Phenylboronic Acid-Based Complex Micelles with Enhanced Glucose-Responsiveness at Physiological pH by Complexation with Glycopolymer
Phenylboronic Acid-Based Complex Micelles with Enhanced Glucose-Responsiveness at Physiological pH by Complexation with Glycopolymer
复制标题
通过与糖聚合物络合增强生理 pH 下葡萄糖响应性的基于苯基硼酸的复合胶束
DOI：
10.1021/bm3012715
复制
发表时间：
2012-10-01
影响因子：
6.2
通讯作者：
Shi, Linqi
中科院分区：
文献类型：
--
作者：
Ma, Rujiang;Yang, Hao;Shi, Linqi
在生理条件下具有葡萄糖响应性的聚合物纳米粒在开发用于治疗糖尿病的药物递送系统方面具有极大的兴趣。本文基于苯基硼酸与糖基之间的共价络合作用，将含苯基硼酸的嵌段共聚物PEG-b-P（AA-co-APBA）和含糖共聚物P（AA-co-阿加）自组装成具有葡萄糖响应性的复合胶束。通过核磁共振氢谱（HNMR）分析证实了以P（AA-co-APBA）/P（AA-co-阿加）为核、PEG为壳的复合胶束的形成。通过测定胶束溶液的光散射强度和荧光强度，研究了复合胶束的葡萄糖响应性。与单纯PEG-b-P（AA-co-APBA）胶束相比，复合胶束对葡萄糖的敏感性增强，且复合胶束对葡萄糖的敏感性随P（AA-co-阿加）含量的减少而增加。MTT法测定了聚合物及其复合胶束的细胞毒性。这种复合胶束可能是一种很好的胰岛素载体，并可能在糖尿病的治疗中得到应用。
Polymeric nanoparticles with glucose-responsiveness under physiological conditions are of great interests in developing drug delivery system for the treatment of diabetes. Herein, glucose-responsive complex micelles were prepared by self-assembly of a phenylboronic acid-contained block copolymer PEG-b-P(AA-co-APBA) and a glycopolymer P(AA-co-AGA) based on the covalent complexation between phenylboronic acid and glycosyl. The formation of the complex micelles with a P(AA-co-APBA)/P(AA-co-AGA) core and a PEG shell was confirmed by HNMR analysis. The glucose-responsiveness of the complex micelles was investigated by monitoring the light scattering intensity and the fluorescence (ARS) of the micelle solutions. The complex micelles displayed an enhanced glucose-responsiveness compared to the simple PEG-b-P(AA-co-APBA) micelles and the sensitivity of the complex micelles to glucose increased with the decrease of the amount of P(AA-co-AGA) in the compositions. The cytotoxicity of the polymers and the complex micelles was also evaluated by MTT assay. This kind of complex micelles may be an excellent candidate for insulin delivery and may find application in the treatment of diabetes.