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Biocompatibile 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. The problem of large particle size, etc., achieves good biocompatibility and blood compatibility, which is beneficial to long circulation and reduces phagocytosis.

Inactive Publication Date: 2008-09-10
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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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

The invention relates to a monodisperse nano-polymer carrier with biological compatibility and a method for preparation and carrying drug thereof. Firstly, a reversible addition fragmentation chain transfer (RAFT) polymerization method is used for preparing amphiphilic block copolymers with smaller polydispersity index, wherein the hydrophilic segment is methylacryoyloxyethyl phosphorylcholine (MPC) and the hydrophobic segment is n-butyl methacrylate (BMA). Then through the method of solvent evaporation, the amphiphilic block copolymers are used for preparing nano-polymer micelle, drugs are encapsulated in the micelle through physical action, thus obtaining the monodisperse nano-polymer carrier system with good biological compatibility.

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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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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