Drug-induced hierarchical self-assembly of poly(amino acid) for efficient intracellular drug delivery
Drug-induced hierarchical self-assembly of poly(amino acid) for efficient intracellular drug delivery
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药物诱导的聚氨基酸分层自组装用于有效的细胞内药物递送
DOI：
10.1016/j.cclet.2020.10.016
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发表时间：
2021-04-25
影响因子：
9.1
通讯作者：
Ding, Mingming
中科院分区：
文献类型：
--
作者：
Li, Zifen;Yang, Yanxue;Ding, Mingming
藤黄酸（GA）作为一种有效的抗癌药物，其水溶性差，化学稳定性低，临床疗效有限。为了解决这个问题，我们在这里报告了一种使用可还原的二嵌段聚（氨基酸）作为模型固定和递送GA的简单有效的策略。GA和聚合物之间的静电相互作用使得高载药量含量高达53.6%。此外，药物络合诱导胶束到囊泡的转变，结合从无规卷曲到？螺旋。分级组装的药物纳米复合物可以作为一种智能载体，用于有效的细胞内化和在细胞内酸性和还原性条件下触发多种药物的释放，从而在体外产生协同抗肿瘤功效。这项工作提供了一个新的见解药物载体的相互作用和药物输送应用程序的一个简易的纳米平台。? 2020中国化学会、中国医学科学院药物研究所。Elsevier B.V.出版，保留所有权利。
As a potent anticancer drug, gambogic acid (GA) suffers from its poor water solubility and low chemical stability and shows a limited clinical outcome. To address this problem, we report here a simple and effective strategy to immobilize and deliver GA using a reducible diblock poly(amino acid) as a model. The electrostatic interaction between GA and polymer enables a high drug loading content up to 53.6%. Moreover, the drug complexation induces a micelle-to-vesicle transformation, combined with a conformation transition from random coil to ?-helix. The hierarchically assembled drug nanocomplexes can serve as a smart carrier for efficient cell internalization and triggered release of multiple drugs under intracellular acidic and reductive conditions, resulting in a synergistic antitumor efficacy in vitro. This work provides a new insight into the drug-carrier interaction and a facile nanoplatform for drug delivery applications. ? 2020 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.