Smart nanocarriers for pH-triggered targeting and release of hydrophobic drugs
Smart nanocarriers for pH-triggered targeting and release of hydrophobic drugs
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DOI：
10.1016/j.actbio.2012.08.049
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发表时间：
2012-12-01
影响因子：
9.7
通讯作者：
Jerome, C.
中科院分区：
文献类型：
--
作者：
Cajot, S.;Van Butsele, K.;Jerome, C.
研究了以（PEO）（129）（P2 VP）（43）（PCL）（17）ABC杂臂星星共聚物为主体的pH敏感性杂化胶束作为潜在触发给药系统的应用。在此考虑该星星共聚物与在pH敏感性嵌段（聚-2-乙烯基吡啶）上由靶向配体（即生物素）标记的第二共聚物的共胶束化，以赋予肿瘤细胞的可能的活性靶向。研究了这些标记的共聚物的两种结构，即杂臂星星或线性ABC胶束，并在细胞毒性（细胞活力）和细胞摄取（使用荧光染料加载的胶束）方面比较了相应的杂化胶束。最后，通过一方面研究内化后的溶酶体完整性，另一方面研究随pH变化的释放曲线，研究了肿瘤细胞胞质溶胶中的触发药物释放。由爱思唯尔有限公司出版。保留所有权利。
The use of hybrid pH-sensitive micelles based mainly on the (PEO)(129)(P2VP)(43)(PCL)(17) ABC miktoarm star copolymer as potential triggered drug delivery systems was investigated. Co-micellization of this star copolymer with a second copolymer labeled by a targeting ligand, i.e. biotin, on the pH sensitive block (poly-2-vinylpyridine) is considered here in order to impart possible active targeting of the tumor cells. Two architectures were studied for these labeled copolymers, i.e. a miktoarm star or a linear ABC terpolymer, and the respective hybrid micelles are compared in terms of cytotoxicity (cells viability) and cellular uptake (using fluorescent dye loaded micelles). Finally, the triggered drug release in the cytosol of tumor cells was investigated by studying, on the one hand, the lysosomal integrity after internalization and, on the other hand, the release profile in function of the pH. (c) 2012 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.