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聚(γ-谷氨酸)-接枝-聚(L-丙交酯)胶束的制备、表征及其细胞摄取

The preparation and characterization of micelles from poly(γ-glutamic acid)-graft-poly(L-lactide) and the cellular uptake thereof.

作者信息

Liu Meiqing, Huang Gang, Cong Yingying, Tong Guoquan, Lin Zhanqiu, Yin Yihua, Zhang Chao

机构信息

School of Chemistry, Chemical Engineering and Life Sciences, Wuhan University of Technology, Wuhan, 430070, Hubei, China.

出版信息

J Mater Sci Mater Med. 2015 May;26(5):187. doi: 10.1007/s10856-015-5519-y. Epub 2015 Apr 28.

Abstract

Chemotherapy is a traditional therapeutic approach for the treatment of many solid tumors, but the poor solubility and low bioavailability of hydrophobic anti-cancer drugs greatly limit their applications. In this article, DOX-loaded micelles were fabricated based on an amphiphilic graft polymer composed of hydrophilic poly(γ-glutamic acid) (γ-PGA) and hydrophobic poly (L-lactide) (PLLA). The structure of the copolymers and the characteristic of the micelles were studied. The release profiles of doxorubicin as a model drug from the micelles were measured. Due to the protonation of the amino group of DOX and the conformational alteration of γ-PGA, the release of DOX from γ-PGA-g-PLLA micelle was faster in the acid condition, which is beneficial to tumor therapy. The cellular uptake of the DOX-loaded γ-PGA-g-PLLA micelle was proved to be a GGT-mediated process.

摘要

化疗是治疗多种实体瘤的传统方法,但疏水性抗癌药物的低溶解度和低生物利用度极大地限制了它们的应用。在本文中,基于由亲水性聚(γ-谷氨酸)(γ-PGA)和疏水性聚(L-丙交酯)(PLLA)组成的两亲性接枝聚合物制备了载有阿霉素的胶束。研究了共聚物的结构和胶束的特性。测定了作为模型药物的阿霉素从胶束中的释放曲线。由于阿霉素氨基的质子化和γ-PGA的构象改变,阿霉素从γ-PGA-g-PLLA胶束中的释放在酸性条件下更快,这有利于肿瘤治疗。载有阿霉素的γ-PGA-g-PLLA胶束的细胞摄取被证明是一个γ-谷氨酰转肽酶介导的过程。

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