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基于聚（L-组氨酸）的pH敏感胶束用于阿霉素对MCF-7/ADR细胞的细胞内递送的制备与评价

Preparation and evaluation of poly(l-histidine) based pH-sensitive micelles for intracellular delivery of doxorubicin against MCF-7/ADR cells.

作者信息

Jia Nan, Ye Yuqing, Wang Qi, Zhao Xiuli, Hu Haiyang, Chen Dawei, Qiao Mingxi

机构信息

Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.

出版信息

Asian J Pharm Sci. 2017 Sep;12(5):433-441. doi: 10.1016/j.ajps.2017.05.007. Epub 2017 May 24.

DOI:10.1016/j.ajps.2017.05.007
PMID:32104356
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7032172/
Abstract

In this study, a pH-sensitive micelle self-assembled from poly(l-histidine) based triblock copolymers of poly(ethylene glycol)-poly(d,l-lactide)-poly(l-histidine) (mPEG-PLA-PHis) was prepared and used as the intracellular doxorubicin (Dox) delivery for cancer chemotherapy. Dox was loaded into the micelles by thin-film hydration method and a Box-Behnken design for three factors at three levels was used to optimize the preparations. The optimized mPEG-PLA-Phis/Dox micelles exhibited good encapsulation efficiency of 91.12%, a mean diameter of 45 nm and narrow size distribution with polydispersity index of 0.256. drug release studies demonstrated that Dox was released from the micelles in a pH-dependent manner. Furthermore, the cellular evaluation of Dox loaded micelles displayed that the micelles possessed high antitumor activity with an IC of 35.30 µg/ml against MCF-7/ADR cells. The confocal microscopy and flow cytometry experiments indicated that mPEG-PLA-Phis micelles mediated efficient cytoplasmic delivery of Dox with the aid of poly(l-histidine) mediated endosomal escape. In addition, blank mPEG-PLA-Phis micelles were shown to be nontoxic to MCF-7/ADR cells even at a high concentration of 200 µg/ml. The pH-sensitive mPEG-PLA-PHis micelles have been demonstrated to be a promising nanosystem for the intracellular delivery of Dox for MDR reversal.

摘要

在本研究中，制备了一种由聚（乙二醇）-聚（d，l-丙交酯）-聚（l-组氨酸）（mPEG-PLA-PHis）的聚（l-组氨酸）基三嵌段共聚物自组装而成的pH敏感胶束，并将其用作癌症化疗的细胞内阿霉素（Dox）递送载体。通过薄膜水化法将Dox负载到胶束中，并采用三因素三水平的Box-Behnken设计来优化制剂。优化后的mPEG-PLA-Phis/Dox胶束表现出91.12%的良好包封率，平均直径为45nm，粒径分布窄，多分散指数为0.256。药物释放研究表明，Dox以pH依赖的方式从胶束中释放。此外，对负载Dox的胶束进行的细胞评估显示，该胶束具有高抗肿瘤活性，对MCF-7/ADR细胞的IC50为35.30μg/ml。共聚焦显微镜和流式细胞术实验表明，mPEG-PLA-Phis胶束借助聚（l-组氨酸）介导的内体逃逸介导了Dox的高效细胞质递送。此外，空白mPEG-PLA-Phis胶束即使在200μg/ml的高浓度下对MCF-7/ADR细胞也无毒。pH敏感的mPEG-PLA-PHis胶束已被证明是一种有前途的纳米系统，用于Dox的细胞内递送以逆转多药耐药性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fd/7032172/39e5bf9d5dc9/ajps445-fig-0007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fd/7032172/ce7cd3c355fe/ajps445-ga-5001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fd/7032172/1990824d50c4/ajps445-fig-0001.jpg
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