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Smart nanocarriers for pH-triggered targeting and release of hydrophobic drugs

机译:用于pH触发的靶向和疏水药物释放的智能纳米载体

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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.
机译:研究了主要基于(PEO)129(P2VP)43(PCL)17 ABC miktoarm星型共聚物的混合pH敏感胶束作为潜在触发药物递送系统的用途。为了赋予肿瘤细胞可能的活性靶向,这里考虑将该星形共聚物与在pH敏感的嵌段(聚-2-乙烯基吡啶)上被靶向配体即生物素标记的第二种共聚物的共胶化。研究了这些标记共聚物的两种结构,即miktoarm star或线性ABC三元共聚物,并比较了各自的杂化胶束的细胞毒性(细胞活力)和细胞摄取(使用荧光染料负载的胶束)。最后,一方面通过研究内在化后的溶酶体完整性,另一方面通过研究pH值对释放曲线的影响,来研究肿瘤细胞在胞质溶胶中触发的药物释放。

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