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Bio-compatible monodisperse nano polymer carrier and its preparation and medicine-carrying method

A nano-polymer, biocompatible technology, used in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc. It can achieve good biocompatibility and hemocompatibility, facilitate long circulation, and reduce phagocytosis.

Inactive Publication Date: 2009-12-02
SOUTHEAST UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Many antineoplastic drugs (such as paclitaxel, doxorubicin, methotrexate, etc.) have very low solubility in water, and they also have strong toxic and side effects. Therefore, the direct use of such antineoplastic drugs has very low efficacy. and cause greater harm to the human body
In order to solubilize hydrophobic drugs and achieve drug sustained release, researchers have extensively studied many drug delivery systems, such as liposomes, microspheres, surfactant micelles, etc., but these systems still have many shortcomings, such as: lipid Surfactants and microspheres have large particle sizes and are easily phagocytosed by the human reticuloendothelial system (RES); surfactant micelles have a high critical micelle concentration (CMC) and lack good anti-dilution properties, etc.

Method used

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  • Bio-compatible monodisperse nano polymer carrier and its preparation and medicine-carrying method

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Embodiment Construction

[0041] In the invention, the amphiphilic block copolymer with small molecular weight distribution and good biocompatibility is firstly prepared by RAFT polymerization method. Wherein the hydrophilic block is polymethacryloyloxyethyl phosphorylcholine, and the hydrophobic block is poly-n-butyl methacrylate. A solvent evaporation method is used to prepare an aqueous solution of polymer micelles by using the above block copolymer. Hydrophobic drugs can be physically encapsulated in the hydrophobic core of the micelle during micelle formation.

[0042] 1: Preparation of PBMA 80 macromolecular chain transfer agent

[0043] Add 14.200 g (100 mmol) of n-butyl methacrylate, 279 mg (1.0 mmol) of tetracyanovaleric acid dithiobenzoate, and 4,4'-azobis(4-cyanovaleric acid) into the three-necked flask successively. ) 56mg (0.2mmol) and ethanol 50ml. Bubble high-purity nitrogen for 30 minutes to remove the oxygen in the solvent. After vacuuming and flushing nitrogen three times, place t...

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Abstract

Biocompatible monodisperse nanopolymer carrier and methods for its preparation and drug loading. First, an amphiphilic block copolymer with a small molecular weight distribution index was prepared by reversible addition-fragmentation chain transfer (RAFT) polymerization, in which the hydrophilic segment was methacryloyloxyethylphosphorylcholine (MPC ), and the hydrophobic segment is n-butyl methacrylate (BMA). Then, the above-mentioned amphiphilic block copolymer is used to prepare nanometer polymer micelles by a solvent evaporation method, and drugs are encapsulated in the micelles by physical action to obtain a monodisperse nanometer polymer drug-carrying system with good biocompatibility.

Description

technical field [0001] The invention relates to a biocompatible monodisperse nanometer polymer drug-carrying system and a preparation method thereof, belonging to the technical field of pharmaceutical engineering. Background technique [0002] Many antineoplastic drugs (such as paclitaxel, doxorubicin, methotrexate, etc.) have very low solubility in water, and they also have strong toxic and side effects. Therefore, the direct use of such antineoplastic drugs has very low efficacy. and cause greater harm to the human body. In order to solubilize hydrophobic drugs and achieve drug sustained release, researchers have extensively studied many drug delivery systems, such as liposomes, microspheres, surfactant micelles, etc., but these systems still have many shortcomings, such as: lipid Surfactants and microspheres have large particle sizes and are easily phagocytosed by the human reticuloendothelial system (RES); surfactant micelles have a high critical micelle concentration (...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/32A61K9/107C08F293/00A61K31/337A61K31/704A61K31/519A61P35/00C08F230/06C08F220/18
Inventor 陈志明焦真褚洪雨刘娜邵利
Owner SOUTHEAST UNIV
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