Abstract: A method and related agent for detecting novel post-translational modification. This novel post-translational modification is in the form of crotonylation of lysine residues in proteins. The method includes the steps of (a) preparing a mixture of polypeptides from a protein sample; (b) separating the polypeptides by molecular weight; (c) contacting the separated polypeptides with a binding affinity reagent which binds specifically to a polypeptide containing a crotonyllysine residue; and (d) detecting presence of a binding complex between the affinity reagent and one or more of the polypeptides. An example of the binding agent is an antibody, which may be prepared from animal serums, or is a monoclonal antibody or single-chain variable fragment.

Abstract: Disclosed herein is a delivery composition for administering a hydrophobic active agent. In one embodiment, a delivery composition for local administration of a hydrophobic active agent to a tissue or organ of a patient is disclosed. In one embodiment, the delivery composition includes a cationic delivery agent, a therapeutically effective amount of a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier. In one embodiment, the cationic delivery agent includes polyethyleneimine (PEI). In a more specific embodiment, the cationic delivery agent includes branched PEI. Methods of making the delivery composition, as well as kits and methods of use are also disclosed.

Abstract: A particle includes an aqueous core; a first amphiphilic layer surrounding the aqueous core; and a polymeric matrix surrounding the first amphiphilic layer.

Abstract: The present invention is directed membrane active poly(vinyl ester) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cells in vivo. RNAi polynucleotides are conjugated to the poly(vinyl ester) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(vinyl ester) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.

Abstract: Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems.

Abstract: The invention is directed to methods and compositions for obtaining uniform sized muscle fiber fragments for transplantation. These muscle fiber fragments are able to reconstitute into long fibers that are oriented along native muscle. The implanted muscle cells integrate with native vascular and neural network, as confirmed by histology and immunohistochemistry. This invention is particularly advantageous because autologous muscle can be harvested from a donor site, processed and injected into target sites in the operating room. The fragmented muscle fibers can be readily integrated within the host.

Abstract: The present invention provides stable pharmaceutical compositions of poorly water soluble pharmaceutical agents and stabilizing agents which function to increase stability of the compositions. The use of stabilizing agents provide extended stability of nanoparticle suspensions and other formulations of poorly water soluble pharmaceutical agents such as docetaxel under certain conditions, for example upon dilution for administration.

Abstract: The present invention relates to an injection solution for intra-articular administration for treating arthritic disorders comprising a cross-linked hyaluronic acid derivative wherein part of functional groups of a hyaluronic acid are cross-linked with a cross-linking group to the extent of 0.6 to 15% of cross-linking extent as an active ingredient in an amount having a long-lasting analgesic effect and a pharmaceutically acceptable carrier, and an analgesic composition for suppressing a cartilage degeneration caused by arthritic disorders or a composition for suppressing a cartilage degeneration or an inflammation of synovium caused by arthritic disorders each comprising the cross-linked hyaluronic acid derivative and a pharmaceutically acceptable carrier.

Abstract: The invention contemplates a copolymer which is a graft or block copolymer useful to change wettability and surface characteristics of biological surfaces. Methods for use of these formulations and coatings to change wettability and sterically stabilize, and lubricate biological surfaces in a subject, for example, in the treatment of dry eye syndrome, and to prevent adherence of unwanted proteins, for example in the treatment of contact lens intolerance, are provided.

Abstract: The present invention relates to a water-in-oil emulsified skin cosmetic comprising the following ingredients (a) through (e): (a) Water: 5-50 wt % (b) Ethanol: 1-20 wt % (c) Volatile oil component: 2-50 wt % (d) Carboxy decyl trisiloxane represented by the following formula (1): 0.1-5 wt % (e) One, two or more selected from a group consisting of hydrophobized titanium dioxide, hydrophobized zinc oxide, and hydrophobized iron oxide: 2-50 wt %; wherein the object of the present invention is to provide a water-in-oil emulsified skin cosmetic containing the aforementioned powder (e) wherein powdery squeakiness over time after application on the skin is suppressed and at the same time absorption into the skin at the time of application and the absence of stickiness after application on the skin are improved.

Abstract: Pharmaceutical compositions for and methods of treating an animal, including a human, and methods of preparing such compositions. The pharmaceutical compositions contain crosslinked amine polymers and may be used, for example, to treat diseases or other metabolic conditions in which removal of protons and/or chloride ions from the gastrointestinal tract would provide physiological benefits such as normalizing serum bicarbonate concentrations and the blood pH in an animal, including a human.

Abstract: A hydrogel formulation of oxidized dextrin is reticulated with adipic acid dihydrazide, which may embody polysaccharides, proteins, nanogels, granular materials, bioactive molecules and cells for tissue regeneration and controlled drug delivery. A hydrogel can be injectable, highly biocompatible and biodegradable, for tissue regenerative applications, performing simultaneously as a vehicle e.g. for nanogels, granular materials and cells, and as controlled drug delivery systems, e.g. of hydrophobic molecules and therapeutic proteins.

Abstract: Fulvestrant formulations suitable for intramuscular injection at concentration in excess of 40 mg/ml in the absence of castor oil and castor oil derivatives are disclosed.

Abstract: The present application discloses a nanoparticle comprising compounds of the formula A-B-C(-D), wherein A designates an anchoring moiety having self-organizing properties in relation to the nanoparticle; B designates a cleavable linker; C designates an anionic moiety having a net charge of at least ?2 at pH 6.0; and D, which is optional, designates a polymer moiety which induces long circulating properties of the nanoparticle in mammalian tissue; and wherein the average net charge of the compounds is at least ?1 at pH 6.0. The application also discloses the individual compounds of the formula A-B-C(-D) as well as a drug delivery system comprising the self-organized nanoparticle having included in the interior thereof one or more pharmaceutically active agents and/or diagnostically relevant species, and a method of treating a cancerous or inflammatory condition in a mammal, involving the administration of the drug delivery system to the mammal.

Abstract: A method for immobilizing dyes and antimicrobial agents on a polymeric cover or housing for a medical device is disclosed and described. The surface may be that of a catheter, a connector, a drug vial spike, a bag spike, a prosthetic device, an endoscope, a surface of an infusion pump, a key pad, a touch screen or a handle. The surfaces may also be one or more of those associated with a infusion of a medicament or dialysis treatment, such as peritoneal dialysis or hemodialysis, where it is important that the working surface for the dialysis fluid be sterile. These surfaces include connectors for peritoneal dialysis sets or for hemodialysis sets, bag spikes, dialysis catheters, and so forth. A method for determining whether a surface has been sterilized, and a dye useful in so indicating, is also disclosed.

Abstract: The present invention is directed membrane active poly(vinyl ester) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cells in vivo. RNAi polynucleotides are conjugated to the poly(vinyl ester) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(vinyl ester) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.

Abstract: A diesel oxidation catalyst (DOC) catalytic converter for at least the conversion of carbon monoxide and hydrocarbons, removal of a fraction of particulate matter, and decrease of sulfur trioxide emissions within exhaust gases from an engine and consequently of sulfuric acid, is disclosed. The DOC may include any suitable configuration including at least a substrate and a washcoat, where the substrate has a plurality of channels, suitable porosity, offers a three-dimensional support for the washcoat, and is made of any suitable material. The washcoat may be deposited on the substrate by any suitable method, and may include a mixture of at least one or more carrier material oxides and one or more catalysts. Suitable materials for the carrier material oxides may include titanium dioxide, tin dioxide, and zirconium dioxide, among others, excluding aluminum oxide (Al2O3), which may serve for a decrease of sulfur trioxide emissions and consequently of sulfuric acid mist.

Abstract: A compound is provided that is useful for, among other things, preparing water-soluble polymer derivatives bearing a terminal N-succinimidyl ester.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.

Abstract: Antimicrobial quaternized polyurethane materials and methods of forming and using the materials are disclosed. The quaternized polyurethane antimicrobial materials may be synthesized from one or more diisocyanates and one or more diols or triols. The quaternized polyurethane materials may be stand alone or coated onto other surfaces, such as medical devices, table tops, air/water filters, or the like to provided desired antimicrobial devices and surfaces.

Abstract: A nanoformulation that includes nanoparticles. Each nanoparticle includes a shell in which a glycosaminoglycan (GAG is encapsulated. The GAG is ionically or covalently bonded to the shell. The GAG is selected from the group consisting of sulfated non-anticoagulant heparin (SNACH), super-sulfated non-anticoagulant heparin (S-SNACH), and a combination thereof. The shell includes Poly (lactic-co-glycolic acid) (PLGA), Polyethylene Glycol (PEG)-PLGA, maleimide-PEG-PLGA, chitosan, chitosan-PLGA, methoxy-polyethyleneglycol-poly (lactide-co-glycolide) (MPEG-PLGA)-(maleimide-PEG-PLGA), PLGA-Polycaprolate, or calcium alginate. A method of using the nanoformulation to treat a cancer in a subject includes administering to the patient a therapeutically effective amount of the nanoformulation for treating the cancer.

Abstract: Methods and compositions are provided that load and encapsulate an agent, such as a protein, in a porous self-healing polymer. A delivery system includes a porous self-healing polymer, an ionic affinity trap within the pores of the self-healing polymer, and an agent associated with the ionic affinity trap. Methods of encapsulating an agent in a polymer include providing a porous self-healing polymer comprising an ionic affinity trap within the pores. The polymer is incubated with an agent having an affinity for the ionic affinity trap. At least a portion of the pores in the polymer are then healed. Active encapsulation of macromolecules at low concentrations may be achieved due to affinity of the agent for the ionic affinity trap within the pores.

Abstract: The present invention relates to dendrimer compositions configured for treating inflammatory disorders and autoimmune disorders, and related methods of synthesis. Specifically, the present invention relates to methods for treating rheumatoid arthritis with PAMAM dendrimers having functional ligands configured for treating rheumatoid arthritis (e.g., therapeutic agents, pro-drugs, targeting agents, trigger agents, imaging agents) (e.g., methotrexate).

Abstract: The invention relates to nitric oxide-releasing compositions comprising polyacrylonitrile polymers that are diazeniumdiolated, and to medical devices comprising such compositions, as well as to methods of making and using the compositions and medical devices.

Abstract: Compositions and methods of using the compositions are provided for forming an embolus within a region of an anatomical lumen for a transitory period in order to achieve a therapeutic effect.

Abstract: The present invention is directed to a composition for treating vaginal dryness and lack of lubrication comprising: a poloxamer component; a phospholipid component; an optional oil component; and a non-aqueous carrier; wherein the composition is substantially anhydrous. In another aspect, the present invention is directed to a method of treating vaginal dryness comprising the step of administering to a patient suffering from vaginal dryness the above composition.

Abstract: Surgical adhesives that include a blend of two different thermoreversible gelling polymers and a crosslinking agent are described. The first thermoreversible gelling polymer is partially or fully acrylated and the second thermoreversible gelling polymer includes dual functionality including acrylate functionality and amine-reactive functionality. The adhesives can provide gelling and covalent crosslinking within the polymers of the adhesive as well as crosslinking with surrounding tissue.

Abstract: Polymers and compositions utilizing such polymers are disclosed for treating hyperphosphatemia and other illnesses associated with elevated serum phosphate levels. Phosphate binding polymers, or a pharmaceutically acceptable salt of the polymers, comprise pendent groups extending from a backbone of the polymer. Each pendent group comprises at least two nitrogen-bearing functional groups which bind phosphate. Variations of such polymer and compositions are disclosed.

Abstract: A method of covalently bonding a cyclic nitroxide radical compound to a hydrophobic block of a specific hydrophylic-phobic block copolymer, and polymerized cyclic nitroxide radical compound copolymerized in this manner, as well as use of such a compound, for instance, in the medical field are provided. The compound demonstrates long term stability in vivo under reductive environment.

Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: Elastogenic nanoparticles including a polymeric core having a surface that is functionalized with a cationic amphiphilic compound, and comprising an active agent having pro-elastogenic and/or anti-proteolytic activity, are described herein. The elastogenic nanoparticles can be used in method of stimulating elastogenesis in a subject by administering to the subject a therapeutically effective amount of elastogenic nanoparticles.

Abstract: The present disclosure is directed generally to gold/lanthanide nanoparticle conjugates, such as gold/gadolinium nanoparticle conjugates, nanoparticle conjugates including polymers, nanoparticle conjugates conjugated to targeting agents and therapeutic agents, and their use in targeting, treating, and/or imaging disease states in a patient.

Abstract: The present invention provides a method for preparing a material in the form of liquid for forming an antimicrobial surface coating with multi-level antimicrobial properties, comprising: encapsulating one or more volatile or gaseous biocides in two or more amphiphilic block copolymers to obtain a w/o/w double emulsion, and mixing the w/o/w double emulsion with one or more nonvolatile biocides, each of which is selected from the group consisting of a metal containing biocide, triclosan, a carboxylic acid, a sugar acid and a combination thereof.

Abstract: Carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle and related compositions, methods and systems.

Abstract: Methods for making biomaterials for use as a tissue sealant, kits containing precursors for forming the biomaterials, and the resulting biomaterials are described herein. The biomaterials are formed from a composition comprising at least a first and a second precursor molecule, wherein: i) the first precursor molecule is a poly(ethylene glycol) based polymer having x nucleophilic groups selected from the group consisting of thiol or amino groups, wherein x is greater than or equal to 2 ii) the second precursor molecule is of the general formula: A-[(C3H6O)n—(C2H4O)m—B]i wherein m and n are integers from 1 to 200 i is greater than 2 A is a branch point B is a conjugated unsaturated group The precursors are selected based on the desired properties of the biomaterial. Optionally, the biomaterials contain additives, such as thixotropic agents, radiopaque agents, or bioactive agents.

Abstract: Methods for constructing tyrosine-derived biotinylated polymers. Biotinylated polymers and polymer scaffolds constructed with the biotinylated polymers are also disclosed.

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: The present disclosure relates to amphiphilic compounds, self assembling compositions formed from the amphiphilic compounds and methods of making such compositions.

Abstract: Formulations of drugs and crystalline side chain polymers to provide controlled and/or sustained release drug formulations.

Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ?5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of an active compound having the chemical structure: where n=1-4 and X is selected from the group consisting of hydrogen, lithium sodium, potassium, rubidium, cesium and francium.

Abstract: The present invention is directed membrane active poly(vinyl ester) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cells in vivo. RNAi polynucleotides are conjugated to the poly(vinyl ester) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(vinyl ester) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.

Abstract: This invention discloses a surface anti-biomolecule agent for an artificially or naturally charged substrate. The anti-biomolecule agent comprises a copolymer employing anchoring blocks or domains to binds sites of the substrate via electrostatic attractive force, and employing zwitterionic blocks or domains extended outwardly to reduce the attachment of biomolecules to the substrate.

Abstract: The present invention relates to an anti-adhesion polymer composition capable of supporting growth factor, which effectively exhibits anti-adhesion function and, at the same time, has an excellent adhesive property so as to be able to easily and continuously adhere to a wound site, has antibacterial and hemostatic properties, and is composed of an injectable formulation suitable for use in minimally invasive surgery, laparoscopic surgery or the like. The anti-adhesion polymer composition capable of supporting growth factor comprises: 24-50 wt % of a polyethyleneglycol-polypropyleneglycol-polyethyleneglycol (PEG-PPG-PEG) block copolymer having a polyethyleneglycol (PEG) content of 65-85 wt % and a molecular weight of 6,000-20,000 Da; 0.03-5 wt % of gelatin; 0.03-5 wt % of chitosan; and distilled water.

Abstract: A therapeutic agent delivery system formed of a specific type of poly(ester amide) (PEA), a therapeutic agent, and a water miscible solvent is described herein. A method of delivering the therapeutic agent delivery system by delivering the therapeutic agent delivery system formed of a PEA polymer, a therapeutic agent, and a water miscible solvent to a physiological environment and separating the phase of the therapeutic agent delivery system to form a membrane from the polymer to contain the therapeutic agent within the physiological environment is also described. Additionally disclosed is a kit including a syringe and a therapeutic agent delivery system within the syringe.

Abstract: The present invention relates to a process for the preparation of polymer conjugates of indolocarbaxole compounds, in particular of polymer conjugates of K-252a and derivatives thereof, by a synthetic route which results in a highly pure product, with a high product yield. In a further aspect the present invention relates to novel polymer conjugates of K-252a and derivatives thereof, wherein the chemical group linking the polymer unity to the K-252a or to the K-252a derivative compound is characterized by a 5-member oxazolidindionic cyclic structure. These novel polymer conjugates are obtained through the novel synthetic route with high purity and high yields.

Abstract: The present invention relates to compositions and methods by which surface modification techniques can be used to modify wide range polymeric or metal substrates using metal nanoparticles.

Abstract: Disclosed is a water-soluble high-molecular weight conjugate of physiologically active substances which enable medicament to release without depending on the enzymes in a living body and which is expected to have a useful therapeutic effect. A high-molecular weight conjugate of a physiologically active substance has a substituent group represented by a general formula (1) bonded to a side-chain carboxy group of a block copolymer which has a polyethylene glycol moiety and either a polyaspartic acid moiety or a polyglutamic acid moiety.

Abstract: A series of peptides with divergent confirmations including structures of formula (1A), (1B), (2) and (3) are provided. In the formula, wherein U, G, A, B, R1, R2 and T are as defined in the specification. The divergent peptides disclosed in the present invention are characterized in a mineral binding affinity function.

Abstract: A pharmaceutical composition or combination drug, which contains, as active ingredients, (a) a coordination compound composed of a block copolymer represented by the following formula I or formula II and cisplatin, and (b) gemcitabine hydrochloride. In the formulae I and II, R1, A, R2, R3, m and n are as defined in the description.