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A kind of amphiphilic block copolymer, its shell cross-linked micelles and its preparation method and application

An amphiphilic block and copolymer technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and emulsion delivery, etc., and can solve problems such as block copolymer assembly damage.

Active Publication Date: 2021-02-12
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the assembly formed by block copolymers has a lower critical micelle concentration (CMC) than small molecule surfactants and exhibits better thermodynamic stability, there are still some uncontrollable factors that may It will lead to the destruction and dissociation of block copolymer assemblies, such as temperature, concentration and solvent conditions, etc. (Elsabahy M, Heo G S, LimSM, Chemical revlews, 2015, 115(19): 10967-11011)

Method used

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  • A kind of amphiphilic block copolymer, its shell cross-linked micelles and its preparation method and application
  • A kind of amphiphilic block copolymer, its shell cross-linked micelles and its preparation method and application
  • A kind of amphiphilic block copolymer, its shell cross-linked micelles and its preparation method and application

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preparation example 1

[0107] The first step is to prepare ABEMA with aldehyde functional groups:

[0108]

[0109] Its characteristics are: the monomer can be well copolymerized with the hydrophilic monomer oligoethylene glycol methacrylate to obtain a hydrophilic segment, and the side group of the monomer contains an aldehyde functional group, which can be combined with The shell cross-linking agent 9,10-aminoethoxyanthracene undergoes a cross-linking reaction, and finally a shell-cross-linked nanomicelle assembly is obtained.

[0110] Preparation:

[0111] Dissolve 2.44g of 4-hydroxybenzaldehyde (Chinese medicine) in 50mL of acetone, then add potassium carbonate (4.146g, 30mmol, Chinese medicine) and bromoethanol (3.75g, 30mmol, Chinese medicine) to the system, and reflux overnight. Then filter to remove inorganic salts and remove acetone by rotary evaporation, then extract after dissolving with dichloromethane, keep the organic phase, remove dichloromethane by rotary evaporation, and finally...

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Abstract

The invention provides an amphiphilic block copolymer, a polymer nanoshell cross-linked micelle composed of it, a preparation method and application thereof. The amphiphilic block copolymer is obtained by reversible addition-fragmentation chain transfer (RAFT) polymerization from a hydrophilic segment and a hydrophobic segment exhibiting hydrophobic properties in neutral and alkaline environments, wherein the hydrophilic segment The segment is obtained by copolymerization of oligoethylene glycol methacrylate and methacrylate compound with aldehyde functional group for shell crosslinking, and its molecular weight is 5000-10000Da. The present invention realizes the controlled release of hydrophobic drugs loaded on polymer nanoshell cross-linked micellar carriers, and at the same time the amphiphilic block copolymer covalently bonds photosensitizers with red light emission and aldehydes for shell cross-linking The base functional group cooperates with the hydrophobic chain segment that exhibits hydrophobic characteristics in neutral and alkaline environments, and can accurately realize the controlled release of drugs in a weak acid microenvironment and under the excitation of red light irradiation.

Description

technical field [0001] The invention belongs to the field of polymer material and its preparation and application. Specifically, it relates to a stimuli-responsive amphiphilic block copolymer, a polymer nanomicelle composed of the amphiphilic block copolymer, and a preparation method and application thereof. Background technique [0002] The use of supramolecular assemblies to simulate cell structures to achieve highly biomimetic structures and functions has always attracted people's attention, especially the use of nano-assemblies of amphiphilic block copolymers to achieve drug delivery in human lesions. However, although the assembly formed by block copolymers has a lower critical micelle concentration (CMC) than small molecule surfactants and exhibits better thermodynamic stability, there are still some uncontrollable factors that may It will lead to the destruction and dissociation of block copolymer assemblies, such as temperature, concentration and solvent conditions ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F2/38C08F2/50A61K9/107A61K47/32
CPCA61K9/1075A61K47/32C08F2/38C08F2/50C08F293/005C08F2438/03
Inventor 张国颖吴学刘固寰
Owner UNIV OF SCI & TECH OF CHINA
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