Abstract: The present invention provides novel calcium phosphate nanoparticles suitable for efficient encapsulation of biologically active molecules. The invention further provides pharmaceutical compositions comprising these nanoparticles, as well as methods of making such nanoparticles and using them as carriers for therapeutic delivery of biologically active macromolecules.

Abstract: A method for producing a composite nanoparticle, including the steps of, collapsing at least a portion of a polyelectrolyte polymer in solution about one or more precursor moieties to form a composite precursor moiety having a mean diameter in the range between about 1 nm and about 100 nm, wherein the polyelectrolyte polymer has an extended conformation in a first solution state and a more compact conformation in a second solution state; and cross-linking the polyelectrolyte polymer of the composite precursor moiety to form a composite nanoparticle wherein the precursory moiety is a charged organic ion.

Abstract: A formulation for an inhaler device comprises carrier particles having a diameter of at least 50 ?m and a mass median diameter of at least 175 ?m; active particles; and additive material to which is able to promote release of the active particles from the carrier particles on actuation of the inhaler device. The formulation has excellent flowability even at relatively high fine particle contents.

Abstract: The invention provides a formulation of water insoluble or poorly water soluble drugs encapsulated in lipidated glycosaminoglycan particles for targeted drug delivery.

Abstract: Polymeric nanoparticles, microparticles, and gels for delivering cargo, e.g., a therapeutic agent, such as a peptide, to a target, e.g., a cell, and their use for treating diseases, including angiogenesis-dependent diseases, such as age-related macular degeneration and cancer, are disclosed. Methods for formulating, stabilizing, and administering single peptides or combinations of peptides via polymeric particle and gel delivery systems also are disclosed.

Abstract: The invention relates to a process for the preparation of anhydrous lactose agglomerates, said process comprising (i) subjecting essentially anhydrous lactose primary particles comprising at least 60 wt % crystalline-lactose in a granulator to a wet granulation step at a temperature in the range of 30-100° C. using a binder solution, wherein the granulation mass is subjected to drying for at least part of the granulation step, and (ii) after-drying the granulation mass. The anhydrous lactose agglomerates thus produced comprise at least 50 wt %-lactose crystallites and have a total water content in the range of 0-1.0 wt %, which is required according to the standards laid down by the Pharmacopoeia for anhydrous lactose excipients. These agglomerates combine have excellent compactibility and flowability properties and are particularly useful as excipient in moisture-sensitive applications.

Abstract: A water-dispersible particle for delivery of nitrogen to a plant is disclosed. The water-dispersible particle also delivers an active ingredient such as a plant hormone to a desirable plant or a pesticide or herbicide to an undesirable organism. Methods for making and using the water-dispersible particle are described.

Abstract: A process for preparing ultrafine powders of biological macromolecules comprises atomizing liquid solutions of the macromolecules, drying the droplets formed in the atomization step, and collecting the particles which result from drying. By properly controlling each of the atomization, drying, and collection steps, ultrafine dry powder compositions having characteristics particularly suitable for pulmonary delivery for therapeutic and other purposes may be prepared.

Abstract: The present invention relates to the delivery of antipsychotics through an inhalation route. Specifically, it relates to aerosols containing antipsychotics that are used in inhalation therapy. In a method aspect of the present invention, an antipsychotic is delivered to a patient through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises an antipsychotic, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles with less than 5% antipsychotic drug degradation products. In a kit aspect of the present invention, a kit for delivering an antipsychotic through an inhalation route is provided which comprises: a) a thin coating of an antipsychotic composition and b) a device for dispensing said thin coating as a condensation aerosol.

Abstract: Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds to prepare liposomes and other lipid aggregates suitable for transfection or delivery of compounds to target cells, either in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules, particularly polyanions such as nucleic acids. These compounds have the property, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.

Abstract: Disclosed herein are a class of small molecules, referred to as Small Peptide Sequences (SPS), that can stabilize biomolecules, particles containing the SPS and biomolecules, and compositions and methods of making the particles. The SPS are composed solely of amino acids common to humans and too small to trigger an immunological response (typically less than seven amino acids in total) and which will self assemble into particles sufficiently small to stay in liquid suspension at a first pH, typically a non-physiological pH, but which dissociate, releasing the biomolecule entrapped therein into solution, at a second pH, typically a physiological pH. The particles contain a SPS and a biomolecule, wherein the biomolecule is entrapped with the particle, immobilized on the surface of the particle, or combinations thereof. The particle releases the biomolecule upon contact with physiological fluids.

Abstract: The invention provides a medicament-containing particle wherein an unpleasant taste of the medicament is alleviated, which is obtainable by mixing and granulating the following ingredients: (1) the medicament with an unpleasant taste, (2) methylcellulose and (3) mannitol; and a solid preparation including the particle. The invention can make an unpleasant taste of the medicament alleviated and furthermore when the formulation including the particle is administered, the unpleasant taste can be masked and the formulation has a good dissolvability in gastrointestinal tract.

Abstract: In a method for treating a carcinoma in a patient, a medicine is administered via the blood stream of the patient that appears, to the patient's immune system, that tissue of the carcinoma is an inflammation source. The medicine employs two active components that are coupled to each other in a form allowing administration of the two active components to the carcinoma via the blood stream of the patient. A first of the active components is at least one coupling molecule that specifically tethers to a target molecule formed by cancer tissue of the carcinoma. A second of the active ingredients is at least one signal molecule typical to inflammation, or at least one originating molecule encoding such a signal molecule, that induces the immune system of the body to attack the cancer cells.

Abstract: A method of killing a cell that is lacking in effective p53 protein activity, particularly as compared to wild type, is provided characterised in that it comprises delivering to the cell a single stranded DNA including a portion with at least one base, internally located with respect to any 3? and 5? ends of the DNA, that is unbasepaired with another base in a form that is capable of being internalised by the cell.

Abstract: Disclosed herein are methods comprising suspending microparticles in a surfactant/non-polar alkane solution to remove residual solvent that is present in the microparticle.

Abstract: The present technology provides a nanoparticulate in-situ gelling vitreous substitute, which is a liquid at room temperature to aid easy administration, such as e.g. through a small needle incision, and forms a gel within the eye, which is hydrophilic in nature, similar to the natural vitreous. The vitreous substitute formulation may include a water-soluble natural or synthetic polymer and a gelling-agent which are blended together in the presence of a cross linker, to form a gel having the properties of the vitreous humor. The process of cross linking and gelation may occur in-situ. This can be achieved by dispensing to the eye, different components of the vitreous substitute in liquid state, along with the cross linking agent.

Abstract: The present invention provides a particulate pharmaceutical composition which has improved drug encapsulation stability and is suitable for a drug delivery system. The particulate pharmaceutical composition 1 contains: a plurality of block copolymer unit 2 arranged radially, each of which has a hydrophobic polymer-chain segment 2b, which is arranged radially inside, and a hydrophilic polymer-chain segment 2a, which is arranged radially outside; a drug 4, which includes a biomacromolecule; and a charged lipid 3, which has an electrical charge opposite to that of the drug 4; wherein the charged lipid 3 is being attracted to the hydrophobic polymer-chain segment 2b, and the drug 3 is positioned radially inside the hydrophobic polymer-chain segment 2b. The pharmaceutical composition 1 can effectively prevent the drug 4 from disengaging from the particle.

Abstract: The present invention provides an apparatus and methods of producing particles that include a polymer, a wax and/or lipid and, optionally, a biologically active substance. In accordance with the methods of the invention, a load stock including a polymer, a wax and/or a lipid that is a solid at standard temperature and pressure and, optionally, a biologically active substance is provided. The load stock is contacted with a supercritical fluid to form a melt. The melt is contacted with a polar solvent under suitable conditions to form an emulsion. The emulsion is expanded across a pressure drop to form solid particles that include the load stock. The methods and apparatus facilitate the production of very small particles that have a narrow particle size distribution.

Abstract: The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.

Abstract: This invention provides a peptide/nucleic acid composition for oral/mucosal, dual-modal activation of immune protection systems.

Abstract: The present invention application relates to a pharmaceutical preparation to be administered into respiratory organs for treating or preventing inflammatory respiratory diseases, comprising a peptide which acts on formyl peptide receptors (FPRs) or receptors analogous thereto, in an amount which is effective in suppressing respiratory inflammation. The present invention application also relates to a method for treating or preventing inflammatory respiratory diseases by using the preparation, and to a kit containing the preparation. As compared with systemic administration of the peptide by injection, direct administration of the peptide to respiratory organs remarkedly improves the effect in suppressing respiratory inflammation.

Abstract: Pharmaceutical compositions are provided comprising (a) nanoparticles of an active agent and a dextran polymer derivative, and (b) a carrier material.

Abstract: The present invention provides a sustained-release pharmaceutical composition, characterized in that, there are contained tamsulosin or a pharmaceutically acceptable salt thereof and a carrier for a sustained-release pharmaceutical composition and the ratio (Cmin/Cmax ratio) of the plasma tamsulosin concentration at 24 hours after the administration of the preparation per os (Cmin) to the maximum plasma tamsulosin concentration after the administration (Cmax) is about 0.4 or more.

Abstract: The present invention is directed to improved compositions for cellular delivery of peptides. Using segments of only 3-5 positively-charged residues, one can effectively transfer peptides, including therapeutic peptides, into cells. Also provided are modified peptides such as those include stapled and cyclized peptide technology, as well as peptoids/peptidomimetics.

Abstract: A process for inhibiting symptoms of a subject with celiac disease is provided that includes administration of monoclonal-, or polyclonal-, monomeric, dimeric, or polymeric IgA. Joining secretory component to the IgA limits oral administration degradation. Formulating agents are mixed with the monomeric, dimeric, or polymeric IgA to yield a dosing form of a capsule, tablet, and a suppository. The therapeutic is amenable to enrobement directly through microencapsulation or the dosing form is coated with an enteric coating.

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: The invention relates to a composition and a method for manufacturing semi-dry or dry particles containing a mucoadhesive polymer and a bioactive agent such as, but not limited to, an Immunogenic Substance (e.g., a vaccine), that allows the oral or nasal administration and delivery of the bioactive agent essentially unaltered to mucosal surfaces in the animal, including an aquatic animal.

Abstract: The present invention provides effective new methods and materials for maxillofacial bone augmentation, particularly alveolar ridge augmentation, that are free of problems associated with prior art methods. In one embodiment, these materials include human recombinant platelet derived growth factor (rhPDGF-BB) and a biocompatible matrix. In another embodiment, these materials include rhPDGF-BB, a deproteinized bone block or calcium phosphate, and a bioresorbable membrane. The use of these materials in the present method is effective in regenerating maxillofacial bones and facilitating achievement of stable osseointegrated implants. The mandible and maxilla are preferred bones for augmentation, and enhancement of the alveolar ridge is a preferred embodiment of the present invention.

Abstract: A method of preparing a granular delivery system by creating a melt emulsion having a continuous phase and a dispersed active, wherein the continuous phase includes trehalose and a low dextrose equivalent carbohydrate that is not a hydrogenated starch hydrolysate, forcing the melt emulsion through an die or orifice to form an extrudate, cooling and granulating the extrudate to form granules of the delivery system and optionally drying the granules. The melt extrusion provides excellent viscosity and Tg characteristics for the extrusion process.

Abstract: A nanoparticle capable of delivery of an encapsulated molecule into a living cell. The nanoparticle includes an encapsulation media and an isolated nucleic acid homolog sequence. The encapsulation media is primarily polymeric. The nanoparticles release the encapsulated molecule over an extended period of time. Further disclosed are pharmaceutical compositions and articles of manufacture including nanoparticles and methods of preparing and using the nanoparticles.

Abstract: Nutritional compositions delivered in vivo in a time controlled manner sustainable over long periods of time, provide enhancing athletic performance, increased hand/eye coordination and concentration on the task at hand.

Abstract: The present invention provides dynamic charge state cationic polymers that are useful for delivery of anionic molecules. The dynamic charge state cationic polymers are designed to have cationic charge densities that decrease by removal of removable functional groups from the polymers. The present invention also provides interpolyelectrolyte complexes containing the polymers complexed to a polyanion. Methods for using the interpolyelectrolyte complexes to deliver anionic compounds are also provided.

Abstract: The present invention provides AAV capsid proteins (VP1, VP2 and/or VP3) comprising a modification in the amino acid sequence in the three-fold axis loop 4 and virus capsids and virus vectors comprising the modified AAV capsid protein. In particular embodiments, the modification comprises a substitution of one or more amino acids at amino acid positions 585 to 590 (inclusive) of the native AAV2 capsid protein sequence or the corresponding positions of other AAV capsid proteins. The invention also provides methods of administering the virus vectors and virus capsids of the invention to a cell or to a subject in vivo.

Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.

Abstract: Dry cross-linked gelatin compositions are prepared that rapidly re-hydrate to produce gelatin hydrogels suitable as hemostatic sealants. Gelatin is cross-linked in the presence of certain re-hydration aids, such as polyethylene glycol, polyvinylprovidone, and dextran, in order to produce a dry cross-linked gelatin powder. The use of the re-hydration aids has been found to substantially increase the re-hydration rate in the presence of an aqueous re-hydration medium, typically thrombin-containing saline.

Abstract: The present invention is directed to a solid form comprising an active ingredient and croscarmellose, wherein: (i) the croscarmellose has a median particle size of ?56 microns, (ii) the croscarmellose is present in an amount of ?4% by weight based on the total weight of the solid form, and (iii) the solid form is a tablet, capsule, caplet, lozenge or granule. The present invention is also directed to a method of decreasing the disintegration time (for example, in water) of a solid form that comprises croscarmellose in an amount ?4% by weight based on the total weight of the solid form.

Abstract: The invention provides a polymeric film-forming medical sealant. The medical sealant is useful for application to the tonsils and adenoids, wherein the sealant performs at least one of the following functions, a) inhibit the colonization of bacteria, b) inhibit the binding of bacteria to tissue, c) reduction of tissue morbidity, d) hemostasis, e) coating and protection of tissue during healing. e) promotion of healing, and f) reduction of pain.

Abstract: The present invention provides an immunostimulatory complex specifically adapted to act as adjuvant and as a peptide immunogen stabilizer. The immunostimulatory complex comprises a CpG oligonucleotide and a biologically active peptide immunogen. The immunostimulatory complex is particulate and can efficiently present peptide immunogens to the cells of the immune system to produce an immune response. The immunostimulatory complex may be formulated as a suspension for parenteral administration. The immunostimulatory complex may also be formulated in the form of w/o-emulsions or in-situ gelling polymers for the efficient delivery of immunogens to the cells of the immune system of a subject following parenteral administration, to produce an immune response.

Abstract: Embodiments of the invention relate to particles of active substances, methods for preparing the particles, formulations containing the particles, and metered dose inhalers containing the particles or formulations. In one embodiment, an inhaler contains an aerosol formulation containing a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 ?m. The particles may be suspended in a nonsolvent hydrofluorocarbon fluid vehicle (e.g., HFA 134a or 227ea) at a concentration within a range from about 0.2% w/v to about 5% w/v. The formulation exhibits a flocculation volume of about 85% or greater about 1 minute after mixing the particulate active substance and the vehicle. The particulate active substance may contain salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, or derivatives thereof. In some examples, the active substance is dihydroergotamine mesylate.

Abstract: This invention describes a quick-dissolving thin film strips comprising bioactive components encapsulated within pH-sensitive polymeric microparticles. The microparticles are embedded within the thin film and provide protection to components encapsulated within. The invention further describes methods to incorporate bioactive components encapsulated within pH-sensitive polymeric microparticles into a quick-dissolving thin film strip while maintaining the bioactivity of the contained therapeutic agents during thin film formation and microencapsulation.

Abstract: One example embodiment of the present invention relates to an implant with a coating or a cavity filling containing a nucleic acid, which i) can inhibit the expression of at least one representative of the Ras gene family by means of RNA interference; or ii) encodes for a nucleic acid that can inhibit the expression of at least one representative of the Ras gene family by means of RNA interference.

Abstract: The present invention relates to polymer conjugated releasable lipids and nanoparticle compositions containing the same for the delivery of nucleic acids and methods of modulating gene expression using the same. In particular, this invention relates to releasable polymeric lipids containing an acid-labile linker based on a ketal or acetal-containing linker, or an imine-containing linker.

Abstract: The present invention is directed to cationic lipid for the delivery of oligonucleotides and methods of modulating an expression of a targeted gene using the nanoparticle compositions. In particular, the invention relates to cholesterol and its derivatives having multiple positively charged moieties via branching spacers, and nanoparticle compositions of oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.

Abstract: Peptides of general formula (I): R1-Wp-Xn-AA1-AA2-AA3-AA4-Ym-R2 their stereoisomers, mixtures thereof, and/or their cosmetically or pharmaceutically acceptable salts, a method of preparation, cosmetic or pharmaceutical compositions containing them and their use for the treatment, prevention and/or care of conditions, disorders and/or diseases of the skin, mucous membranes and/or scalp.

Abstract: A composition as disclosed is comprised of a plurality of groups of particles. The particles are comprised of a biocompatible polymer which maybe a co-polymer such as PLGA combined with a peptide of a sequence of interest, e.g. a sequence which corresponds to a sequence presented on a surface of a cell infected with a virus. A plurality of different groups of particles are provided in the formulation wherein the particles within any single group include peptides of identical amino acid sequence. The particles are sized such that they are sufficiently large so as to prevent more than the contents of a single particle from being presented to a single immune system cell.

Abstract: The present invention provides novel nanoscale cellulose particles and also a process for their production. The cellulose-based particles obtained have volume -averaged particle sizes of less than 300 nm. These nanoparticles are produced from amorphous cellulose or by amorphization of cellulose, optional subsequent hydrolysis and by input of energy into a water-containing medium after or during dispersion.

Abstract: A self-assembling nanoparticle drug delivery system for the delivery of drugs including peptides, proteins, nucleic acids or synthetic chemical drugs is provided. The self-assembling nanoparticle drug delivery system described herein includes viral capsid proteins, such as Hepatitis B Virus core protein, encapsulating the drug, a lipid bi-layer envelope and targeting or facilitating molecules anchored in the lipid bilayer. A method for construction of the self-assembling nanoparticle drug delivery system is also provided.

Abstract: Inhalation of low levels of nitric oxide can rapidly and safely decrease pulmonary hypertension in mammals. Precise delivery of nitric oxide at therapeutic levels of 20 to 100 ppm and inhibition of reaction of nitric oxide with oxygen to form toxic impurities such as nitrogen dioxide can provide effective inhalation therapy for pulmonary hypertension.

Abstract: The present invention relates to stable active compound complexes of salts of o-acetylsalicylic acid with basic amino acids and glycine, to a process for their preparation and to their use as medicaments.

Abstract: A non-aqueous cleansing formulation having cleansing, moisturizing and/or exfoliating properties includes an oil phase and a natural surfactant derived from legumes and/or grains. The oil phase can include an oil component and a thickening agent. The natural surfactant can be in the form of a particulate flour product derived from Vigna radiata, Vigna mungo, Glycine max, Cicer aerientinum, Vigna unguicalata, Pisum sativum, Phaseolus vulgaris, or combinations thereof, which is dispersed in the oil phase. The flour product suitably includes a high protein flour to emulsify the oil phase and provide improved cleansing action. Such non-aqueous cleansing formulation can be used as skin care products, hand cleansers, hair cleaners or general use cleansers. Advantageously, the cleansing formulations are free of synthetic soaps and/or synthetic surfactants.