Abstract: A particle includes a ferromagnetic material, a radiopaque material, and/or an MRI-visible material.

Abstract: The invention concerns particulate vectors designed to improve oral absorption of active principles, characterized in that they consist of a polymeric matrix comprising at least a biodegradable polymer associated with at least a polycationic polymer.

Abstract: This invention relates to methods and compositions for the treatment, management or prevention of injuries to one or more of the organs of the body, such as the brain, heart, lung, kidneys, liver, and gastrointestinal tract, of humans or other mammals caused by one or more anticancer agents. The methods of this invention consist of the administration of an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds, which includes native human PACAP38, native human PACAP27, native human vasoactive intestinal peptide (VIP), their agonists, analogs, fragments, and derivatives, with activities toward one or more of the PACAP/VIP receptors, including all of their various isoforms.

Abstract: A composition intended to be employed for therapeutic purposes incorporates a source of nicotine and at least one levulinate moiety. Representative forms of nicotine include free base (e.g., as a mixture of nicotine and microcrystalline cellulose), a nicotine salt (e.g., as nicotine bitartrate) or nicotine polacrilex. The levulinate moiety can have the form of an acid (e.g., levulinic acid), a levulinate salt (e.g., sodium levulinate), or an ester of levulinic acid (e.g., methyl levulinate or ethyl levulinate). The composition can incorporate nicotine and levulinic acid in a salt form (e.g., nicotine levulinate). The composition can be composed of at least two forms of nicotine, and one of the forms of nicotine is in the form of nicotine levulinate. The composition is useful for treatment of central nervous system conditions, diseases, and disorders, and as a nicotine replacement therapy.

Abstract: Polymeric microparticles are used to deliver recombinagenic or mutagenic nucleic acid molecules such as donor nucleic acid alone, or in combination with triplex-forming molecules, to induce a site-specific mutation in the target DNA. Target cells endocytose the particles, releasing the nucleic acid molecules inside of the cell, where they induce mutagenesis or recombination at a target site. The examples demonstrate that triplex forming oligonucleotides, preferably PNAs, preferably in combination with a donor nucleotide molecule, can be encapsulated into polymeric microparticles, which are delivered into cells. Results demonstrate significantly greatly levels of uptake and expression, and less cytotoxicity, as compared to direct transfer of the nucleic acid molecules into the cell by nucleofection.

Abstract: The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-1 receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.

Abstract: A method for preparing drug in hemisphere-shaped dosage form. A high molecular weight solution containing the drug is prepared, and the solution is then dropped on a base material. The interface phenomena between the solution and different base materials makes the drop of high molecular weight solution containing the drug form a hemisphere-shape. After solidifying by cross-link or evaporation, the drug in hemisphere-shaped dosage form is obtained. The advantages of the preparation method are a simple and fast process, and simple operation. Applications of the method to prepare a drug in hemisphere-shaped dosage form are also provided.

Abstract: The present invention relates to compositions comprising 4-(2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazol-3-ylthio)acetamido)-3-chlorobenzoic acid or pharmaceutically acceptable salts thereof, and to the preparation and use of such compositions, in particular for the treatment of diseases.

Abstract: Novel calcium phosphate core particles, methods of making them, and methods of using them as vaccine adjuvants, as cores, as carriers of biologically active material, and as controlled release matrices for biologically active material are disclosed. The core particles may have a surface modifying agent and/or biologically active material, such as antigenic material or natural immunoenhancing factor, polynucleotide material, or therapeutic proteins or peptides, partially coating the particle or impregnated therein.

Abstract: Gel particles or beads can be prepared by forming a hot aqueous solution of a gelling agent, and discharging the hot gelling agent solution through a discharge orifice into a cold moving stream of hydrophobic liquid so that the gelling agent solution cools rapidly and good quality gel particles coalesce in the cold hydrophobic liquid stream. The cold hydrophobic liquid stream can be contained in a conduit so that the cold hydrophobic liquid stream moves past the discharge orifice and exerts a force on hot solution in the discharge orifice, the force acting to withdraw the hot solution from the discharge orifice. Optionally, the gel particles can be crushable gel beads 10 formed of an agar complex providing cosmetic, pharmaceutical, etc. delivery vehicles for topical delivery of biologically or cosmetically active agents. Preferred agar beads 10 are complexes of a continuous phase of agar gel 12 in a self-supporting solid or semi-solid form with a restraining polymer 14.

Abstract: The present invention is directed to releasable cationic lipids and nanoparticle compositions for the delivery of nucleic acids and methods of modulating an expression of a target gene using the same. In particular, the invention relates to cationic lipids including an acid labile linker, and nanoparticle compositions containing the same.

Abstract: The present invention relates to a haemostatic composition comprising a biologically absorbable material and hyaluronic acid or a derivative thereof, methods of producing such compositions and the use of these compositions. In particular the method of producing said haemostatic composition comprises treating it with dry heat at a temperature between 110-200° C.

Abstract: A tissue adhesive including cyanoacrylate and polyethylene glycol (PEG), wherein the PEG remains a polyether and wherein the tissue adhesive is bioabsorbable. A tissue adhesive including cyanoacrylate bulk monomer and cyanoacrylate nanoparticles containing a therapeutic therein. A kit for applying a tissue adhesive, including the tissue adhesive described above and an applicator. Methods of accelerating degradation of a cyanoacrylate tissue adhesive applying a tissue adhesive, closing an internal wound, administering a therapeutic to tissue, treating cancer, and preventing infection in a wound. Methods of method of making a bioabsorbable tissue adhesive and making a therapeutic tissue adhesive.

Abstract: The invention relates to injectable long-acting insulin formulations for the treatment of types I and II diabetes in humans and animals. The essential object of the invention is to provide an injectable long-acting insulin formulation in the form of a colloidal suspension which is stable, which has a good local tolerance and toxicity compatible with the chronic treatment of diabetics, and which maintains a substantial hypoglycemic effect extending over at least 24 hours after a single administration, e.g. by the subcutaneous route. To achieve this object, the invention relates to a stable aqueous colloidal formulation of insulin-laden nanoparticles of at least one poly(Leu-block-Glu) in which the pH is between 5.8 and 7.0, the osmolarity O (in mOsmol) . . . : 270?O?800, and the viscosity v (in mPa·s) is low, namely v?40. The nanoparticles of poly(Leu-block-Glu) have a mean hydrodynamic diameter Dh such that: 15?Dh?40.

Abstract: Use of a polyamino acid as an adjuvant; an application of a polyamino acid as an adjuvant in the production of a vaccine; a vaccine comprising a polyamino acid as an adjuvant; a biodegradable nanoparticle having a virus antigen immobilized thereon; and a vaccine comprising the biodegradable nanoparticle.

Abstract: A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration—time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.

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

Abstract: Neutrophil elastase (NE) is a protease secreted by neutrophils during inflammation. Aberrant expression of NE such as in chronic respiratory inflammatory diseases, results in tissue destruction and decline in lung function. Compositions including an NE-targeting agent that targets the pathologic elements of respiratory inflammation are provided. Non-anticoagulant heparin derivatives or fragments are exemplary NE-targeting agents. The compositions preferably include a carrier, such as chitosan, to facilitate delivery of the active agent. Methods of manufacturing non-anticoagulant heparin are also provided. Methods of administering the disclosed compositions to treat respiratory diseases are also disclosed. In preferred methods, an effective amount of the pharmaceutical composition is administered to subject in need thereof to reduce, inhibit, or alleviate one or more symptoms of chronic respiratory inflammation.

Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, b) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.

Abstract: A method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting is disclosed. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate is lubricated and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa. A method for evaluating binders is also disclosed.

Abstract: The present invention provides compositions and methods for the delivery of interfering RNAs that silence APOB expression to liver cells. In particular, the nucleic acid-lipid particles provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of APOB at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: This invention relates to a flowable collagen/glycosaminoglycan (GAG) material including particles of collagen/GAG matrix that, when hydrated, can be effectively delivered to wounds having varying depths and geometries. The flowable collagen/GAG matrix allows a more intimate contact between the wound matrix and the wound bed, and provides a structural framework that serves as a scaffold for cell ingrowth.

Abstract: The present invention relates to the modification of hyaluronic acid (HA) with aryl/alkyl succinic anhydrides (ASA) to produce aryl/alkyl succinic anhydride HA derivatives, to the derivatives as such, and to their applications and uses, particularly in the cosmetic and biomedical industries. The ASA-HA derivatives are expected to have interesting properties that can be used for advanced formulation (bind stronger to the skin compared to non-modified HA), possibly also in delivery systems for actives or drugs by encapsulation (nano/micro capsules) or formation of nano/micro spheres. Further, the low MW ASA-HA derivatives are expected to penetrate the skin more efficiently than non-modified HA of the same MW.

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

Abstract: Provided herein, for example, are microspheres comprising a gelatin or gelatin substitute and a copolymer of a N-tris-hydroxymethyl methylacrylamide monomer unit, a diethylaminoethylacrylamide monomer unit and a N,N-methylene-bis-acrylamide monomer unit. Also provided are methods of producing microspheres comprising a gelatin or gelatin substitute and a copolymer of a N-tris-hydroxymethyl methylacrylamide monomer unit, a diethylaminoethylacrylamide monomer unit and a N,N-methylene-bis-acrylamide monomer unit. Further provided herein, for example, are compositions comprising the microspheres and methods of using the microspheres and compositions thereof.

Abstract: Described herein are compounds such as macromolecules that have been modified in order to facilitate crosslinking by introduction of at least one hydrazide-reactive group and/or aminooxy-reactive group, and methods of making and using thereof for scar-free wound healing, for delivering bioactive agents or living cells, for preventing adhesion after a surgical procedure or for bone and cartilage repair. The macromolecule can be an oligonucleotide, a necleic acid, a polypeptide, a lipid, a glycoprotein, a glycolipid, a polysaccharide, a protein or a synthetic polymer, preferably a glycosaminoglycan like hyaluronan.

Abstract: Particulate ?-glucan is solubilized at elevated pressure and temperature to form particulate-soluble ?-glucan. The particulate-soluble ?-glucan is capable of being dried to a powder form and subsequently re-solubilized.

Abstract: The present invention relates to a composition of at least one protease and a mode of application for treating patients suffering from pancreatic enzyme insufficiency, pancreatitis or cystic fibrosis. The composition of enzymes comprises at least one protease which has a pH optimum below 5.0 and wherein said protease is further active in the presence of pepsin. In a preferred embodiment, said protease is of microbial origin.

Abstract: The invention relates to a recombinant protein used for immunoprophylaxis of human Helicobacter pylori infection and a degradable slow-releasing microsphere-encapsulated oral vaccine preparation prepared from the same, and the preparation method thereof. Said recombinant protein is composed of A2 subunit and B subunit of the LT of enterotoxigenic Escherichia coli and urease B subunit. The vaccine provided in the invention used in human Helicobacter pylori infection is safe and effective and convenient for oral intake.

Abstract: Group C rotaviruses are a cause of acute gastroenteritis in children and adults that is distinct from group A RV. However, human group C rotaviruses cannot be grown in culture, resulting in a lack of tools for detection and treatment of GrpC RV disease. Consequently, the burden of GpC RV disease has not been clearly established. Isolated recombinant human rotavirus group C virus-like particles are provided according to embodiments of the present invention along with methods of their production and use in, inter alia, detection of Grp C RV infection, diagnostic assays and immunogenic compositions.

Abstract: Macromolecular contrast agents for magnetic resonance imaging are described. Biomolecules and their modified derivatives form stable complexes with paramagnetic ions thus increasing the molecular relaxivity of carriers. The synthesis of biomolecular based nanodevices for targeted delivery of MRI contrast agents are described. Nanoparticles (NP) have been constructed by self-assembling of chitosan (CHIT) as polycation and poly-gamma glutamic acids (PGA) as polyanion. NP's are capable of Gd-ion uptake forming a particle with suitable molecular relaxivity. Folic acid (FA) is linked to the NP's to produce NP-FA bioconjugates that can be used for targeted in vitro delivery to a human cancer cell line.

Abstract: The invention provides porous biomaterials and methods for forming porous biomaterials. The porous biomaterials of the invention comprise a biocompatible polymer scaffold defining an array of pores, wherein substantially all the pores have a similar diameter, wherein the mean diameter of the pores is between about 20 and about 90 micrometers, wherein substantially all the pores are each connected to at least 4 other pores, and wherein the diameter of substantially all the connections between the pores is between about 15% and about 40% of the mean diameter of the pores. The invention also provides implantable devices comprising a layer of a biomaterial, and methods for promoting angiogenesis in and around an implantable biomaterial.

Abstract: The invention concerns a pharmaceutical composition containing micronized fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, preferably hydroxypropylmethylcellulose. The cellulose derivative represents less than 20 wt. % of the composition. The association of micronized fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enables enhanced bioavailability of the active principle. The invention also concerns a method for preparing said composition without using any organic solvent.

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: Coprocessed compositions containing microcrystalline cellulose and calcium carbonate, wherein the weight ratio of microcrystalline cellulose to calcium carbonate is relatively high, are useful as excipients in the preparation of solid dosage forms containing active pharmaceutical ingredients, particularly those prepared by processes involving multiple compaction steps. Such compositions may be obtained, for example, by preparing aqueous slurries or wet masses of microcrystalline cellulose and calcium carbonate and drying such slurries or wet masses to produce particulate products. The coprocessed products exhibit improved recompactibility, as compared to coprocessed products having lower microcrystalline cellulose:calcium carbonate weight ratios or as compared to physical dry blends of the two excipients.

Abstract: In various aspects provided are methods for producing a nanoparticle within a cross-linked, collapsed polymeric material, said method including (a) providing a polymeric solution comprising a polymeric material; (b) collapsing at least a portion of the polymeric material about one or more precursor moieties; (c) cross-linking the polymeric material; (d) modifying at least a portion of said precursor moieties to form one or more nanoparticles and thereby forming a composite nanoparticle. In various embodiments, a non-confined nanoparticle can be produced by complete pyrolysis of the confined nanoparticle, and a carbon-coated nanoparticle by incomplete pyrolysis of the confined nanoparticle.

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

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: There is described the use of the Human herpesvirus type 6 (HHV-6) U94 gene and its product, the protein Rep, expression vectors and pharmaceutical compositions suitable for the delivery of the U94 gene or the protein encoded therefrom to the therapeutic sites, to inhibit angiogenic and lymphangiogenic processes in a subject in need thereof.

Abstract: The present invention relates to a nanoparticulate system useful for the delivery of pharmacologically active molecules, and especially for transfecting polynucleotides into cells. It comprises nanoparticles of chitosan of low molecular weight and hyaluronan.

Abstract: This invention pertains to the formulation of nanoparticles that have intrinsic antimicrobial and anti-inflammatory activity. The nanoparticles can be impregnated with one or more therapeutic agents and thereby enhance the antimicrobial and/or anti-inflammatory activity of such agents, and also other properties that the therapeutic agents provide.

Abstract: The present invention generally relates to suspension compositions having a carboxyvinyl polymer such as a carbomer, a galactomannan such as guar, and a borate compound. A sparingly soluble particulate compound such as nepafenac is also included in the compositions. The sparingly soluble particulate compound has a small particle size to enhance bioavailability of the compound.

Abstract: The invention provides, among other things, lyophilized compositions of high surface area that comprise a protein and that reconstitute quickly and efficiently to solution of high protein concentration with minimal formation, if any, of foam, effervescence, bubbles, turbidity, or particulates that might be deleterious. The invention also provides, among other things, methods for making the lyophilized compositions. The invention in additional aspects also provides Raman Imaging Spectrographic methods for real time analyses of polymorphs in a sample using PLS algorithms. By way of particular example, the use of the method for the analysis of mannitol polymorphs is described, and the use of the analysis to determine optimum compositions and lyophilization methods for producing lyophilates of pharmaceutical proteins having a predefined distribution of mannitol polymorphs and having the aforementioned reconstitution properties is also described.

Abstract: A process for treating foliage by retaining an active agent in contact with the foliage is provided that includes the application of a biologically active ingredient carrier granule. The granule includes a mineral component, a cellulosic component, and a binder flowing upon wetting intermixed with the mineral component and the cellulosic components. A biologically active ingredient is added to the granule to treat the foliage. The foliage in either a dry or pre-wetted state. The contact of the granule with water causes the granule to flow to form a coherent film bound by the binder on the foliage with the active agent retained in the film in contact with the foliage.

Abstract: The invention relates to a novel suspension delivery system for the sustained and controlled release of pharmaceuticals. Methods of preparation and use are also disclosed.

Abstract: A drug delivery particle including a reservoir region having primarily large pores and a metering region. The particle can be highly spherical.

Abstract: Provided herein are hemostatic compositions. In one embodiment, the hemostatic composition includes cross-linked polymer microspheres, such as cross-linked gelatin microspheres with pores. In another embodiment, the hemostatic composition comprises an additive such as a wetting agent, a suspending agent, or both. The hemostatic compositions may also include a hemostatic agent such as thrombin, and may include a high concentration of thrombin. The hemostatic compositions may also include plasma. Also provided herein are devices for dispersing said hemostatic compositions in a diluent, and delivering said dispersed hemostatic composition. The hemostatic compositions may also fabricated with a selected geometry as administration suggests.

Abstract: The present invention relates to protamine/RNA nanoparticles of defined average size, a pharmaceutical composition containing said nanoparticles and to a method of producing the same. The nanoparticles of the present invention is particularly useful as an immunostimulating medicament with a precise pattern of immunostimulation different from the prior art.

Abstract: The present application relates to methods of providing thermodynamically stable calcium phosphate nanoclusters and uses thereof.

Abstract: Novel classes of multi-arm polyalkylene oxide-based materials including PEG nanocarriers, nanogel particles, and aggregated nanogel particles are disclosed. These classes of compositions may be associated with therapeutic agents and targeting moieties, or visibility enhancing agents, and may have a modified surface structure. In some embodiments the PEG-based materials can be made to provide relatively high drug loads with improved solubility and targeted delivery.