Abstract: This invention relates to micro-encapsulated particles of solid matter and a quasi-continuous method for producing the same, especially those having water-insoluble characteristics or a hydrophobic form, taking into careful consideration ecologically and economically favorable ways of recycling the media used, and the resulting smallest possible amount of waste products such as waste water and polymer residues, while simultaneously ensuring that even exposed parts of the solid bodies are coated, such as crystal tips and grooves, which are insufficiently coated using standard methods due to the hydrodynamic conditions on these areas.

Abstract: A new method of producing liposomes is described using an in-line mixing system. The liposomes produced by this method find utility in numerous therapeutic applications.

Abstract: The present invention relates to microspheres, processes for the manufacture of said microspheres, pharmaceutical compositions comprising said microspheres, and sustained release methods of administering an effective pharmaceutical amount of a bioactive compound to a subject. The microspheres of the present invention comprise a water insoluble organic matrix comprising an interior region, throughout which are homogeneously dispersed a plurality of microcapsules consisting essentially of a core of bioactive compound coated with material containing charged organic groups and a surface region substantially free of said bioactive compound.

Abstract: This invention relates to proliposomal drug-delivery systems for medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and a coating material. The present invention provides enhanced stability and bioavailability for pharmaceutical formulations.

Abstract: The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water-insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.

Abstract: The present invention provides biocompatible vesicles comprising semi-permeable, thin-walled encapsulating membranes which are formed in an aqueous solution, and which comprise one or more synthetic super-amphiphilic molecules. When at least one super-amphiphile molecule is a block copolymer, the resulting synthetic vesicle is termed a “polymersome.” The synthetic, reactive nature of the amphiphilic composition enables extensive, covalent cross-linking of the membrane, while maintaining semi-permeability. Cross-linking of the polymer building-block components provides mechanical control and long-term stability to the vesicle, thereby also providing a means of controlling the encapsulation or release of materials from the vesicle by modifying the composition of the membrane. Thus, the encapsulating membranes of the present invention are particularly suited for the reliable, durable and controlled transport, delivery and storage of materials.

Abstract: The present invention is an encapsulated yeast composite comprising a core comprising yeast and a coating containing an emulsifiable lipid. The yeast includes Saccharomyces cerevisiae. The invention also relates to other encapsulated bioactive substance composites. The nature of the coating provides controlled release of the bioactive substance from the encapsulate. The encapsulated composites are useful in the production of food compositions, food products, and animal feed products.

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: Microencapslated particles having improved resistance to moisture and extended release capabilities are produced by microencapsulating the particles in a film-forming, cross-linked, hydrolyzed polymer.

Abstract: An improved process for the preparation of microcapsules consist sentially of a wall material and a core material in condensing a melamine-formaldehyde precondensate and/or methyl ethers thereof in an aqueous dispersion of a water-insoluble core material and in the presence of an acrylic acid/acrylamide copolymer at acidic pH and at a temperature in the range of from 20° to 100° C., and hardening thereafter the melamine-formaldehyde precondensate to form the walls of the microcapsules at an elevated temperature, wherein the core material is dispersed in the precondensate/copolymer solution without initial partial condensation of the precondensate and copolymer and wherein the hydrophobe point of the precondensate and/or its methyl esters is less than 90° C., as well as microcapsules, paper and pressure-sensitive recording material comprising such microcapsules.

Abstract: A process for encapsulation of polar organic solvents with amphiphilic copolymer shell using controlled/living polymerization is provided for the first time. To encapsulate polar core-oils an amphiphilic polymer is required that has low interfacial tensions with both the oil phase and the water phase. For example, Poly(methyl methacrylate-co-poly(ethylene glycol) methacrylate) (PMMA-co-PegMA) was prepared in suspension polymerization conditions using atom transfer radical polymerization (ATRP). ATRP ensures that the water soluble comonomer, PegMA, is incorporated into every polymer chain throughout the polymerization reaction so that all chains possess the desired amphiphilic character. Crosslinking of PMMA-co-PegMA with diethylene glycol dimethacrylate (DegDMA) yielded hollow capsular particles at 31 mol % PegMA in the terpolymer.

Abstract: The invention involves methods and products related to the micronization of hydrophobic drugs. A method of micronizing hydrophobic drugs using a set of solutions including an aqueous solution is provided. The invention also relates to products of micronized hydrophobic drugs and related methods of use.

Abstract: A method for administering a radiosensitizer to a tumor site in a subject is described. The method includes preparing liposomes composed of a vesicle-forming lipid and a lipid-derivatized radiosensitizer. In one embodiment, the radiosensitizer is dipalmitoyl-5-iodo-2′-deoxyuridine. A method for preparing the liposome composition including the lipid-derivatized radiosensitizer is also disclosed.

Abstract: Plasmid-lipid particles which are useful for transfection of cells in vitro or in vivo are described. The particles can be formed using either detergent dialysis methods or methods which utilize organic solvents. The particles are typically 65-85 nm, fully encapsulate the plasmid and are serum-stable.

Abstract: A particle coated with a nonlamellar material such as a nonlamellar crystalline material, a nonlamellar amorphous material, or a nonlamellar semi-crystalline material includes an internal matrix core having at least one a nanostructured liquid phase, or at least on nanostructured liquid crystalline phase or a combination of the two is used for the delivery of active agents such as pharmaceuticals, nutrients, pesticides, etc.

Abstract: A microcapsule encapsulating a disperse system is produced by preparing a liquid organic dispersion containing a resin whose acid group has been neutralized, a colored particle, and an organic solvent; dispersing the liquid organic dispersion in an aqueous medium to produce a capsule particle in the aqueous medium, the capsule particle comprising a disperse system in which the colored particle is dispersed in the organic solvent, and a wall encapsulating the disperse system; and separating the capsule particle from the aqueous medium for dryness. The liquid organic dispersion may comprise, as an organic solvent, a hydrophobic organic solvent and a polar solvent dissolving the resin constituting the wall and being miscible to the aqueous medium. The wall of the capsule particle may be crosslinked or cured with a crosslinking agent. The microcapsule is utilized for an image display device in which the colored particle is electrophoretically movable in the oil phase by a potential difference.

Abstract: Reactive polymeric surfactants are disclosed, and their use in processes for preparation of microcapsules, and in stabilising emulsions. The surfactants are random graft polymers or block copolymers which contain both hydrophobic and hydrophilic units and in which the hydrophobic unit includes a hydrophilic cross-linking unit which reacts with (a) a wall forming ingredient in a microencapsulation process, or (b) an ingredient in the disperse phase of an emulsion.

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: Highly efficient cationic liposomes have been developed as an improved delivery system for biologically-active reagents. A novel structure, the sandwich liposome, is formed and comprises one or more biologically active agents internalized between two bilomellar liposomes. This structure protects the incoming agent and accounts for the high efficiency of in vivo delivery and for the broad tissue distribution of the sandwich liposome complexes. These novel liposomes are also highly efficient carriers of nucleic acids. By using extruded DOTAP:cholesterol liposomes to form complexes with DNA encoding specific proteins, expression has been improved dramatically. Highest expression was achieved in the lung, while increased expression was detected in several organs and tissues.

Abstract: Inorganic-organic hybrid mixture sol-gel encapsulated lipid vesicles which are composed of silyl lipids or a mixture of silyl lipids and phospholipids are provided. The present invention also provides encapsulated Langmuir Blogget (LB) membranes and biological macromolecules. The sol-gel encapsulated lipid vesicles, LB membranes and proteins possess a higher stability than conventional vesicles. Inorganic-organic hybrid mixture sol-gels are provided as novel sol-gel materials possessing desirable mechanical and physicochemical properties. Also provided are methods of preparing encapsulated lipid vesicles, LB membranes and proteins. Methods of performing renal dialysis using compositions of the invention are also provided.

Abstract: A method for generating a plurality of drug-containing microcapsules employs one or more atomizers to form the microcapsules by the phenomenon of solvent exchange. A plurality of microdroplets of an aqueous solution is contacted with a plurality of microdroplets containing a polymer dissolved in a hydrophilic solvent under conditions whereby the polymer solution envelops the aqueous microdroplet. Exchange of solvent molecules between the aqueous core and its polymer-containing shell deposits the polymer as a membrane around the aqueous core. A preferred atomizer is a coaxial ultrasonic atomizer. Microcapsules can be generated in air as well as when submersed in a collection bath. Desired properties of the microcapsules, e.g., controlled release, can be achieved by providing protective excipients within the aqueous core, providing a hydrophilic polymer capable of undergoing a sol-to-gel transition within the aqueous core, optimizing selection of the polymer solvent, adjusting relative flow rates, and the like.

Abstract: A stable proteoliposome containing an integral membrane protein in a lipid membrane around an elliptoid or spherical shape. The shape preferably contains an attractant such as streptavidin or avidin and the lipid membrane contains a moiety that binds to the attractant such as biotin. The integral membrane protein is bound to a ligand which is anchored in the shape. Methods for making the proteoliposomes are provided. Kits for making the proteoliposome are described, as are the uses of the proteoliposome.

Abstract: Microencapsulated particles having improved resistance to moisture and extended release capabilities are produced by microencapsulating the particles in a film-forming, cross-linked, hydrolyzed polymer.

Abstract: The invention involves methods and products related to the micronization of hydrophobic drugs. A method of micronizing hydrophobic drugs using a set of solutions including an aqueous solution is provided. The invention also relates to products of micronized hydrophobic drugs and related methods of use.

Abstract: Liposomal encapsulated camptothecin formulations are provided. The liposomes have improved pharmacokinetics, enhanced efficacy as anti-tumor agents and provide an increased therapeutic index as compared to the free drug and topotecan. The formulations include liposomes comprising at least one phospholipid and a camptothecin or analog thereof.

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: An electrophoretic display comprises a fluid and a plurality of nanoparticles having diameters substantially less the wavelengths of visible light such that, when the nanoparticles are in a dispersed state and uniformly dispersed throughout the fluid, the fluid presents a first optical characteristic, but when the nanoparticles are in an aggregated state in which they are gathered into aggregates substantially larger than the individual nanoparticles, the fluid presents a second optical characteristic different from the first optical characteristic. The electrophoretic display further comprises at least one electrode arranged to apply an electric field to the nanoparticle-containing fluid and thereby move the nanoparticles between their dispersed and aggregated states. Various compound particles comprising multiple nanoparticles, alone or in combination with larger objects, and processes for the preparation of such compound particles, are also described.

Abstract: Described is a process for preparing a dispersion of microcapsules by condensing a partially methylated melamine-formaldehyde resin having a molar ratio of melamine:formaldehyde:methanol of from 1:3.0:2.0 to 1:6.0:4.0 in water in which the essentially water-insoluble material forming the capsule core is present in dispersion in the presence of an alkali metal salt of a homopolymer or copolymer of 2-acrylamido-2-methylpropanesulfonic acid as protective colloid at a pH of from 3 to 6.5 by preforming the microcapsules at a temperature of from 20 to 50° C. and then curing the capsule wall of the preformed microcapsules at >50 to 100° C., which comprises adding from 5 to 100% by weight of melamine, based on the melamine-formaldehyde resin, in the course of curing. The microcapsule dispersions are formaldehyde-reduced and of low viscosity.

Abstract: A manufacturing method for oral quick-dissolving capsules, includes the steps of: preparing a core liquid that contains a filler material; preparing a shell liquid by having dissolved therein a shell material that includes one or more plasticizer and a shell forming agent; supplying to a multiple nozzle having an inner nozzle and an outer nozzle, and forming multilayer liquid drops by extruding the multilayer liquid drops from the multiple nozzle; hardening the shell liquid by bringing the multilayer liquid drops into contact with a hardening liquid; separating the seamless capsules from the hardening liquid; and drying their surface to form seamless capsules. The seamless capsules have a particle diameter of 1 to 10 mm, a mass ratio of shell material to filler material of 5:95 to 70:30, and the amount of added plasticizer is 20 to 70% by mass with respect to the total amount of the shell material, excluding water.

Abstract: Microcapsules or particles of a matrix are formed by interfacial reaction between reactants that can form a membrane, one of the reactants comprising anhydride moieties. These can be used to encapsulate materials, particularly materials for controlled release. Examples include pheromones that are slowly released during the breeding season of insects to control the insect population.

Abstract: A process for producing parenterally administrable microparticles, in which an at least 20% by weight aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are made to gel, and the gelled starch particles are dried. A release-controlling shell is optionally also applied to the particles. Microparticles which essentially consist of said starch, have an amino acid content of less than 50 &mgr;g and have no covalent chemical cross-linking.

Abstract: Liposomal bupivacaine compositions are prepared using an ammonium sulfate gradient loading procedure, at a pH which prevents precipitation of the drug from the loading solution. Also described are liposome suspensions comprising ‘GMV’ (giant multivesicular) liposomes and methods for their preparation. The liposomal compositions are characterized by high drug-to-lipid ratios and provide long term analgesia.

Abstract: The invention relates to a process for preparing microcapsules by coacervation, wherein the cross-linking of a protein is carried out by a plant extract rich in substituted or unsubstituted phenolic compounds.

Abstract: Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to the free drug. The formulations include liposomes comprising at least one phosphatidylcholine, a cholesterol, and a benzoquinazoline thymidylate synthase inhibitor.

Abstract: The invention relates to a method and facility for industrial scale production of micromembrane capsules for immobilizing active ingredients, proteins, live cells and/or microorganisms. According to the invention, the material dissolved in a base material or in suspended form that is to be encapsulated is fed from a reservoir into a reactor, wherein drops are produced from said material and balls are formed by precipitating said drops. The balls enclose the material and are then in turn coated by repeated rinsing in the same and/or different vessel.

Abstract: The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water-insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.

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: The invention concerns liposome vectors, in powder form, of active principles, and more particularly active principles sensitive to digestive and/or plasmatic degradation, such as proteins, and their application as medicine. Said liposome vectors of active principles consist of a powder composition essentially constituted of unilamellar liposomes comprising an external lipid phase consisting of class 4 lipids (phospholipids), optionally associated with class 2 substances, class 3 substances and/or class 5 substances and an internal aqueous nucleus consisting of a mixture M of at least two different non-polymerisable gelling agents (G1 and G2) whereof the gel-sol phase transition is not less than 37° C.

Abstract: Compositions for sustained delivery of a biomolecule including an anionic polymer and a cationic polymer which ironically interact with each other and, optionally, with the biomolecule. Methods for making the compositions, including the step of combining the negatively charged polymer with the positively charged polymer to form an ionic complex are also provided. The biomolecule may be complexed with one of the polymers before it is complexed with the oppositely charged polymer. The complex is exposed to conditions that cause the formation of precipitated microcarriers, such as a change in pH or the addition of a complexing molecule. The compositions are preferably formulated into microcarriers.

Abstract: An apparatus for forming composite pellets containing active ingredients encapsulated in encapsulating material for the controlled release of the active ingredient in the treatment of humans, animals or plants that is capable of the following steps: producing solid granules containing encapsulating material and active ingredient; generating a flow of granules; heating the granules in flight so as to melt a portion of encapsulating material located at the surface of each granule, of melted encapsulating material spreading on the surface of each granule to form a substantially uniform surface layer so as to confer on the granules the form of pellets; cooling the pellets in flight so as to solidify at least the surface layer; collecting the pellets.

Abstract: What is disclosed is a process for making small thermoplastic polymer particles comprising the steps of:

Abstract: A method of sizing liposomes by passing a suspension of liposomes through an aluminum oxide porous film by entering the film via the smaller pores and extruded via the larger pores, under pressure, is disclosed. In a preferred embodiment, the porous film is a branched-pore type anodic aluminum oxide porous film. The process produces a population of liposomes substantially free of liposomes above a predetermined maximum size. Also disclosed is an apparatus for carrying out the invention.

Abstract: A process for producing microparticles containing biologically active substance, in which process an aqueous solution of the said substance is prepared, this solution is mixed with an aqueous solution of PEG such that the substance is concentrated and/or solidified, the substance is optionally washed, the substance is mixed with an organic polymer solution, the composition obtained is mixed, after the admixture of said polymer solution, with an aqueous polymer solution, thereby forming an emulsion of droplets of first mentioned polymer as the internal phase, said droplets are solidified into microparticles, the microparticles are dried and a release-controlling shell is optionally applied to these.

Abstract: Production of purified, parenterally administrable starch by washing starch containing more than 85% amylopectin in order to remove surface-localized proteins, lipids and endotoxins, subjecting the starch to a molecular weight reduction by acid hydrolysis, and optionally removing residual water-soluble proteins. Purified starch and microparticles based on such starch.

Abstract: The invention relates to a liposomal formulation that is capable of fusing with cells. The liposomal formulation may contain an agent for delivery to cells. The invention also provides compositions and methods for making the liposomal formulation and for liposomal drug delivery. These include methods of killing microbes and of treatment and prevention of microbial infections through the administration of such a formulation.

Abstract: The present invention provides a method for preparing submicron sized particles of an organic compound, the solubility of which is greater in a water-miscible first solvent than in a second solvent which is aqueous, the process including the steps of (i) dissolving the organic compound in the water-miscible first solvent to form a solution, (ii) mixing the solution with the second solvent to define a pre-suspension; and (iii) adding energy to the pre-suspension to form particles having an average effective particle size of 400 nm to 2 microns.

Abstract: The invention provides a composition for delivering at least one biologically active compound to a living organism, said composition comprising at least one micelle-forming membrane lipid

Abstract: A solvent exchange method is employed to provide microencapsulated compositions, such as microcapsules of pharmaceutical preparations. The method is based on an exchange of water and a hydrophilic organic solvent, whereby a decline in solvent quality for the organic solvent causes a polymer dissolved therein to be deposited onto an aqueous core. Optimal results are rationalized in terms of a balance of water solubility and surface tension for the organic solvent. In a preferred embodiment, microcapsules of selected drugs are formed by contacting microdroplets of an aqueous solution containing the drug with the organic solvent containing a polymer dissolved therein. A preferred method employs biodegradable poly(lactic acid-co-glycolic acid) (PLGA) dissolved in acetic acid, ethyl acetate, methyl acetate, or ethyl formate, to form a PLGA membrane around an aqueous drug core. The method is particularly attractive for encapsulating protein-based drugs without substantial denaturation.

Abstract: A process for producing liposomes having a desired mean particle size wherein the desired mean particle size is obtained by varying the initial organic solvent concentration.

Abstract: A process of micro-encapsulating a volatile liquid includes selecting a volatile liquid, such as Isophorone, and porous ceramic particles for encapsulating the volatile liquid. The volatile liquid and porous particles are mixed and a vacuum is applied to the mixture to impregnate the volatile liquid in the porous particles. A polymer catalyst for the polymer resin, such as an epoxy catalyst for use with an epoxy resin, is mixed with the volatile liquid and porous particles to saturate the particles. The polymer resin, such as epoxy resin, is added to the mixture for forming a resin cured shell around the porous particle holding the volatile liquid to form a microencapsulated volatile liquid. The resin is only cured on the outer shell of the porous particle when coming in contact with the catalyst supported with the volatile liquid in the porous particle.