Patent classifications
A61K9/1273
NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF
Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises
##STR00001##
wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.
LIPID ANALOGS AND LIPOSOMES COMPRISING SAME
A polymeric compound is disclosed herein, having the general formula I:
##STR00001##
wherein m, n, X, Y, Z and L are as defined herein. Further disclosed herein are lipid bilayers comprising at least one bilayer-forming lipid and the aforementioned polymeric compound, and liposomes comprising such a bilayer, as well as methods, uses and compositions utilizing such bilayers and/or liposomes for reducing a friction coefficient of a surface and/or for inhibiting biofilm formation.
NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF
Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises
##STR00001##
wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.
DRUG FORMULATIONS FOR CANCER TREATMENT
Compounds and pharmaceutical formulations containing these compounds are described. Also described are methods of making and using the compounds. The compounds include nucleobases, nucleobase analogues, or combinations thereof. In one embodiment, a nucleobase analogue is combined with doxorubicin and encapsulated within a liposome for use in inhibiting or preventing the growth of cancer cells. Further described are pharmaceutical compositions containing two or more therapeutically active agents encapsulated within a vesicle, such as a liposome, wherein the molar ratio of the agents provides a synergistic therapeutic effect.
TRANSMEMBRANE PH-GRADIENT POLYMERSOMES FOR THE QUANTIFICATION OF AMMONIA IN BODY FLUIDS
The present invention provides polymersomes comprising amphiphilic block-copolymers and their use to quantify ammonia in samples (e.g., body fluid samples). More particularly, it provides a polymersome comprising (a) a membrane, which comprises a block copolymer of poly(styrene) (PS) and poly(ethylene oxide) (PEO), wherein the PS/PEO molecular weight ratio is higher than 1.0 and lower than 4.0; and (b) a core which encloses an acid and at least one pH-sensitive dye. Compositions, strips and kits comprising the polymersomes are also provided along with methods of quantifying ammonia in a sample using the polymersomes, compositions and kit.
Biodegradable amphiphilic polymer, polymeric vesicles prepared therefrom, and application of biodegradable amphiphilic polymer in preparation of medicines for targeted therapy of lung cancer
Disclosed in the present disclosure is a biodegradable amphiphilic polymer containing disulfide in the side chain, a self-crosslinked polymeric vesicle thereof and an application in the targeted therapy of lung cancer. The polymer is obtained by an activity-controllable ring-opening polymerization based on a cyclic carbonate monomer containing a functional group of dithiolane ring, which has a controllable molecular weight and a narrow molecular weight distribution, and does not require processes of protection and deprotection; the polymer obtained by the ring-opening polymerization of the cyclic carbonate monomer of the present disclosure has biodegradability and can be used to control the drug release system, the prepared lung cancer-targeted reduction-sensitive reversibly-crosslinked polymeric vesicle as a nanomedicine carrier supports stable long circulation in vivo. However, it is highly enriched in lung cancer tissues, enter cells efficiently, and rapidly decrosslinks in the cells to release drugs, so as to kill cancer cells with high potency and specificity and inhibit the growth of tumor effectively without causing toxic and side effects.
FUNCTIONALIZED LIPOSOMES FOR IMAGING MISFOLDED PROTEINS
Phospholipid-polymer-aromatic conjugates comprising binding ligands, liposome compositions including the phospholipid-polymer-aromatic conjugates, and binding ligands having an affinity for misfolded proteins are described. The phospholipid-polymer-aromatic conjugate may be represented by Structural Formula I: PL-AL-HP-X-BL (I). In Formula I, PL is a phospholipid, AL is an aliphatic linkage, HP is hydrophilic polymer, X is a link between the phospholipid-polymer and the binding ligand, and BL is polycyclic aromatic compound that functions as a binding ligand. The liposomal compositions may be useful for the imaging of misfolded and/or aggregated proteins.
Amphiphilic molecules layers
The disclosure relates to a layer comprising at least one hydrophilic part and at least one hydrophobic part, the layer comprising self-assembled amphiphilic molecules polymerized with each other on both the hydrophilic part and the hydrophobic part of the layer; a detecting device comprising a substrate and the above-mentioned layer; and a liposome, a micelle, transport system for a substance and a biomimetic system comprising the above-mentioned layer. The disclosure also relates to a process for producing a layer, the process comprising: providing amphiphilic molecules; allowing sufficient time for the amphiphilic molecules to self-assemble and form at least one hydrophilic part and at least one hydrophobic part of the layer; polymerizing the self-assembled amphiphilic molecules with each other on both the hydrophilic part and the hydrophobic part of the layer.
Facile Assembly of Soft Nanoarchitectures and Co-Loading of Hydrophilic and Hydrophobic Molecules via Flash Nanoprecipitation
Described herein are flash nanoprecipitation methods capable of encapsulating hydrophobic molecules, hydrophilic molecules, bioactive protein therapeutics, or other target molecules in amphiphilic copolymer nanocarriers.
Brush-poly (glycoamidoamine)-lipids and uses thereof
The present disclosure provides brush-poly(glycoamidoamine)-lipids (PGALs) (e.g., polymers of any one of Formulae (I)-(IV)) and methods of preparing the PGALs. A described PGAL may include poly(glycoamidoamine)-derived moieties (e.g., ##STR00001##
such as ##STR00002##
which may assist the PGAL and/or a complex of the PGAL and an agent to pass through cell membranes or be taken up by cells. Also provided are compositions including a described PGAL and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that include or involve the PGALs or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing in a subject a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, musculoskeletal diseases, genitourinary diseases, and metabolic disorders ##STR00003##