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

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

Inactive Publication Date: 2010-11-24
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
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Effect test

Embodiment 1

[0071] (1) Synthesis of P(MMA-co-tBMA)-Br macromolecular initiator (A:B=50:50, A represents the hydrophobic group MMA, B represents the pH-responsive group tBMA, the ratio is the mass percentage, the same below ). Take a 50ml dry reaction flask and put it into a stirrer. Weigh CuBr (143.5 mg) into a reaction flask, then seal it with a reverse rubber stopper, and vacuum-purge with argon three times. Monomer MMA (3181 μl), tBMA (5072 μl), and ligand PMDETA (209 μl) were sequentially added to the reaction flask by syringe, and the catalyst complex was formed by stirring for 10 minutes. After three cycles of freezing-pumping-heating with liquid nitrogen, the mixture was transferred to a 90°C oil bath under argon protection and stirred for 15 minutes, and then the initiator EBriB (147 μl) was rapidly added dropwise with a syringe. React in a 90°C oil bath for 30 minutes. After the reaction was completed, it was cooled to room temperature, 20 ml of tetrahydrofuran was added and s...

Embodiment 2

[0075] (1) Synthesis of P(BA-co-tBMA)-Br macroinitiator (A:B=40:60). Take a 50ml dry reaction flask and put it into a stirrer. Weigh CuBr (143.5 mg) into a reaction flask, then seal it with a reverse rubber stopper, and vacuum-purge with argon three times. Monomer BA (2237 μl) and tBMA (5072 μl), and ligand PMDETA (209 μl) were added to the vial sequentially by syringe and stirred for 10 minutes to allow the formation of the catalyst complex. After three cycles of freezing-pumping-heating with liquid nitrogen, the mixture was transferred to a 90°C oil bath under argon protection and stirred for 15 minutes, and then the initiator EBriB (147 μl) was rapidly added dropwise with a syringe. React in a 90°C oil bath for 30 minutes. After the reaction was completed, it was cooled to room temperature, 20 ml of tetrahydrofuran was added and stirred to dissolve, and then the catalyst was removed by filtration through a neutral alumina column (using tetrahydrofuran as the eluent). The...

Embodiment 3

[0079] (1) Synthesis of P(BMA-co-tBMA)-Br macroinitiator (A:B=60:40). Take a 50ml dry reaction flask and put it into a stirrer. Weigh CuBr (143.5 mg) into a reaction flask, seal it with a rubber stopper, and evacuate-argon for three times. Monomer BMA (6710 μl) and tBMA (6760 μl), and ligand PMDETA (209 μl) were added to the vial sequentially by syringe and stirred for 10 minutes to allow the formation of the catalyst complex. After three cycles of freezing-pumping-heating with liquid nitrogen, the mixture was transferred to a 90°C oil bath under argon protection and stirred for 15 minutes, and then the initiator EBriB (147 μl) was rapidly added dropwise with a syringe. React in a 90°C oil bath for 45 minutes. After the reaction was completed, it was cooled to room temperature, 50 ml of tetrahydrofuran was added and stirred to dissolve, and then the catalyst was removed by filtration through a neutral alumina column (using tetrahydrofuran as the eluent). The resulting solut...

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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 present invention relates to the field of high molecular polymer materials for medicine, in particular to an amphiphilic copolymer brush with pH responsiveness, a preparation method and application thereof. Background technique [0002] Polymer 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 small particle size and large surface area / volume ratio, which can avoid the phagocytosis of the reticuloendothelial system (RES) in vivo or be absorbed by tissues such as liver and spleen. It is beneficial to prolong the circulation of micelles in blood and passive accumulation in tumor tissue. At the same time, it also has its unique advantages in reducing drug toxicity and increasing solubility. Polymer micelles have lower critical micelle concentration, larger solubilization space, and stable structure. According to th...

Claims

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Application Information

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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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