Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: Disclosed are methods for isolating polymerase complexes from a mixture of polymerase complex components. The polymerase complexes can comprise a nanopore to provide isolated nanopore sequencing complexes. The methods relate to the positive and negative isolation of the polymerase complexes and/or nanopore sequencing complexes. Also disclosed is a nucleic acid adaptor for isolating active polymerase complexes, polymerase complexes comprising the nucleic acid adaptor, and methods for isolating active polymerase complexes using the nucleic acid adaptor.

Abstract: Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

Abstract: Polycationic polymeric antimicrobial surfactant and polymeric biocompatible antimicrobial surfactant compositions are useful in dispersing various compounds in a carrier liquid. The polycationic polymeric antimicrobial surfactant and polymeric biocompatible antimicrobial surfactant compositions employ polymers having both hydrophilic domains and hydrophobic domains so that the compositions can disperse particles such as polymer particles or droplets in a continuous phase as well as provide stable dispersions that have not been provided before. The antimicrobial properties of the compositions provide much-needed capabilities of fighting infectious agents such as bacteria and viruses in a wide spectrum of products such as paint, adhesives, and coatings. Methods of using these compositions as well as methods of making products using the compositions are disclosed.

Abstract: Being used for drug modification, the multi-arm single molecular weight polyethylene glycol and an active derivative thereof provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the active derivative of the multi-arm single molecular weight polyethylene glycol provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.

Abstract: Provided herein are polymers, pH-sensitive polymers and/or linkers; conjugates comprising said polymers and/or linkers, optionally, coupled to one or more agents and/or targeting moieties; and particles (e.g., nanoparticles comprising the aforesaid polymers, linkers and/or conjugates), which can be used to enhance the delivery and/or efficacy of one or more agents in a subject.

Abstract: Hypotonic formulations of hydrogel forming polymers, preferably poloxamers, have been developed for enhanced delivery through mucosa of therapeutic, diagnostic, prophylactic or other agents, to epithelial tissues, especially those having a mucosal coating. The polymers are administered at a concentration above, at or less than their critical gelling concentration (CRC) under isotonic conditions. The hypo tonicity of the formulation is adjusted so that the polymer gels at the lower concentration. A Poloxamer gel administered into the vagina or colorectal at its CRC will form a “plug” of gel in the lumen.

Abstract: Disclose herein are dosing regimens for targeted NaPi2b antibody-drug conjugates for treating cancer.

Abstract: Defined multi-conjugate oligonucleotides can have predetermined sizes and compositions. For example, in various embodiment, defined multi-conjugate oligonucleotides can have advantageous properties, for example in the form of defined multi-conjugate siRNA (i.e., including two, three or more siRNA) having enhanced intracellular delivery and/or multi-gene silencing effects. In various embodiment, the defined multi-conjugate oligonucleotides can be synthesized via new synthetic intermediates and methods. The defined multi-conjugate oligonucleotides can be used, for example, in reducing gene expression, biological research, treating or preventing medical conditions, or to produce new or altered phenotypes in cells or organisms.

Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: The subject disclosure is directed to techniques for enhancing the selectivity and efficacy of therapeutic polymers against a broad spectrum of pathogens and cancer cell lines. According to an embodiment, a method is provided that comprises forming a therapeutic polymer based on polymerization of a plurality of therapeutic monomers, wherein the therapeutic polymer provides a therapeutic functionality. The method further comprises attaching biotin to the therapeutic polymer, resulting in a biotin-functionalized therapeutic polymer, wherein the biotin-functionalized therapeutic polymer provides greater therapeutic efficacy relative to the therapeutic polymer.

Abstract: The present invention provides a polymer having antimicrobial and/or antifouling (protein-repellent) properties, a monomer that can be used in a method of producing the polymer of the invention, and a use of the polymer of the invention, including a method for coating the surface of a material, substrate or product with the polymer of the invention, as well as to products comprising the polymer of the invention and/or a coating comprising the polymer of the invention.

Abstract: The present disclosure provides click-crosslinked hydrogels and methods of use.

Abstract: The present invention relates to a polymeric nanoparticle conjugate of formula (I). The present invention also relates to pharmaceutical compositions including these polymeric nanoparticle conjugates, and methods of preparation and use thereof.

Abstract: The present invention relates to the use of uncrosslinked copolymers having a backbone comprising i) a plurality of thermo-responsive structural units derived from one or more than one N-alkyl or N,N-dialkyl substituted (alkyl)acrylamide monomer and ii) a plurality of hydrophilic structural units derived from one or more than one second ethylenically unsaturated monomer as excipients in solid mixtures with poorly water-soluble substances for effective solubilization of the latter in aqueous media. Solid dosage forms comprising a solid mixture of such copolymer(s) and poorly water-soluble substance(s) are also within the scope of the invention.

Abstract: Fumaric acid or a salt thereof, such as a fumaryl halide (e.g. fumaryl chloride), which contains unsaturated carbon-carbon double bonds that can be used for in situ crosslinking, is copolymerized with poly(caprolactone) diol in the presence of an alkali metal salt. The resulting photocrosslinkable biocompatible and bioresorbable poly(caprolactone fumarate) biomaterial is useful in the fabrication of injectable an in-situ hardening scaffolds for application in skeletal reconstruction.

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: Hypotonic formulations of hydrogel forming polymers, preferably poloxamers, have been developed for enhanced delivery through mucosa of therapeutic, diagnostic, prophylactic or other agents, to epithelial tissues, especially those having a mucosal coating. The polymers are administered at a concentration above, at or less than their critical gelling concentration (CGC) under isotonic conditions. The hypotonicity of the formulation is adjusted so that the polymer gels at the lower concentration. A Poloxamer gel administered into the vagina or colorectum at its CGC will form a “plug” of gel in the lumen.

Abstract: Embodiments of the invention are directed to a macromolecular chemotherapeutic. A non-limiting example of the macromolecular chemotherapeutic includes a block copolymer. The block copolymer can include a water-soluble block, a cationic block, and a linker, wherein the linker is connected to the water-soluble bock and the charged block.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.

Abstract: Photodynamic therapy of tumors such as bladder tumors includes photosensitizing with a photosensitizer that is a complex or a compound of hypericin and a polymeric complexing agent. The photosensitizer is formed from an alkali salt of hypericin and the polymeric complexing agent. The alkali salt of hypericin is a sodium salt or a potassium salt. The complexing agent is a polyethylene glycol or a poly-N-vinyl amide.

Abstract: A tobacco lozenge provided herein includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and tobacco plant tissue dispersed in the soluble-fiber matrix. In some cases, a tobacco lozenge provided herein includes at least 40 weight percent of soluble fiber. In some cases, soluble fiber in tobacco lozenge provided herein can include maltodextrin. The tobacco lozenge is adapted to release the tobacco plant tissue from the body when the body is received within the oral cavity of an adult tobacco consumer and exposed to saliva. A method of making tobacco lozenges provided herein includes forming a molten mixture of at least 40 weight percent soluble fiber, tobacco, and less than 15 weight percent water, while maintaining a mixture temperature of less than 200° C. and portioning the molten mixture into a plurality of tobacco lozenges. In some cases, the ingredients can be mixed to form the molten mixture in an extruder.

Abstract: An antibacterial spectacle part comprises a spectacle part, and a film formed on at least one surface of the spectacle part. The film is formed by a self-polymerization reaction of dopamine, and comprises a plurality of silver nano particles deposited on a surface of the film away from the spectacle part. The disclosure also provides an antibacterial treatment method.

Abstract: The present invention relates to polyethylene glycol (PEG) modified protein drugs, and a PEGylated tissue kallikrein, a preparation method and use thereof are disclosed. The tissue kallikrein has a sequence as shown in SEQ ID No. 1 or SEQ ID No. 2, and the tissue kallikrein may be natural or recombinant. The PEG has a molecular weight of 20 to 40 kDa, and is conjugated to the N-terminal primary amino of the tissue kallikrein. In addition to the advantages of significantly extended half-life, significantly reduced immunogenicity and stable and uniform structure, the biological activity of the PEGylated KLK1 provided in the present invention is improved to a higher extent, which is more significant in the treatment of cerebral apoplexy and diabetic nephropathy in particular.

Abstract: Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.

Abstract: Methods of treating subjects having a disease or disorder responsive to IL-10, including methods of administration and dosing regimens associated therewith, are provided.

Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.

Abstract: The present invention relates to methods and other technologies that may be used to determine whether compositions (e.g., pharmaceutical compositions) comprising interleukin-10 molecules (e.g., pegylated interleukin-10) meet particular product-related specifications prior to being administered to a subject for the treatment and/or prevention of the diseases, disorders and conditions, and/or the symptoms thereof, described herein.

Abstract: The present invention relates to an amphiphilic polymer which includes a large amount of hydrophilic structures and hydrophobic structures, and thereby effectively stabilizing a membrane protein having a hydrophobic surface in an aqueous solution. A method of preparing an amphiphilic polymer represented by Formula 1 includes reacting a poly-gamma-glutamic acid with a reaction product of a fluorescent dye, biotin, an alkyl carboxylic acid having 1 to 10 carbon atoms or a cycloalkyl carboxylic acid having 5 to 20 carbon atoms having a carboxyl group, and dicyclo-hexylcarbodiimide (DCC) and reacting the poly-gamma-glutamic acid with DCC after reacting the poly-gamma-glutamic acid with the reaction product, and reacting the poly-gamma-glutamic acid with a hydrophilic amine and a hydrophobic amine.

Abstract: In the early detection of cancer, in particular bladder cancer, a photodynamic diagnosis uses, as a photosensitizer, a formulation that contains sodium hypericinate that is bonded to polyvinylpyrrolidone or complexed with polyvinylpyrrolidone.

Abstract: There is provided a conjugate of a delivery agent containing a chemical moiety and at least one flavonoid. The flavonoid exists in a monomeric form or dimeric form before conjugation and remains in the monomeric form or dimeric form after conjugation. Preferably, the conjugate comprises two flavonoids. The delivery agent is conjugated at the C6 and/or the C8 position of the A ring of the flavonoid. An anti-cancer agent delivery vehicle comprising an anti-cancer agent and the conjugate is also provided.

Abstract: The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics.

Abstract: Provided is a capsule having a shell of material that is a supramolecular cross-linked network. The network is formed from a host-guest complexation of cucurbituril (the host) and one or more building blocks comprising suitable guest functionality. The complex non-covalently crosslinks the building block and/or non-covalently links the building block to another building block thereby forming the supramolecular cross-linked network. The capsules are obtained or obtainable by the complexation of a composition comprising cucurbituril and one or more building blocks having suitable cucurbituril guest functionality thereby to form a supramolecular cross-linked network.

Abstract: The present invention discloses a biocarrier for delivery of a bioactive substance near/into a target cell, comprising a bioactive substance-loaded core with a first electricity, and one or more block copolymer, each block copolymer comprising a zwitterionic block and an anchoring block with an initial electricity opposite to the first electricity, wherein the anchoring block binds to the core by electrostatic attraction, and the zwitterionic block extends outwardly to increase the biocarrier stability in mammalian blood. Additionally, the present invention also discloses a method of using the biocarrier.

Abstract: The present invention relates to substrates comprising covalently attached antimicrobial polymers, which act as synthetic mimics of antimicrobial peptides (SMAMPs) and are preferably obtained by ring opening metathesis polymerization (ROMP). The inventive antimicrobial polymers exhibit a molecular weight of more than 100,000 g mol?1 and are preferably covalently attached to the surface of a substrate, e.g. an implant, a medical device, medical equipment or a (tissue-supporting) biomaterial, etc. Covalent bonding may be carried out using a photoreactive crosslinker but also by “grafting onto” or “grafting from”. The present invention is also directed to uses of the inventive antimicrobial polymers as defined herein, e.g. for antimicrobially coating a surface of such a substrate with a layer of the inventive antimicrobial polymer.

Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.

Abstract: There is provided a delivery vehicle comprising an anti-cancer agent together with a conjugate of a delivery agent containing a free aldehyde and a flavonoid, having the delivery agent conjugated at the C6 and/or the C8 position of the A ring of the flavonoid. The resulting delivery vehicles may be used to deliver an anti-cancer agent to a cell.

Abstract: The present invention features, inter alia, constructs for the delivery of therapeutic and diagnostic agents to a patient. The constructs can include a nanoparticle, a targeting agent that specifically binds a targeted tissue or cell, a therapeutic moiety, and a hydrogel. The constructs can be used in the treatment and diagnosis of bowel diseases, including inflammatory bowel disease (IBD) and colon cancer. In one embodiment, the therapeutic agent is a nucleic acid that mediates RNA inhibition (RNAi), and the invention is directed to treatments for IBD that combine the positive aspects of such agents {e.g., siRNAs) with the safety of a biodegradable polymeric delivery system to facilitate specific targeting of colonic tissues and cells. As the constructs can be formulated for oral administration, they are well tolerated and offer advantages with regard to patient compliance.

Abstract: A consumable film adapted to adhere and to dissolve in the oral cavity that provides a local anesthetic and therapeutic agents for the treatment of oral burns or injuries. The film is designed to instantly release benzocaine, or other types of local anesthetic or therapeutic agent, upon adhesion to the affected areas of the mouth, and will continue to release sufficient quantities for pain relief and for healing over an extended period of time.

Abstract: Described herein are MetAP-2 inhibitors and compositions and formulations thereof, and more particularly compositions and formulations of MetAP-2 inhibitors wherein the MetAP-2 inhibitor is associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety. The present invention also relates to compositions and formulations comprising MetAP-2 inhibitors for oral administration or administration via routes such as topical or ocular administration. The present invention also provides methods to treat conditions associated with or related to the over-expression or over-activity of MetAP-2 by administering the compositions and formulations comprising MetAP-2 inhibitors as disclosed herein.

Abstract: A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

Abstract: Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.

Abstract: Catechol-bearing polycarbonates (catechol polymers) were prepared comprising i) a catechol repeat unit comprising a side chain catechol group, ii) a cationic repeat unit comprising a side chain cationic group selected from the group consisting of quaternary amine groups, quaternary phosphine groups, and combinations thereof, and iii) a PEG repeat unit comprising a side chain poly(ethylene oxide) group having a degree of polymerization of about 5 to about 30. The catechol polymers form antimicrobial and antifouling films on a variety of substrate surfaces, in particular silicone rubber.

Abstract: The present disclosure provides injectable synthetic and biodegradable polymeric biomaterials that effectively prevent seroma, a common postoperative complication following ablative and reconstructive surgeries. Provided biomaterials include physically crosslinked hydrogels that are thixotropic, display rapid chain relaxation, are easily extruded through narrow gauge needles, biodegrade into inert products, are well tolerated by soft tissues, and effectively prevent seroma in a radical breast mastectomy animal model.

Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

Abstract: This present invention relates generally to the use of novel formulations comprising a surface active polymer to enhance oxygenation in skin and other soft tissue. The present invention also discloses formulations that can be used to improve clinical outlook and reducing bacteria. Methods of making and using the same are also disclosed.

Abstract: The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.

Abstract: Disclosed herein are an in situ-forming, bioadhesive hydrogel and the medical uses thereof. Being formed by in situ crosslinking through an enzymatic reaction, the hydrogel has an advantage over conventional bioadhesive hydrogels in terms of biocompatibility. In addition, the in situ-forming bioadhesive hydrogel has excellent biocompatibility and mechanical strength and has excellent tissue adhesiveness thanks to modification with/without dopa derivatives. The hydrogel finds a variety of applications in the biomedical field, including bioadhesives or hemostats, implant substances for tissue regeneration and augmentation, carriers for delivering biologically active materials or drugs, etc.