Amphiphilic copolymer brush with pH responsiveness, preparation method thereof and use thereof

An amphiphilic copolymer and responsive technology, applied in the field of medical polymer materials, can solve the problem that the cycle time and stability of the drug-carrying system cannot be guaranteed, the controlled release cannot be effectively achieved, and the response is not accurate and sensitive. and other problems, to achieve the effects of excellent product quality, increased density, and improved controlled release performance.

Inactive Publication Date: 2012-08-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Judging from the existing research reports, the polymer micelle drug-loading system currently used in the oral system of poorly soluble drugs faces two main problems: one is that the excessively high critical micelle concentration (CMC) makes the drug-loading system circulate in vivo Time and stability are not guaranteed; the second is that there is a certain spatial distance between the drug-loaded layer and the pH-responsive layer, which makes the pH response-micelle swelling-drug release process of the micelles slow, so the response to environmental pH changes is not accurate enough and sensitive
The residence time of drug-loaded micelles in the human body is usually less than 10 hours (Journal of Controlled Release, 2008, 132: 222; International Journal of Pharmaceuticals, 2005, 302: 125), so drug-loaded micelles have not had time to release or completely The drug contained in it has been excreted by the internal circulation after release, and the purpose of controlled release cannot be effectively achieved

Method used

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  • Amphiphilic copolymer brush with pH responsiveness, preparation method thereof and use thereof
  • Amphiphilic copolymer brush with pH responsiveness, preparation method thereof and use thereof
  • Amphiphilic copolymer brush with pH responsiveness, preparation method thereof and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] (1) Synthesis of P(MMA-co-tBMA)-Br macroinitiator (A: B=50:50, A represents the hydrophobic group MMA, B represents the pH response group tBMA, the ratio is mass percent, the same below ). Take a 50ml dry reaction bottle and put it into a stirring bar. Weigh CuBr (143.5 mg) and place it in a reaction bottle, then seal it with a back-mouth rubber stopper, and vacuumize and pass argon three times. The monomers MMA (3181 μl) and tBMA (5072 μl), and the ligand PMDETA (209 μl) were sequentially added into the reaction vial with a syringe, and stirred for 10 minutes to form the catalyst complex. After three freezing-pumping-heating cycles with liquid nitrogen, the mixture was transferred to a 90°C oil bath under the protection of argon and stirred for 15 minutes, then the initiator EBriB (147 μl) was quickly added dropwise with a syringe. React in an oil bath at 90°C for 30 minutes. After completion of the reaction, cool to room temperature, add 20ml of tetrahydrofuran and...

Embodiment 2

[0075] (1) Synthesis of P(BA-co-tBMA)-Br macroinitiator (A:B=40:60). Take a 50ml dry reaction bottle and put it into a stirring bar. Weigh CuBr (143.5 mg) and place it in a reaction bottle, then seal it with a back-mouth rubber stopper, and vacuumize and pass argon three times. Monomer BA (2237 μl) and tBMA (5072 μl), and ligand PMDETA (209 μl) were sequentially added to the vial by syringe, and stirred for 10 minutes to form the catalyst complex. After three freezing-pumping-heating cycles with liquid nitrogen, the mixture was transferred to a 90°C oil bath under the protection of argon and stirred for 15 minutes, then the initiator EBriB (147 μl) was quickly added dropwise with a syringe. React in an oil bath at 90°C for 30 minutes. After completion of the reaction, cool to room temperature, add 20ml of tetrahydrofuran and stir to make it dissolve, and then remove the catalyst by filtering through a neutral alumina column (using tetrahydrofuran as eluent). The resulting s...

Embodiment 3

[0079] (1) Synthesis of P(BMA-co-tBMA)-Br macroinitiator (A:B=60:40). Take a 50ml dry reaction bottle and put it into a stirring bar. Weigh CuBr (143.5mg) and place it in a reaction bottle, then seal it with a back-mouthed rubber stopper, vacuumize and pass argon three times. The monomeric BMA (6710 μl) and tBMA (6760 μl), and the ligand PMDETA (209 μl) were sequentially added into the vial with a syringe, and stirred for 10 minutes to form the catalyst complex. After three freezing-pumping-heating cycles with liquid nitrogen, the mixture was transferred to a 90°C oil bath under the protection of argon and stirred for 15 minutes, then the initiator EBriB (147 μl) was quickly added dropwise with a syringe. React in 90°C oil bath for 45 minutes. After the reaction was completed, cool to room temperature, add 50ml of tetrahydrofuran and stir to make it dissolve, and then remove the catalyst by filtering through a neutral alumina column (using tetrahydrofuran as eluent). The re...

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Abstract

The invention discloses an amphiphilic copolymer brush with pH responsiveness and a preparation method thereof. Particularly, the invention discloses an amphiphilic copolymer brush with pH responsiveness comprised of a block, which is formed by the copolymerization of a hydrophobic group and a pH response group, and a hydrophilic brush-shaped block. In the invention, a copolymer of a hydrophobic monomer and a pH response functional monomer is obtained by atom transfer radical polymerization (ATRP), then the copolymer is used as a macromolecular initiator to perform the ATRP polymerization of monomethoxypoly (ethylene glycol) methacrylate (PEGMA) which is a hydrophilic macromolecular monomer, and finally, a selective hydrolysis reaction is performed to prepare the amphiphilic copolymer brush with pH responsiveness. The preparation method of the invention has the advantages of simple process and high yield. The synthesized amphiphilic copolymer brush with pH responsiveness has a novel structure and an adjustable functional group proportion, and is suitable to be used in the transmission of entrapped insoluble medicaments.

Description

technical field [0001] The invention relates to the field of high-molecular polymer materials for medical use, in particular, the invention relates to a pH-responsive amphiphilic copolymer brush and its preparation method and application. Background technique [0002] Polymeric micelles are generally spherical nanoparticles with a core / shell structure assembled from amphiphilic polymers in a solvent. As a typical nano drug delivery system, polymer micelles have a small particle size and a large surface area / volume ratio, which can avoid phagocytosis by the reticuloendothelial system (RES) or absorption by tissues such as liver and spleen in vivo, which is beneficial. It is beneficial to prolong the circulation of micelles in the blood and the passive accumulation in tumor tissues. At the same time, it also has its unique advantages in reducing drug toxicity and increasing solubility. Polymer micelles have a low critical micelle concentration, large space for solubilization...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F220/28C08F220/18C08F220/14C08F8/00A61K47/32
Inventor 章莉娟钱宇杨友强陈赟郑灵珊
Owner SOUTH CHINA UNIV OF TECH
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