Abstract: “Frozen ionic liquid” microparticles and nanoparticles are disclosed, as are alternative methods of making the particles. The particles may be monodisperse or polydisperse, with spherical or other shapes. The particles may be prepared without specialized equipment, and without harsh conditions. The microparticles and nanoparticles have uses in biomedical, materials, analytical, and other fields.

Abstract: The present invention is directed to new oral formulations of chemotherapeutic agents, their process of preparation as well as their therapeutic uses. More specifically, said invention is related to nanoparticles comprising at least one chemotherapeutic agents as an active ingredient, at least one polymer and at least one cyclic oligosaccharide capable of complexing said camptothecin derivative, said nanoparticles being for therapeutic oral administration.

Abstract: The present invention relates to purification and use of a novel emulsion stabilizing polysaccharide. In particular, a polyelectrolyte exopolysaccharide with high molecular weight comprising a high molecular weight polymer with a tri-saccharide repeating unit is disclosed. In one aspect of the invention, methods are directed to isolating and purifying a high molecular weight exopolysaccharide (EPS) from a cell supernatant. In another aspect, methods are disclosed for isolating a lipopolysaccharide (LPS) and a high molecular weight Acinetobacter polyelectrolyte exopolysaccharide (APE) from Acinetobacter bacteria. Compositions are also directed to lipid nanoparticles comprising a therapeutic agent encapsulated by a high molecular weight polysaccharide and nanoparticles comprising a therapeutic agent bound to a cationic polysaccharide cross-linked with a polyanion.

Abstract: Nanoemulsion compositions with low toxicity that demonstrate broad spectrum inactivation of microorganisms or prevention of diseases are described. The nanoemulsions contain an aqueous phase, an oil phase comprising an oil and an organic solvent, at least one anti-inflammatory agent, and one or more surfactants. Methods of making nanoemulsions and inactivating pathogenic microorganisms are also provided.

Abstract: The invention provides a nanoparticle composition that is decorated with a urea-based small-molecule peptidomimetic inhibitor of prostate specific membrane antigen (PSMA), which is expressed by almost all solid tumors. This strategy takes advantage of both the avidity of the functionalized nanoparticle for binding to PSMA and the ability of the nanoparticle to be retained for longer periods of time in the tumor due to enhanced leakage via EPR into the tumor interstitium and poor clearance due to underdeveloped or non-existent lymphatics within the tumor.

Abstract: The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; R1 and R2 are selected from H, —R7—NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R3 and R4 are selected from: H, —R8—SH, R8—NH—NH2/—R8—CO—R9 or —R8—NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.

Abstract: The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also be of a specific polymorphic structure and which may be formed in either hydrophobic or hydrophilic type liquid media.

Abstract: The invention provides a use of a long-circulating microvesicle comprising a sterol, partially synthetic or wholly synthetic vesicle-forming phospholipids, and a corticosteroid in water soluble form, which microvesicle has a mean particle diameter size range of between about 75 and 150 nm and which microvesicle is non-charged or negatively charged at physiological conditions, for the preparation of a medicament for the treatment of atherosclerosis and/or cardiovascular disease. A method for treating a subject suffering from, or at risk of suffering from, atherosclerosis and/or cardiovascular disease, comprising administering to said subject a therapeutically effective amount of such long-circulating microvesicles is also provided.

Abstract: The present invention provides a ceramide dispersion which includes (1) ceramide-containing particles which contains a ceramide, which are dispersed in an aqueous phase as an oil-phase component, and which have a volume average particle diameter from 1 nm to 100 nm; and (2) a fatty acid component which is at least one of a fatty acid having a melting temperature not higher than 30° C. or a fatty acid salt; the amount of nonionic surfactant being 0 or not more than 0.1 times the total mass of the ceramide; the amount of an ionic surfactant other than the fatty acid component being 0 or less than 0.05 times the total mass of the ceramide; and the pH being from 6 to 8.

Abstract: Systems and methods for enhancing the selective targeting of agents for preferential action at a target with reduced action with healthy tissue distal the target tissue. One or more agents can be combined with nano scale structures/particles for delivery to the target tissue. Appropriate bombardment with accelerated particle radiation, such as proton radiation, induces the release of the agents at the target site. Nano carriers can be combined with therapeutic and/or imaging enhancement agents. Imaging of the target tissue can provide a verification of the delivered dose of particle radiation. Nanocarriers can be provided with an outer shell selected for biocompatibility and durability in the in vivo environment and further selected to provide a feedback mechanism in the treatment environment to accelerate the release of the agent and reduce a total radiation dose needed for that release.

Abstract: A composition comprises a surface modified nanoparticle comprising a core comprising a material selected from the group consisting of organic materials, organometallic materials, inorganic materials, metals, metal oxides, and combinations thereof; and a surface branch covalently linked to the core having the general formula (3):

Abstract: The invention relates to polymerase inhibitors, particularly polymerase alpha inhibitors, and the use thereof in the treatment of cell growth disorders, particularly tumor disorders, preferably actinic keratoses, basal cell carcinomas, and/or spinocellular carcinomas.

Abstract: The eye is effectively treated by providing it with formulations including uncoated cationically charged microparticles of reversed cubic phase or reversed hexagonal phase material. The treatment methods are effective; for a variety of diseases and conditions including dry eye. The structure, charge and components of the microparticles in dispersion, with or without an active ingredient, provide mucoadhesion, layering, protection and prolonged duration of ophthalmic action.

Abstract: Provided are a method of manufacturing a solid microstructure capable of controlling multidrug release by mixing a biocompatible or biodegradable material with microparticles or nanoparticles and/or an emulsion as drug carriers and a solid microstructure structure manufactured using the same.

Abstract: Described are drug carriers useful in magnetic resonance imaging (MRI)-guided drug release comprising a shell capable of releasing an enclosed biologically active agent as a result of a local stimulus, e.g. energy input, such as heat, wherein the shell encloses a 19F MR contrast agent. Preferably, the carrier also acts as a contrast enhancement agent for MRI based on the principle of Chemical Exchange-dependent Saturation Transfer (CEST). To this end the shell encloses a cavity that comprises a paramagnetic chemical shift reagent, a pool of proton analytes, and the 19F contrast agent, and wherein the shell allows diffusion of the proton analytes.

Abstract: Devices, compositions, and methods are described which provide a tubular nanostructure or a composite tubular nanostructure targeted to a lipid bilayer membrane. The tubular nanostructure includes a hydrophobic surface region flanked by two hydrophilic surface regions. The tubular nanostructure is configured to interact with a lipid bilayer membrane and form a pore in the lipid bilayer membrane. The tubular nanostructure may be targeted by including at least one ligand configured to bind to one or more cognates on the lipid bilayer membrane of a target cell.

Abstract: The present invention relates to methods of delivering nucleic acids into cells using a nucleic acid binding molecule containing a multimeric or spacer-incorporated protein transduction domain (PTD). The invention also relates to novel compositions that contain a nucleic acid complexed or conjugated with a nucleic acid binding molecule. The nucleic acid binding molecule may contain a multimeric or spacer-incorporated PTD, and may further contain a nucleic acid binding region. The nucleic acid complexes or conjugations of the present invention may be employed to inhibit expression of a target gene, and/or determine the function of a target gene.

Abstract: Iron oxide nano contrast agents for Magnetic Resonance Imaging which have superior T2 contrast effect, and also can be used as a storage or a carrier for drugs and so on, are disclosed. The iron oxide nano contrast agents can be prepared by the steps of: coating surfaces of hydrophobic FeO nanoparticles with a coating material selected from the group consisting of polyethylene glycol-phospholipid conjugate, dextran, chitosan, dimercaptosuccinic acid and mixtures thereof in an organic solvent to form hydrophilic FeO nanoparticles having hydrophilic surfaces and dispersibility in water; dispersing the hydrophilic FeO nanoparticles in water to oxidize FeO; and exposing the oxidized hydrophilic FeO nanoparticles to an acidic buffer to dissolve and remove interior unoxidized FeO portions, and thereby to form Fe3O4 nanoparticles having an interior space.

Abstract: This invention provides novel nanofiber enhanced surface area substrates and structures comprising such substrates for use in various medical devices, as well as methods and uses for such substrates and medical devices. In one particular embodiment, methods for enhancing cellular functions on a surface of a medical device implant are disclosed which generally comprise providing a medical device implant comprising a plurality of nanofibers (e.g., nanowires) thereon and exposing the medical device implant to cells such as osteoblasts.

Abstract: Disclosed herein are methods and materials for influencing proliferation of stem cells. Specifically exemplified herein are compositions comprising cerium oxide nanoparticles which can be used to stimulate proliferation of stem cells under common culture conditions, or which can be utilized to improve therapeutic outcomes.

Abstract: The invention provides products of manufacture, e.g., biomaterials and implants, for cartilage maintenance and/or formation in-vivo, in-vitro, and ex-vivo, using nanotechnology, e.g., using nanotube, nanowire, nanopillar and/or nanodepots configured on surface structures of the products of manufacture.

Abstract: The invention discloses nanoparticles composed of chitosan, poly-glutamic acid, and at least one bioactive agent characterized with a positive surface charge. The bioactive agent is hydrophobic or lipophilic in nature and is associated with micelles before being encapsulated in nanoparticles.

Abstract: The present invention concerns size- and shape-controlled, colloidal superparticles (SPs) and methods for synthesizing the same. Ligand-functionalized nanoparticles such as nonpolar-solvent-dispersible nanoparticles, are used, and the solvophobic interactions can be controlled. Advantageously, supercrystalline SPs having a superlattice structure, such as a face-centered cubic structure, can be produced. Further, the methods of the invention can provide SPs that self-assemble and are monodisperse. The SPs can be doped with organic dyes and further assembled into more complex structures.

Abstract: The present invention relates to pharmaceutical compositions comprising modulators of kinases, kinase binding polypeptides or/and an inhibitor for influenza virus replication for the prevention or/and treatment of influenza.

Abstract: The present invention provides compositions comprising a poorly water soluble pharmaceutical agent, a carrier protein, and an antimicrobial agent, wherein significant microbial growth is inhibited in the composition. The amount of the antimicrobial agent in the composition may be below the level that induces a toxicological effect or at a level where a potential side effect can be controlled or tolerated. Also provided are compositions comprising a poorly water soluble pharmaceutical agent, a carrier protein, a sugar, and optionally an antimicrobial agent. Methods of using the compositions are also provided.

Abstract: The present invention provides a composition comprising vesicles and encapsulated within the vesicles, nucleic acid comprising less than 1000 nucleotides, wherein the vesicles comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block. Methods of forming vesicles and methods of delivering nucleic acid, in particular, iRNA into cells, are also provided.

Abstract: Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.

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

Abstract: Compositions that include Toll-like Receptor 5 agonists and at least a portion of at least one viral antigen can be employed in methods that stimulate an immune response in a subject, in particular, a protective immune response in a subject. Compositions can be associated with particles and employed in the methods in relatively low doses to provide protective immunity to viral infection.

Abstract: The presently disclosed subject matter provides nanoscale coordination polymers for use as anticancer agents and as dual anticancer/imaging agents. The nanoscale coordination polymers can comprise a plurality of platinum metal complexes; nonplatinum anticancer drug bridging ligands complexed to multiple metal centers; or combinations thereof. The nanoscale coordination polymers can be targeted for delivery to cancer cells. They can also comprise stabilizing agents to allow for controlled and/or sustained release of anticancer agents in vivo.

Abstract: The invention relates to a method for the production of nanoparticles from oil-in-water nanoemulsions, in which the nanoemulsion is prepared by phase inversion techniques. The phase inversion may be achieved by using a constant temperature, where the inversion occurs by continuous addition of water or by varying the temperature involving heating and rapid cooling.

Abstract: Magnetically responsive therapeutic carriers comprise nanoparticles including single-domain nanoparticles comprising magnetite and having an average particle size ranging between 1 and 50 nanometers, clusters of the single-domain nanoparticles, the clusters having an average cluster size ranging between 5 and 1000 nanometers, and mixtures of the two. The single-domain nanoparticles are encapsulated with a silica coating. A silane coupling agent is bonded to the silica coating and has a specific pendant functional group capable of selectively binding with the therapeutic. Preferably, the bond between the specific pendant functional group and the therapeutic is a covalent bond. The movement of magnetically responsive nanoparticle therapeutic constructs, with concentration and extravasation/endocytosis at a target site, such as cancerous tumors, uses a controllable magnetic field generator adapted to move the therapeutic constructs in three dimensions, and is enhanced using a repetitively-varying magnetic field.

Abstract: Non-aggregating resorbable calcium phosphosilicate nanoparticles (CPNPs) are bioconjugated to targeting molecules that are specific for particular cells. The CPNPs are stable particles at normal physiological pH. Chemotherapy and imaging agents may be integrally formed with the CPNPs so that they are compartmentalized within the CPNPs. In this manner, the agents are protected from interaction with the environment at normal physiological pH. However, once the CPNPs have been taken up, at intracellular pH, the CPNPs dissolve releasing the agent. Thus, chemotherapeutic or imaging agents are delivered to specific cells and permit the treatment and/or imaging of those cells. Use of the bioconjugated CPNPs both limits the amount of systemic exposure to the agent and delivers a higher concentration of the agent to the cell. The methods and principals of bioconjugating CPNPs are taught by examples of bioconjugation of targeting molecules for breast cancer, pancreatic cancer, and leukemia.

Abstract: The invention is based on the identification of aminopeptidase N (APN) as the receptor for F4 fimbriae of enterotoxigenic E. coli (ETEC). Based on the observation that oral administration of F4 fimbriae induces a protective intestinal mucosal immune response against a subsequent challenge with F4 ETEC, and the observation that the internalization of said F4 fimbriae is clathrin-mediated, the present invention provides the characterization of APN as a target useful in: in an in vitro assay to screen for molecules that are capable to mimic the clathrin-mediated F4 endocytosis; in an in vitro assay to screen for molecules that are capable to modulate the binding of F4 fimbriae with APN; in the development of a carrier for the delivery of antigens/therapeutics, i.e. immunomodulators to the intestinal submucosa or the intestinal mucosa-associated lymphoid tissue, wherein said carrier comprises an APN specific target molecule that mimics the clathrin-mediated F4 endocytosis.

Abstract: The invention relates to ultrasmall, monodisperse nanoparticles comprising silicon dioxide to the surface of which at least one antigen is attached. The nanoparticles can be used for the immunoprophylaxis or immunotherapy of cancer. The invention also relates to a method for the targeting of antigens at antigen-presenting cells and for the activation of the immune system, where the efficiency of targeting and/or immunoactivation are set via the particle characteristics. The invention also relates to a method for the active and passive immunisation of a mammal.

Abstract: A polymeric hollow nanoshell or nanosphere for release of an agent is described, wherein the hollow nanosphere comprises at least one biodegradable polymer, characterised in that the polymer is cross-linked. The biodegradable mono-disperse nanospheres described are suitable for use as carriers of biomolecules, therapeutic agents and/or imaging agents.

Abstract: Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants.

Abstract: A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises poorly water soluble nanoparticles formed by the API together with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

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: This invention concerns a manufacturing process for nanoparticles composted of biodegradable polymers and active ingredients with therapeutic, cosmetic, veterinary, and alimentary applications, and a composition which contains said nanoparticles, which are used in products for animals, including humans. The process consists of emulsifying the hydrosoluble substances to form a w/o emulsion; dissolving the non-emulsionable substances, liposoluble polymer or polymer/compounds in organic solvents; mixing the w/o emulsion and the organic solution of the hydrophobics to form a pre-emulsioned mixture; adding the pre-emulsioned mixture, with the assistance of an injector system, to an aqueous emulsifier solution under ultradispersion to form the final emulsion; leading the final emulsion to evaporation, then centrifuge, freeze, and lyophilize.

Abstract: A bifunctional shRNA-based composition and methods for knocking down the expression of the PDX-1 oncogene in target cells is described herein. The invention also provides methods to deliver the shRNA-containing expression vectors to target tissues overexpressing the PDX-1 oncogene.

Abstract: A gold-creatine nanoparticle is described, preferably covered with albumin, together with a process for its preparation and its use as medicament, in particular for the treatment of stroke. Said gold nanoparticle is capable of crossing the blood-brain barrier.

Abstract: The present invention is directed to nanoparticle compositions 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 oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.

Abstract: The invention relates to a method for preparing an aqueous suspension of nanocapsules comprising an oily core surrounded by a polymeric shell, in which method the following phases are mixed: a) a first phase, called an oily phase, comprising: a hydrophobic polymer, an oil or a mixture of oils, at least one active ingredient, and a surfactant TA1, this oily phase being brought to a temperature T1 higher than the melting point of the hydrophobic polymer, the hydrophobic polymer being miscible, at this temperature T1, with the mixture of the surfactant TA1 and the oil or mixture of oils, and the active ingredient being miscible, soluble or solubilized in the mixture of the surfactant TA1 and the oil or mixture of oils; b) a second phase, called a polar phase, comprising a hydrophilic polymer in the form of a hydrogel in an aqueous solution containing a surfactant TA2, in such a way as to obtain the formation of the nanocapsules in an aqueous suspension.

Abstract: Single-core and multi-core microcapsules are provided, having multiple shells, at least one of which is formed of a complex coacervate of two components of shell materials. The complex coacervate may be the same or different for each shell. Also provided are methods for making the microcapsules.

Abstract: The present invention concerns a composition comprising vesicles and encapsulated within the vesicles, an antibody, wherein the vesicles comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block. Methods of delivering the above compositions into cells are also described.

Abstract: In various embodiments, provided are multi-functional biodegradable particles for selectable targeting, imaging, and delivery of therapeutic agents. Also provided are methods of using the provided particles for treatment of ocular disorders, such as for the treatment of age-related macular degeneration. The provided particles and methods provide a clinician with options for control over, and monitoring of, the delivery of therapeutic agents.

Abstract: An aspect of the present invention is the use of a preparation containing a phytepsin, more specifically a cyprosin, containing the heterodimer, its N-terminal pro-peptide, the mature N-terminal peptide, and mature C-terminal peptide, as well as other precursor species, processing products, and aggregate species, either isolated or in any combinations of the former, native, extracted and partially purified from flowers of Cynara cardunculus, or recombinant, extracted from the supernatant from a culture of Saccharomyces cereviseae genetically modified for the heterologous production of cyprosin, for therapeutic applications more precisely for its use as an antitumor agent.

Abstract: The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.

Abstract: The present invention discloses a magnetic nanocomposite for inhibiting/treating cancer and a method for fabricating the same. The magnetic nanocomposite comprises a core formed of a plurality of magnetic nanoparticles made of ferric ferrous oxide (Fe3O4); a shell made of a carboxy-functionalized polyaniline; and an anti-tumor medicine bound to the external surface of the shell. The method of the present invention fast fabricates the magnetic nanocomposite in a simple way. The medicine of the present invention has a longer half life and a better thermal stability. The present invention disperses the water-insoluble medicine in water uniformly to decrease the biological rejection. Moreover, the magnetic nanocomposite of the present invention is guided to the nidus by an external magnetic field to increase the local concentration of the medicine and provide an effective chemotherapy. Therefore, the present invention has competitive advantage over the conventional BCNU.