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Preparation method and application of polymeric micelle with triple responsiveness

A technology of polymer glue and amphiphilic polymer, which is applied in the field of preparation of triple responsive polymer micelles, and achieves the effect of broad application prospects

Inactive Publication Date: 2012-11-07
UNIV OF SCI & TECH BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] There are still some problems in the application of micelles in the controlled release of drugs, such as the biocompatibility and biodegradability of polymer molecules used to make micelles, the stability of micelles in vivo, the drug-loading ability of micelles, Some issues such as release efficiency need to be studied, so more and better molecules need to be developed to make micelles that meet the requirements
[0003] In addition, most of the current micelles are single-responsive, such as sensitive to pH, temperature, ionic strength, light, ultrasound, etc., and the environment in which the micelles are applied is complex and changeable. In many cases, single-responsive micelles It is difficult to meet the needs, which limits its application, and the multi-responsive micelles can play a better role in controlling release

Method used

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  • Preparation method and application of polymeric micelle with triple responsiveness
  • Preparation method and application of polymeric micelle with triple responsiveness
  • Preparation method and application of polymeric micelle with triple responsiveness

Examples

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example 1

[0030] Preparation of polydimethylaminoethyl methacrylate: the polymerizable monomer is dimethylaminoethyl methacrylate, the initiator is ethyl α-bromoisobutyrate, and the molar ratio of the polymerizable monomer to the initiator is 50 1. Reflux in tetrahydrofuran for 12 hours. After the reaction, the product is precipitated twice in n-hexane ， The solid was dried in a vacuum oven for 24 hours to obtain polydimethylaminoethyl methacrylate as a white solid powder.

[0031] Preparation of pyrene methyl bromide: using pyrene methanol and phosphorus tribromide as raw materials, the molar ratio is 2 to 1, using chloroform as solvent, reacting under ice-water bath conditions for 24 hours, adding saturated sodium bicarbonate solution after the reaction and stirring until the solution The layers were separated and the solution in the lower layer was neutral, and the organic phase in the lower layer was separated with a separatory funnel, rotary evaporated, and recrystallized to obtain...

Embodiment 2

[0035] Preparation of polydimethylaminoethyl methacrylate: the polymerizable monomer is dimethylaminoethyl methacrylate, the initiator is ethyl α-bromoisobutyrate, and the molar ratio of the polymerizable monomer to the initiator is 50 1. Reflux in tetrahydrofuran for 12 hours. After the reaction, the product is precipitated twice in n-hexane ， The solid was dried in a vacuum oven for 24 hours to obtain polydimethylaminoethyl methacrylate as a white solid powder.

[0036] (1) Preparation of pyrene methyl bromide: use pyrene methanol and phosphorus tribromide as raw materials, the molar ratio is 2:1, and chloroform is used as solvent, and react under ice-water bath conditions for 24 hours. After the reaction is completed, add saturated sodium bicarbonate solution and stir , until the solution was separated into layers and the lower layer solution was neutral, the lower organic phase was separated with a separatory funnel, rotary evaporated, and recrystallized to obtain pure pyr...

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Abstract

The invention relates to a preparation method and application of a polymeric micelle with triple responsiveness. The method comprises the following steps of: performing atom transfer radical polymerization on a polymerizable monomer dimethylaminoethyl methacrylate to obtain dimethylaminoethyl polymethacrylate, preparing pyrene methobromide from pyrene methanol and phosphorus tribromide, and grafting the pyrene methobromide to the dimethylaminoethyl polymethacrylate through quaterisation reaction to obtain the micelle with light, temperature and pH responsiveness. The polymeric micelle is stable at room temperature and can be loaded with hydrophobic molecules such as Nile red, the shape of the micelle is changed by ultraviolet irradiation and temperature and pH value regulation, and the loaded molecules are released from the micelle. The polymeric micelle has pH, temperature and light responsiveness and can have a wide application prospect in the field of medicine controlled release.

Description

technical field [0001] The invention belongs to the technical field of polymer materials, and relates to a preparation method and application of triple-responsive polymer micelles responsive to light, temperature and pH. Background technique [0002] There are still some problems in the application of micelles in the controlled release of drugs, such as the biocompatibility and biodegradability of polymer molecules used to make micelles, the stability of micelles in vivo, the drug-loading ability of micelles, Some issues such as release efficiency need to be studied, so more and better molecules need to be developed to make micelles that meet the requirements. [0003] In addition, most of the current micelles are single-responsive, such as sensitive to pH, temperature, ionic strength, light, ultrasound, etc., and the environment in which the micelles are applied is complex and changeable. In many cases, single-responsive micelles It is difficult to meet the needs, which li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F120/34C08F8/44C08J3/09C08J3/03A61K9/00A61K47/32
Inventor 王国杰董杰张瑞辰杨槐
Owner UNIV OF SCI & TECH BEIJING
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