614 results about "Polymeric micelles" patented technology

The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.

Provided are a delivery system that is useful in delivering a double-stranded ribonucleic acid that functions in gene silencing in glomeruli, particularly in mesangial cells and the like, to the tissue or cells, and the like. A polyion complex in the form of a non-polymeric micelle consisting of a double-stranded ribonucleic acid and a block copolymer represented by the formula (I) or (II) below, which are electrostatically bound together, wherein the polyion complex has an average particle diameter of less than 100 nm as measured by a dynamic light scattering measuring method:wherein each symbol is as defined in the specification.

Novel polymeric micelles which are used to deliver therapeutic agents, including anti tumor drugs.

A production method of a preparation containing drug-encapsulating polymer micelles is provided, which comprises dissolving a hydrophilic-hydrophobic block copolymer and a sparingly water-soluble drug in a volatile organic solvent, then removing the solvent, and stirring the residue with water at a temperature not higher than 30° C. to dissolve the drug-encapsulating polymer micelles into the water.

A biodegradable, mixed polymeric micelle used to deliver a selected nucleic acid into a targeted host cell contains an amphiphilic polyester-polycation copolymer and an amphiphilic polyester-sugar copolymer. The polyester-polycation copolymer forms an electrostatic interaction with polyanionic nucleic acids, and the polyester-sugar copolymer directs the micelle-nucleic acid complex to cells in vivo. Additional copolymers with similar properties may also be included. The composition improves delivery efficiency by providing a particulate gene carrier for which particle size and charge density are easily controlled by multivariate means. Various kinds of ligands and other functional compounds may be also be introduced using the composition. The composition may be used in a method for transforming a targeted host cell with a selected nucleic acid.

A composition for the sustained delivery of a drug comprising an amphiphilic diblock copolymer; a poorly water-soluble drug; a biodegradable polymer; and liquid poly(ethylene glycol) or functional derivatives thereof and a process for preparing the composition are disclosed. When administered into a particular body site, the composition forms an implant containing the drug and drug containing polymeric micelles, which are slowly released from the implant to maintain a constant drug concentration for an extended period of time.

Complex coacervate core micelles as surface modification or surface treatment The present invention relates to devices carrying on the surface polymeric micelles and a process for the preparation thereof. It further relates to the use of polymeric micelles as a surface coating for rendering a surface anti-fouling and / or protein-resistant. The present invention relates to modified or treated surfaces carrying on polymeric micelles and a process for the preparation thereof. It further relates to the use of polymeric micelles as a surface coating for surface modification or surface treatment. The surface modification or surface treatment is for example for rendering a surface anti-fouling and / or protein-resistant, or for preventing bacteria proliferation, disinfecting, suppressing odours, preventing malodour, providing easy-cleaning or soil-release properties. These polymeric micelles are of the so-called complex coacervate core type, exhibiting a hydrophilic, neutral corona and a core, which is formed by charge complexation of oppositely charged blocks.

A photopolymerizable polymer micelle includes a spherical micelle that encapsulates a hydrophobic photopolymerization initiator, the spherical micelle being formed by a block copolymer having a hydrophilic block segment and a hydrophobic block segment, the block copolymer having a number average molecular weight exceeding 10000, and the hydrophobic block segment at least partially having a radically polymerizable group.

The present invention relates to vectorization of double stranded RNA oligonucleotides by cationic particles chosen from among surfactant micelles, block or non-block polymer micelles, cationic liposomes and niosomes, cationic oleosomes and cationic nanoemulsions, as well as from among cationic organic or inorganic particles and nanocapsules, and topical compositions for the skin, mucous membranes or eyes.

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

The invention relates to a polymer micelle medicine carrying system using an amino acid as a stabilizing agent and a preparation method thereof, wherein the medicine carrying system can be used as a medicament carrier composition, and the medicament carrier composition comprises an amphipathic segmented copolymer and amino acid, wherein the amphipathic segmented copolymer comprises a diblock copolymer and a triblock copolymer, the amino acid is selected from 20 kinds of common amino acid, and the mixture ratio (w / w) of the amphipathic segmented copolymer to the amino acid is 100 / 0.01-1.00 / 99.99.

The invention relates to polymeric micelle medicine carrying system taking amino acid as stabilizing agent and a preparation method thereof. The medicine carrying system can be acted as a medicine carrying composition which is composed of amphipathy block copolymer and amino acid; wherein the amphipathy block copolymer comprises diblock copolymer and triblock copolymer, amino acid is selected from twenty common amino acids, the ratio (w / w) of amphipathy block copolymer and amino acid is 100-1.00: 0.01-99.9.

The invention relates to a polymeric micellar structure which comprising an ionic porphyrin dendrimer represented by general formula (1): q(c)PM (where q represents the number of charged atoms on the periphery of the dendrimer; c represents a negative (−) or positive (+) charge; and PM is represented by the following general formula (2): wherein M represents two hydrogen atoms or a metal atom, R1, R2, R3 and R4 are the same or different and represents hydrogen or identical or different aryl ether dendrosubunits, provided that at least one of R1, R2, R3 and R4 represent an aryl ether dendrosubunits and that each aryl ether dendrosubunit has an anionic or cationic group at the end optionally though a spacer molecule chain.

Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of making poly(L-histidine), synthetic intermediates, and block copolymers are also described.

The invention provides block polymers, micelles, and micelle formulations for combination drug therapy. Polyamide block polymers, such as those of formulas I and II are useful, for example, for preparation of mixed drug micelles, including simply mixed micelles, physically mixed micelles, and chemically mixed micelles. The invention further provides methods of treating cancer, and inhibiting and killing cancer cells. Also provided are methods for the preparation of polymer drug conjugates and intermediates for their synthesis.

Compositions comprising a heterogeneous polymeric micelle and an agent (e.g., a polynucleotide) associated with the micelle are disclosed, together with methods for intracellular delivery of such agent.

The present invention relates to a biocompatible and thermosensitive poly(ethylene glycol) / polyester block copolymer and a method of its preparation thereof, and particularly to a multi-functional intelligent hydrogel polymer comprising a hydrophilic part of a poly(ethylene glycol) (PEG) having a low molecular weight and a hydrophobic part comprising an ester-based caprolactone (CL) segment as an essential ingredient and further comprising a para-dioxanone (PDO) segment, a trimethylene carbonate (TMC) segment or a PDO / TMC copolymer containing the PDO and the TMC segments in a predetermined ratio, which easily forms a desired-shaped gel and decomposes or disperses without necessitating the operation process for removing the gel due to the temperature-dependent phase transition caused by the coagulation and the expansion of polymer micelles comprising a hydrophilic part and a hydrophobic part, thus being applicable to a drug delivery system or a porous support for tissue engineering purpose.

The invention relates to a folate-targeted reduction sensitive drug-carrying polymer nano-micelle as well as a preparation method and application thereof. The delivery carrier is prepared by taking anamphiphilic triblock copolymer PCL-ss-PEG-ss-PCL as a material, and a chemotherapeutic drug adriamycin amycin and a photosensitizer indocyanine green are entrapped in a hydrophobic core of the micelle. Besides, phospholipid DSPE-PEG-NH2 with an active group is introduced into the preparation process, the DSPE end of the phospholipid has strong hydrophobic property and is inserted into the hydrophobic PCL core of the polymer micelle, the flexible hydrophilic PEG long chain exists on the outer surface of the micelle, FA with a targeting effect is connected to a PEG active distal end of the surface of the polymer micelle, and functions of active tumor targeting and reduction response drug release are integrated. The folate-targeted reduction sensitive drug-carrying polymer nano-micelle disclosed by the invention has the advantages of being small in particle size, high in dispersion property, high in drug loading capacity and encapsulation efficiency and excellent in photothermal conversion effect, can realize reduced trigger drug release, fluorescence imaging of tumor sites, tumor targeting drug delivery and chemotherapy-photothermal combination therapy and improve the tumor inhibition effect, and has wide application prospects in the targeted combination therapy aspect of tumors.

The invention relates to a preparation method of a nanometer graphene oxide carrier for the photodynamic therapy. The method is characterized in that: the surface of nanometer graphene oxide, which is modified by a hydrophilic polymer, loads a hydrophobic photosensitizer containing a large pi-conjugated structure through the pi-pi accumulation and the hydrophobic-hydrophobic interaction, so a product for the photodynamic therapy is obtained. Compared with the prior art, the photosensitizer loading rate of the nanometer graphene oxide carrier, which is high to 14 wt%, is higher than the photosensitizer loading rate of other photosensitizer carriers, such as a polymer micelle, a liposome, a liposome, a nanometer silicon ball and the like, so the nanometer graphene oxide carrier which can be applied to the photodynamic therapy has a good treatment effect, and has an obvious inhibitive ability on the growth of cancer cells under the irradiation of near infrared light, so a novel high efficiency loading photosensitizer system is provided for the treatment of cancers of tumors at shallow skin surfaces.

Polymeric micelles for encapsulation of hydrophobic molecules are provided. Methods and formulations for delivering hydrophobic molecules to a host via these micelles are also provided. Methods of stabilizing liposomes or lipid based formulations by addition of polymeric micelles are also provided.

The invention relates to a method for making medicinal preparation, in particular a polymer micelle drug loading system and preparation, wherein the micelle is methyl polyethylene glycol - polyester segmented copolymer micelle, characterized by that, the ratio of methyl polyethylene glycol and polyester is less than 50 / 50, and the advantages of the segmented copolymer micelle is low critical micelle concentration, high drug loading capacity and stabilized micelle.

The present invention relates to a biodegradable branched polylactic acid derivative of formula 1, and preparation method and use thereof: <formula 1> 1-(R—X)n wherein each of X, R, I and n is defined as in the detailed description.

A biocompatible stable composition containing a hydrophobic drug, such as paclitaxel. The composition, which forms a syringeable polymeric micellar solution in aqueous or body fluids, is a freeze-dried product comprising a hydrophobic drug, i.e. paclitaxel, and an amphiphilic block copolymer wherein a hydrophobic group having affinity or attraction with the hydrophobic drug, such as paclitaxel, is incorporated on its end.

A stable polymer micella carrier system for medicines is composed of an amphipathic block copolymer including diblock copolymer and triblock copolymer and a phosphatide chosen from glyceryl phosphatide, sphingomyelin, and their derivatives.

The invention relates to pH-triggering-to-release multilevel targeting polymer micelle in tumor cells and a preparation method of the multilevel targeting polymer micelle. The micelle is formed by self assembly of hydrophobic modified polysaccharide polymer with an endosome pH sensitive characteristic in a water medium. A hyaluronic acid-deoxycholate-histidine polymer is used as a carrier, and caner initiatively-targeting endosome pH sensitive polymer micelle is prepared by virtue of an ultrasonic method or a dialysis method to wrap an antitumor drug difficult to dissolve. By using the synergistic mechanism of EPR-mediated passive targeting, CD44 receptor initiative targeting and pH sensitive targeting strategies, the 'whole-course targeting' guidance is performed at four medicine delivery key steps, i.e., blood long circulation, tumor tissue accumulation, cell digestion and intracellular drug release, so that multilevel targeting drug delivery is realized, the intracellular drug concentration is effectively increased, and a novel carrier and a preparation strategy are provided for improving the antitumor effect of the difficultly-soluble antitumor drug.