Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: The invention provides a cyclodextrin-containing polymer comprising one or more cyclodextrin residues. The polymer is selected from a peptide, a polypeptide, an oligonucleotide or a polynucleotide or a mixture thereof. The peptide or polypeptide has at least one amino acid residue containing a functional side group and at least one of the cyclodextrin residues is covalently linked to the functional side group of the amino acid residue of said peptide or polypeptide or to the sugar moiety of a nucleotide residue of the oligonucleotide or polynucleotide.

Abstract: The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide chelated with at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such us for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic is pulmonary embolus.

Abstract: A nose and throat anti-influenza solution is described that decreases the likelihood influenza infection and its spread. The solution's components are readily available and have been used to treat humans for other ailments previously, leading to an easily implemented, scalable, safe, and cost-effective solution. The core components of the solution include: specially denatured alcohol (SDA); Triton x-100; sodium saccharin; 1,8 cineole (eucalyptol); thymol; methyl salicylate; menthol; sorbitol and/or glycerin; sodium benzoate; poloxamer 407; polysorbate 80; and distilled water. Optionally, the solution also includes one or more of the following: citric acid; sambucus nigra agglutinin; a lectin that binds 2,3 sialic acid; nonoxynol-9; sialyllactose; a protease; a protease inhibitor; and/or chloroquine. The solution is applied to the nasal cavity via a pre-moistened cotton swab or a pre-moistened facial tissue and the solution is applied to the back of the throat via a spray, gum, or gargle solution.

Abstract: Compositions are provided comprising a family of peptides having binding specificity for bone, and their use to produce coating compositions. The coating compositions are used to deliver a pharmaceutically active agent to bone, and are used in methods related to bone implants, bone repair, and bone-related diseases.

Abstract: The present invention concerns a delivery system comprising a polymer-based nanoparticle; and a linker comprising a first portion non-covalently anchored to said nanoparticle, wherein at least part of said first portion comprises a hydrophobic/lipophilic segment embedded in said nanoparticle; and a second portion comprising a maleimide compound exposed at the outer surface of said nanoparticle. In accordance with one embodiment, the delivery system comprises one or more targeting agents, each covalently bound to said maleimide compound. In accordance with yet another embodiment, the delivery system comprises a drug. A specific example for a linker in accordance with the invention is octadecyl-4-(maleimideomethyl)cyclohexane-carboxylic amide (OMCCA).

Abstract: Devices, methods, and compositions for improving vision or treating diseases, disorders or injury of the eye are described. Ophthalmic devices, such as corneal onlays, corneal inlays, and full-thickness corneal implants, are made of a material that is effective in facilitating nerve growth through or over the device. The material may include an amount of collagen greater than 1% (w/w), such as between about 10% (w/w) and about 30% (w/w). The material may include collagen polymers and/or a second biopolymer or water-soluble synthetic polymer cross-linked using EDC/NHS chemistry. The material may additionally comprise a synthetic polymer. The devices are placed into an eye to correct or improve the vision of an individual or to treat a disease, disorder or injury of an eye of an individual.

Abstract: Self-dissolving needle-like or filamentous shape percutaneously absorbable preparations, by which inherently poorly absorbable drugs into the body through the skin is efficiently administered. The preparations are made of at least one material selected from the group consisting of proteins, polysaccharides, polyvinyl alcohols, carboxyvinyl polymers and sodium polyacrylic acids. An active substance contained therein is released in a sustained-release fashion (1) by forming a water-insoluble layer on its surface, (2) by holding the active substance in porous materials, or (3) by imparting a long-acting characteristic to the active substance. The present invention also provides a sheet-like carrier for holding the preparations on at least one of the sides thereof, and a piece of equipment for holding the preparations so as to facilitate the administration of them.

Abstract: The present invention provides a non-naturally occurring lipoprotein nanoplatform (“LBNP”) comprising at least one cell surface receptor ligand; at least one lipoprotein; and at least one diagnostic agent and/or at least one therapeutic agent. In embodiments of the present invention, the cell surface receptor ligand is not a low-density lipoprotein receptor ligand and the cell surface receptor ligand is covalently bonded to the apoprotein. The present invention also provides pharmaceutical formulations comprising LBNPs and methods of making the LBNPs.

Abstract: The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.

Abstract: A medicament for administration to a non-human animal, wherein the medicament includes at Least partially hydrolysed protein and one or more pharmacologically active substances. In a preferred embodiment, the protein is derived from meat which is hydrolysed using a fruit-derived proteolytic enzyme such as actinidin from kiwifruit which enhances the palatability of the resulting hydrolysate. A method of manufacturing the medicament, and a method of medicating a non-human animal by administering to the animal a medicament are also disclosed.

Abstract: A graft prostheses (11), materials and method for implanting, transplanting, replacing, or repairing a part of a patient. The graft prosthesis includes a purified, collagen-based matrix structure removed from a submucosa tissue source. The submucosa tissue source is purified by disinfection and removal steps to deactivate and remove contaminants, thereby making the purified structure biocompatible and suitable for grafting on and/or in a patient.

Abstract: Improved methods and preparations are provided for ocular administration of therapeutic drugs. The preparations include respective quantities of a drug and a peptide which enhances transport of the drug across ocular tissues. The drug and peptide components may be separately administered or used as a mixture. The preferred peptide is NC-1059 (Seq. ID No. 1).

Abstract: The non-invasive administration of many active ingredients fails with efflux pumps which sharply reduce the active ingredient absorption on mucous membranes. According to the invention, the active ingredient absorption on mucous membranes can be drastically improved by using dosages containing glutathione and/or compounds comprising numerous thiol groups, in addition to the active ingredient(s). Forms of administration such as matrix tablets, capsules, eye drops, or microparticles, containing the cited combination of active ingredients and auxiliary substances, can be used.

Abstract: The invention relates to tissue filler compositions that are alterable or removable on demand. Also provided are methods for filling or augmenting tissue using the tissue fillers described herein, and correcting such tissue implants as required.

Abstract: The present invention refers to uses of crotamine and compositions containing it, based on its characteristic of interaction with genetic material. Under submicromolar quantities, the polypeptide is no longer toxic, presenting the characteristics properties of cell penetration, transport of molecules to the surface, cytoplasm or cell nucleus and particularly, selective cell penetration. The invention also refers to compositions comprising a pharmaceutically effective concentration of crotamine and its use for the treatment of diseases and dysfunctions, based on its characteristics of interaction with genetic material, such as DNA and RNA, and cell selectivity.

Abstract: A biodegradable biopolymer material consists of silk fibroin from domesticated silkworm; silk fibroin from wild silkworm; a composite material comprising silk fibroin from domesticated silkworm and silk fibroin from wild silkworm; or a composite material comprising either silk fibroin from domesticated silkworm or silk fibroin from wild silkworm and at least one secondary substance selected from the group consisting of cellulose, chitin, chitosan, chitosan derivatives, keratin from wool and polyvinyl alcohol. The material may be prepared by, for instance, casting an aqueous solution of domesticated silkworm silk fibroin on the surface of a substrate and then cast drying the applied solution. The biodegradable biopolymer material is effectively used as, for instance, a metal ion-adsorbing material, a sustained release substrate for a useful substance such as a medicine, a biological cell-growth substrate and a biodegradable water-absorbing material.

Abstract: Nanostructure-drug conjugates and associated methods of use are provided. In one embodiment, a nanostructure-drug conjugate comprising a Cn, a crosslinker, and a drug is provided, wherein Cn refers to a fullerene moiety or nanotube comprising n carbon atoms. A method of treating cancer is also provided, comprising administering a therapeutically effective amount of a nanostructure-drug conjugate comprising: a Cn, a crosslinker, and a drug, wherein Cn refers to a fullerene moiety comprising n carbon atoms to a mammal.

Abstract: In accordance with the present invention, there are provided methods for treating hyperplasia in a subject in need thereof. In another aspect of the invention, there are provided methods for reducing neointimal hyperplasia associated with vascular interventional procedures. Formulations contemplated for use herein comprise proteins and at least one pharmaceutically active agent.

Abstract: Peptides have been discovered which are capable of binding to and internalizing with the human transferrin receptor (hTfR). The sequences HAIYPRH (Seq. ID No. 1) and THRPPMWSPVWP (Seq. ID No. 2) are capable of binding to and internalizing with the human transferrin receptor. When these molecules were fused with other molecules, the fusion product was internalized in cells expressing hTfR. The sequences have use for targeting other peptides and proteins into cells expressing hTfR.

Abstract: An isolated or purified nucleic acid molecule consisting essentially of a nucleotide sequence encoding the metastasis suppressor gene located at p21-p12 on chromosome 8 of a human (Tey 1), a variant Tey 1, or a fragment of either of the foregoing comprising at least 455 contiguous nucleotides; an isolated or purified nucleic acid molecule consisting essentially of a nucleotide sequence that is complementary to a nucleotide sequence encoding Tey 1, a variant Tey 1, or a fragment of either of the foregoing comprising at least 455 contiguous nucleotides; a vector comprising any of the foregoing, wherein, when the isolated or purifies nucleic acid molecule consists essentially of a nucleotide sequence encoding Tey 1 or a variant thereof, the isolated or purified nucleic acid molecule is optionally part of an encoded fusion protein; a cell comprising and expressing any of the foregoing isolated or purified nucleic acid molecules, optionally in the form of a vector; an isolated or purified polypeptide molecule cons

Abstract: The present invention relates to dry particulate encapsulation compositions comprising a water-insoluble matrix comprising at least 70% by weight of proteins, based on the total weight of the matrix and a moisture content of about 5 to 10% by weight, based on the total weight of the matrix and an encapsulate encapsulated in the matrix, wherein the matrix once wetted in a clear colorless aqueous solution or in mineral oil has a lightness value (L*) greater than about 40, a color vividness or Chroma (C*) lower than about 33 and a hue angle between about 70 and 90. The encapsulation compositions of the present invention are useful in encapsulating dyes, medications and vitamins. Fine particulate encapsulation compositions comprising natural dyes can be used in lieu of artificial lakes in confectionery, cosmetics and caplets color coatings.

Abstract: A method and material for augmenting the shape and thickness of the cornea in situ includes applying a clear liquid collagen mixed with a customized crosslinker onto the augmentation surface or in a cavity (with or without a mold) and exposing the mixture to UVA radiation in vivo. Application of UVA at varying dosages demonstrate progressive optically clear gelation and biomechanical adherence properties, and in vitro optical properties (RI), mechanical suture strength and rheometric parameters are comparable to native corneal stromal tissue. Photochemical corneal collagen augmentation according to the invention makes it suitable to reconstruct and strengthen diseased and damaged eyes, ulcerated corneas, as well as provide a substrate for refractive onlay/inlay procedures and lamellar transplantation.

Abstract: The invention relates to the field of drug delivery, in particular, to compounds and methods for the chemical modification of a proteinaceous channel to be used in pharmaceutical delivery vehicles for controlled and/or localized release of therapeutic molecules (e.g., small molecules, peptides, proteins or other macromolecules). Provided are drug delivery vehicles comprising a pH- and/or light-responsive channel protein.

Abstract: (A compound comprises a thiopeptide, or derivative or analogue thereof, the thiopeptide comprising a C-terminal carboxylic acid group, and a functional group for attachment to a drug, characterised in that the compound is adapted to carry or transport a drug.

Abstract: The invention relates to the treatment and prevention of atherosclerosis and cardiovascular diseases associated with atherosclerosis. The invention further relates to methods of diagnosing atherosclerosis and cardiovascular diseases associated with atherosclerosis. In certain embodiments, the invention provides biological systems and methods for delivering a therapeutic agent or an imaging agent to atherosclerotic lesions such as vulnerable plaques.

Abstract: Compositions for forming a self-reinforcing composite biomatrix, methods of manufacture and use therefore are herein disclosed. Kits including delivery devices suitable for delivering the compositions are also disclosed. In some embodiments, the composition can include at least three components. In one embodiment, a first component can include a first functionalized polymer, a second component can include a second functionalized polymer and a third component can include silk protein or constituents thereof. In some embodiments, the composition can include at least one cell type and/or at least one growth factor. In some embodiments, the composition can include a biologic encapsulated, suspended, disposed within or loaded into a biodegradable carrier. In some embodiments, the composition(s) of the present invention can be delivered by a dual lumen injection device to a treatment area in situ, in vivo, as well as ex vivo applications.

Abstract: The present invention is a composition for providing localized delivery of a therapeutic agent to a subject. The instant composition is a hydrophilic matrix-based prodrug system, wherein a protease substrate peptide acts as extracellular protease degradable spacer binding the therapeutic agent to a hydrophilic matrix. Release of the therapeutic agent is achieved by localized activity of extracellular proteases thereby providing minimal toxicity of the therapeutic agent and maximum release with protease activity. Methods for producing the instant composition and providing localized delivery of a therapeutic agent to a subject are also provided.

Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.

Abstract: A carrier system in the form of protein-based nanoparticles for the cell-specific, intracellular enrichment of at least one pharmacologically active substance. The system has structures that are coupled by reactive groups. The structures enable a cell-specific attachment and cellular absorption of the nanoparticles.

Abstract: The present invention relates to nitric oxide-releasing amidine diazeniundiolates, compositions comprising same, methods of using same, and a method for preparing same from imidate diazeniumdiolates and primary or secondary amines.

Abstract: A composition comprising intact minicells that contain a drug molecule is useful for targeted drug delivery. One targeted drug delivery method employs bispecific ligands, comprising a first arm that carries specificity for a bacterially derived minicell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target drug-loaded minicells to specific mammalian cells and to cause endocytosis of the minicells by the mammalian cells. Another drug delivery method exploits the natural ability of phagocytic mammalian cells to engulf minicells without the use of bispecific ligands.

Abstract: The invention relates to synthetic leptin antagonists in which at least two amino acid residues of the sequence LDFI/S of the hydrophobic binding site at positions 39-42 of a leptin polypeptide sequence are substituted with different amino acid residues such that the site becomes less hydrophobic, and fragments of said leptin antagonists.

Abstract: Disclosed herein is a oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: Polymers containing amino acid and/or polypeptide moieties in their backbones or pendant to their backbones are made by metathesis. A method of making an amino acid or polypeptide containing polymer includes the steps of: providing a amino acid, amino alcohol, or polypeptide-containing monomer; forming a reaction mixture by contacting the monomer with an agent capable of catalyzing the polymerization of the monomer into a polymer; and placing the reaction mixture under conditions that result in the formation of the polymer in reaction mixture.

Abstract: The present invention relates to supplementing the diets to sows during the periods of gestation, lactation, and breeding by feeding L-carnitine and chromium. The supplementation enhances pork productivity by increasing the number of pigs born alive in the subsequent reproductive cycle. Sow diets of this invention include L-carnitine and L-carnitine salts and trivalent chromium salts, such as chromium picolinate and chromium nicotinate. L-Carnitine is generally added to the swine feed formulation in the amount of from about 20 to about 1500 ppm, and the trivalent chromium salt is generally added to the swine feed formulation in the amount of from about 20 ppb to about 1000 ppb. The invention also relates to supplemented sow diets and feed supplement formulation.

Abstract: The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance (having low aqueous solubility and a substantial binding affinity to plasma proteins) and a plasma protein fraction in controlled aggregation state, whereby the said active substance and the said protein fraction are bound to each other by way of non-covalent bonds. It also covers processes for the preparation of the product and pharmaceutical formulation by dissolving the water-insoluble active substance in a water-miscible, pharmaceutically acceptable solvent, combining said solution with the aqueous solution of a plasma protein fraction in controlled aggregation state whereby a true solution is obtained containing the said active substance and the said protein fraction bound together by way of non-covalent bonds.

Abstract: The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with ?-cyclodextrin in an aqueous complexation medium comprising ?-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with ?-cyclodextrin and its inclusion complexes.

Abstract: Crosslinked compositions formed from water-insoluble copolymers are disclosed. These compositions are copolymers having a bioresorbable region, a hydrophilic region and at least two cross-linkable functional groups per polymer chain. Crosslinking of these polymers can be effected in solution in organic solvents or in solvent-free systems. If crosslinking occurs in a humid environment, a hydrogel will form. If crosslinking occurs in a non-humid environment, a xerogel will form which will form a hydrogel when exposed to a humid environment and the resulting crosslinked materials form hydrogels when exposed to humid environments. These hydrogels are useful as components in medical devices such as implantable prostheses. In addition, such hydrogels are useful as delivery vehicles for therapeutic agents and as scaffolding for tissue engineering applications.

Abstract: This invention is directed to a sustained release composition comprised of Compound (A) having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprised of poly-(I)-lactic-glycolic-tartaric acid wherein the amino group of Compound (A) is ionically bound to a carboxyl group of the copolymer and wherein further the composition may be made into a sustained release pharmaceutical composition with pharmaceutically acceptable carrier(s).

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: A substantially solid biomolecular solder for joining tissue comprising a partially denatured biomolecule. The solder can be formed into shapes to suit the needs of a user. The invention also relates to methods for joining tissue and methods for preparing the solder.

Abstract: Multiple myeloma and other hematologic tumors and/or malignancies can be treated by administration of a G1 and/or S phase drug, which is preferably ?-lapachone, or a derivative or analog thereof, combined with a G2/M phase drug such as a taxane derivative, which is advantageously paclitaxel. This combination of the G1 and/or S phase drug with the G2/M phase drug results in an unexpectedly greater than additive (i.e., synergistic) apoptosis in multiple myeloma cells. The invention includes methods of treating multiple myeloma by administering the combination of the G1 and/or S phase drug and the G2/M phase drug, pharmaceutical compositions comprising the combination of drugs used in these methods, as well as pharmaceutical kits.

Abstract: Provided is a pharmaceutical composition comprising a solution comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Also provided is a synthetic peptide-containing pharmaceutical composition as a unit dose comprising an aqueous formulation comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Further provided is a method of treating HIV infection by administering to an HIV-infected individual a pharmaceutical composition according to the present invention.

Abstract: A method of protecting a chemical compound from degradation comprising combining the chemical compound with an amino acid polymer. Disclosed are methods of combining chemical compounds with synthetic amino acid polymers for protection from degradation of the chemical compounds and to provide for controlled release of the compounds. A method is described for the selective release of drug substances from a synthetic amino acid polymer in the stomach or small intestine, utilizing pH-dependent changes in a higher order structure. A pharmaceutical composition comprising a drug substance that has been combined with an amino acid polymer and a pharmaceutically acceptable combination of excipients is disclosed. A cell culture media comprising a polypeptide containing glutamine that has been co-polymerized with an amino acid is described.

Abstract: The invention is directed toward a formable bone composition for application to a bone defect site to promote new bone growth at the site which comprises a new bone growth inducing compound of demineralized lyophilized allograft bone particles. The particle size ranges from about 0.1 mm to about 1.0 cm and is mixed in a hydrogel carrier containing a sodium phosphate saline buffer, the hydrogel component of the carrier ranging from about 1.0 to 5.0% of the composition and a pH between 6.8–7.4 with one or more additives of a cellular material, growth factor, demineralized bone chips or mineralized bone chips.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: A preparation is provided which can be injected or implanted into the human or animal body, and which comprises, as main component, globin that is insoluble at physiological pH, biocompatible and sterile.

Abstract: Water-soluble macromers including at least one hydrolysable linkage formed from carbonate or dioxanone groups, at least one water-soluble polymeric block, and at least one polymerizable group, and methods of preparation and use thereof are described. The macromers are preferably polymerized using free radical initiators under the influence of long wavelength ultraviolet light or visible light excitation. Biodegradation occurs at the linkages within the extension oligomers and results in fragments which are non-toxic and easily removed from the body. The macromers can be used to encapsulate cells, deliver prophylactic, therapeutic or diagnostic agents in a controlled manner, plug leaks in tissue, prevent adhesion formation after surgical procedures, temporarily protect or separate tissue surfaces, and adhere or seal tissues together.