combination with vaccine antigens, and optionally adjuvants, for mucosal delivery. Also provided are methods of making the compositions, as well as methods of immunization using the same.

Abstract: An inorganic particle, to which is bonded a cell binding component and a nucleic acid, is provided for delivery of a nucleic acid to a cell. The disclosed particle acts as a synthetic vector for achieving efficient transfection of associated nucleic acid into a cell.

Abstract: Optically-activated particles for use in cosmetic preparations. The optically-activated particles include a plurality of substrate particles selected from the group consisting of nylons, acrylics, polyesters, other plastic polymers, natural materials, regenerated cellulose, metals and minerals; an optical brightener chemically bonded to each of the plurality of substrate particles to form integral units in the form of optically-activated particles for diffusing light to reduce the visual perception of skin imperfections, including cellulite, shadows, skin discolorations, and wrinkles; and each of the optically-activated particles are encapsulated with a UV transparent coating to increase the diffusion light to further reduce the visual perception of the skin imperfections.

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: Microparticles of a water-soluble material, which are smooth and spherical, and at least 90% of which have a mass median particle size of 1 to 10 &mgr;m, and which carry a therapeutic or diagnostic agent can successfully be used in dry powder inhalers to deliver the said agent.

Abstract: EEM-S obtained by extracting with hot water or a lower alcohol at least one mushroom selected from among Lentinus edodes, Flammulina velutipes, Hypsizygus marmoreus, Pleurotus ostreatus, Pholiota nameko, Grifola fondosa, Volvariella speciosa ver. speciosa, Lyophllum decastes, blanc du pays, Tricholoma matsutake, Ganoderma lucidum and Phellinus yucatensis, treating the obtained extract by the molecular sieve method and thus eliminating low-molecular-weight and high-molecular-weight fractions: and preparations thereof. This EEM-S exerts physiological effects such as anticancer, immunopotentiating, antioxidative, hypotensive and hypoglycemic effects.

Abstract: A method is described for the formation of microcapsules which contain a liquid composition in the core, which is surrounded by a polymeric shell, membrane, or coating. The microcapsules are produced by simultaneously extruding the liquid core material along with a polymerizable liquid through concentrically-aligned nozzles to form spherically-layered biliquid droplets, followed by energy input in the form of heat or light which causes polymerization of the outer layer. The capsules formed by this method are capable of containing a variety of liquid materials having a composition ranging from completely aqueous to completely non-aqueous.

Abstract: The present invention relates to a process for the preparation of microparticles, with an extremely high encapsulation rate, comprising a water-soluble substance in a biodegradable polymer, said water-soluble substance and said biodegradable polymer being first incorporated in an organic liquid phase comprising at least one organic non-water miscible solvent. The organic phase is poured into an aqueous liquid phase having a volume which is sufficient to dissolve said organic solvent, said aqueous phase containing a surfactant, the resulting organic-aqueous phase being homogenised in order to perform in one single step the microparticle formation and the organic solvent removal. The thus obtained microparticles show surprisingly good agent retention qualities.

Abstract: The invention relates to particulate active ingredient vehicles which are in the solid aggregate state at room temperature (20° C.) and consist of a pure lipid-drug conjugate (LDC) or a mixture of several LDCs as particle matrix, the bond in the LDC being effected by covalent bonding, electrostatic interactions, dipole moments, dispersion forces, ion interactions, hydrogen bridges and/or hydrophobic interactions.

Abstract: The invention concerns a device for producing granules, in particular pharmaceutical granules, comprising a drum (4) with peripheral apertures (25) and a member (30) feeding the drum with coating or fixing substance. The drum (4) comprises mutually parallel sections (22) defining between them the apertures (25).

Abstract: The present invention relates to a controlled drug release system in which a certain ratio or retinoic acid is incorporated into a microsphere comprising biodegradable polymer and amphoteric block copolymer having both hydrophilic and hydrophobic groups.

Abstract: The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.

Abstract: In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful election of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered.

Abstract: A microbiological culture for triggering microbiological processes in bodies of water, soils, sediments, and/or muds contains chemo-lithoautotrophic bacteria that are immobilized. The bacteria are immobilized in a matrix having the form of capsules, gels, or gel spheres. The matrix material is selected from a wide range of natural and synthetic polymers.

Abstract: Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear a-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, porous particles having a relatively large mean diameter, for example greater than 5 &mgr;m, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung.

Abstract: It comprises a compound having antifungal activity as active principle, an inert core and a coating including said active principle, and is characterized in that said inert core has a particle size comprised between 50 and 600 &mgr;m, and in that said coating comprises a single layer obtained by spraying, on said inert core, a solution comprising a compound having antifungal activity, a hydrophilic polymer and a non-ionic surfactant. The method consists in carrying out a coating, comprising a single layer, of the inert cores having a size between 50 and 600 &mgr;m, by means of the spraying of a solution composed by the antifungal agent, the hydrophilic polymer and the non-ionic surfactant, at a constant coating speed throughout the whole process; and a single drying step of said coating in the same apparatus.

Abstract: Methods of treatment of benign prostatic hyperplasia and reduction of the level of the prostate specific antigen (PSA) of benign prostate conditions are disclosed. The treatment method includes an initial treatment of patients with orally administration of an initial dosage of about 40 mg 13 cis-retinoic acid daily for a period from about ten days to about twenty days, and followed by a sustaining treatment of the patients with orally administration of a sustaining dosage of about 40 mg 13 cis-retinoic acid about every five to seven days in a sustaining period.

Abstract: A microcapsule having a mean diameter of from about 0.1 to about 5 mm, a membrane and a matrix containing at least one active principle wherein the microcapsule is the product of the process comprising the steps of (a) forming an aqueous matrix by heating an aqueous solution comprised of a gel former, an anionic polymer selected from the group consisting of a salt of alginic acid and an anionic chitosan derivative and active principle; (b) adding the aqueous matrix to an aqueous solution of chitosan.

Abstract: The present invention provides microspheres intended to be administered by injection comprising a protein active ingredient and an agent coating the active ingredient intended to prolong its release, wherein they are free of any trace of organic solvent and they can be obtained according to a coating method involving bringing the active ingredient and the coating agent into contact, with stirring, in a supercritical fluid, said coating agent being soluble in this supercritical fluid.

Abstract: A method and composition for the encapsulation of hydrophilic molecules in submicron particles is disclosed. The particles are composed of a water-in-oil microemulsion surrounded by one or more biocompatible polymers.

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

Abstract: Microparticles of a water-soluble material, which are smooth and spherical, and at least 90% of which have a mass median particle size of 1 to 10 &mgr;m, and which carry a therapeutic or diagnostic agent can successfully be used in dry powder inhalers to deliver the said agent.

Abstract: Compositions and methods are provided for forming tissue-adherent hydrogels using substantially dry precursors. The dehydrated precursors are premixed prior to in situ therapy and utilize naturally-occurring body fluids as an aqueous environment that initiates transformation, which causes dissolution and nearly simultaneous crosslinking of the precursors, thus forming an insoluble hydrogel implant. The dehydrated precursor-based hydrogels may be used as sealants for fluid leaks from tissue, as adherent drug delivery depots, as means for augmenting and/or supporting tissue, and as means for serving a variety of other useful medical and surgical purposes.

Abstract: A method of forming microspheres of a bioactive material, such as a protein polymer or drug by nebulizing a solubilized form of a material to be encapsulated and an encapsulating material, such as albumin, in a stirred chilled solvent system comprising a vegetable oil, mineral oil and/or a lower alcohol such that the formed microspheres demonstrate intracellular bioactivity when taken up by macrophages.

Abstract: An oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof is disclosed. A method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient is also disclosed.

Abstract: The invention concerns a pharmaceutical composition with prolonged release, for oral administration of a single daily dose of 60 to 140 mg of Milnacipran, having a multi-particulate form containing a plurality of microgranules each comprising an active microsphere containing a saccharose and/or starch nucleus of a size between 200 and 2000 &mgr;m and containing 150 to 1000 &mgr;m of Milnacipran and a binding agent, each microgranule being coated with a film having a base of at least one polymer insoluble in water but permeable to physiological liquids, of a thickness between 20 and 100 &mgr;m, the said pharmaceutical composition enabling an in vitro release corresponding to the following pattern: between 10 and 55% of the dose released in 2 hours, between 40 and 75% of the dose released in 4 hours, between 70 and 90% of the dose released in 8 hours, between 80 and 100% of the dose released in 12 hours.

Abstract: Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact, such that the ratio of the amount of antagonist released from said dosage form after tampering to the amount of said antagonist released from said intact dosage form is about 4:1 or greater, based on the in-vitro dissolution at 1 hour of said dosage form in 900 ml of Simulated Gastric Fluid using a USP Type II (paddle) apparatus at 75 rpm at 37 degrees C. wherein said agonist and antagonist are interdispersed and are not isolated from each other in two distinct layers.

Abstract: A method and a process are disclosed for preparation of medical electro-powders. The electro-powder results from preparations of chemical and biological substances to form electro-powders suitable for electrostatic charging and dosing for functionality in a dry powder inhaler device. The electro-powder resulting from the method and process forms an active powder substance or a dry powder medical formulation with a fine particle fraction representing of the order 50% or more of the content having a size ranging between 0.5-5 &mgr;m and provides electrostatic properties with an absolute specific charge per mass after charging of the order 0.1×10−6 to 25×10−6 C/g and presenting a charge decay rate constant Q50>0.1 sec with a tap density of less than 0.8 g/ml and a water activity aw of less than 0.5.

Abstract: Disclosed is a process for producing powders from high viscosity fluids including mixing a mixture comprising a high viscosity fluid and at least one absorbing agent until a dry dispersion is produced; combining, under shear, a combination of the dry dispersion with a naturally derived oil having a melting point at least about 110° F.; and granulating the combination into a powder. Also disclosed are pharmaceutical compositions that include a high viscosity fluid, at least one absorbing agent; and a naturally derived oil with a melting point at least about 110° F., together with sustained-release embodiments of such compositions.

Abstract: The present invention refers to a process for stabilizing LAA in an aqueous medium, which includes the step of contacting the LAA with at least one-compound capable of forming hydrogen bridges with the LAA. In another aspect, the invention relates to a stable aqueous LAA composition which includes, in addition to the ascorbic acid, at least one compound which is linked to the LAA by hydrogen bridges, and to a process for preparing it. The present invention further relates to an emulsion including, in its aqueous phase, at least one compound linked to levogyre ascorbic acid (LAA) by hydrogen bridges. Further according to the present invention a vitamin product is provided, in which a stable LAA composition as described above is contained in organic envelopes which enable a gradual and prolonged release of the LAA into the organism. The vitamin product may further include a compound capable of stimulating the metabolism of the fibroblasts.

Abstract: Pharmaceutical gastroretentive drug delivery systems for the controlled release of an active agent in the gastrointestinal tract are disclosed, which comprise: (a) a single- or multi-layered matrix comprising a polymer that does not retain in the stomach more than a conventional dosage form selected from (1) degradable polymers that may be hydrophilic polymers not instantly soluble in gastric fluids, enteric polymers substantially insoluble at pH less than 5.5 and/or hydrophobic polymers and mixtures thereof; (2) non-degradable polymers; and any mixtures of (1) and (2); (b) a continuous or non-continuous membrane comprising at least one polymer having a substantial mechanical strength; and (c) a drug; wherein the matrix when affixed or attached to the membrane prevents evacuation from the stomach of the delivery system for a period of time of from about 3 to about 24 hours.

Abstract: A method for making a suspension, dispersion or emulsion of non-agglomerated particles comprising forming particles in a liquid medium, wherein sonic energy is applied to the liquid medium at the point of contact of the reactants during the particle forming step to produce the suspension, dispersion or emulsion of non-agglomerated particles. The invention is also directed to a method for making a suspension of non-agglomerated pyrithione salt particles, comprising the steps of forming pyrithione salt particles in a liquid medium, wherein sonic energy is applied to the liquid medium during the forming step to produce the suspension of non-agglomerated pyrithione salt particles.

Abstract: This invention provides reagents and methods for specifically delivering antibiotic, antimicrobial and antiviral compounds, drugs and agents to phagocytic mammalian cells. The invention also relates to specific delivery to and uptake of such compounds by phagocytic cells. The invention specifically relates to reagents and methods for facilitating the entry of antibiotic, antimicrobial and antiviral compounds, drugs and agents into phagocytic cells. The invention specifically provides compositions of matter and pharmaceutical embodiments of such compositions comprising such antibiotic, antimicrobial or antiviral compounds, drugs and agents conjugated to, impregnated with or coated onto particulate carriers generally termed microparticles. In particular embodiments, the antibiotic, antimicrobial and antiviral compounds, drugs and agents are covalently linked to a microparticle via a specifically-degradable linker molecule which is the target of a microorganism-specific protein having enzymatic activity.

Abstract: Microcapsules prepared by encapsulating an aqueous solution of a protein, drug or other bioactive substance inside a semi-permeable membrane by are disclosed. The microcapsules are formed by interfacial coacervation under conditions where the shear forces are limited to 0-100 dynes/cm2 at the interface. By placing the microcapsules in a high osmotic dewatering solution, the protein solution is gradually made saturated and then supersaturated, and the controlled nucleation and crystallization of the protein is achieved. The crystal-filled microcapsules prepared by this method can be conveniently harvested and stored while keeping the encapsulated crystals in essentially pristine condition due to the rugged, protective membrane. Because the membrane components themselves are x-ray transparent, large crystal-containing microcapsules can be individually selected, mounted in x-ray capillary tubes and subjected to high energy x-ray diffraction studies to determine the 3-D structure of the protein molecules.

Abstract: Polysaccharide-based shells are provided having use for forming water-dispersible microcapsular delivery systems for both hydrophilic and lipophilic drugs, pharmaceuticals, cosmetics and other active agents. These shells are prepared by intimately blending a solubilized polysaccharide with a lipophilic material to produce spherical droplets of the lipophilic material coated with the polysaccharide, diluting the emulsion with a solvent, and isolating the polysaccharide shells from the diluted emulsion.

Abstract: Block copolymers based on poly(ortho esters) containing amine groups. These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: There is provided a coating composition that masks the undesirable taste of a pharmaceutically active ingredient, i.e. drug or medicine, that is taken orally. The coating composition is comprised of dimethylaminoethyl methacrylate and neutral methacrylic acid ester, a cellulose ester polymer, and an alkaline modifier.

Abstract: Microcapsules having a carotenoid content of between about 10% and 50% by weight. A crystalline form of one or more carotenoids is processed in a fluidized bed coating machine where a protective coating of a sugar or polyhydric alcohol, a starch, and optionally a protein, is applied. The carotenoid content of the finished microcapsules is in excess of 80% of the carotenoids present in the starting material.

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: Disclosed herein is an aqueous suspension of insecticidally active compounds comprising a solid active compound applied as a coating to an inorganic carrier and auxiliaries, water and glycerol.