Cationic Vesicles Based on Amphiphilic Pillar[5]arene Capped with Ferrocenium: A Redox-Responsive System for Drug/siRNA Co-Delivery
Cationic Vesicles Based on Amphiphilic Pillar[5]arene Capped with Ferrocenium: A Redox-Responsive System for Drug/siRNA Co-Delivery
复制标题
基于二茂铁封端的两亲柱[5]芳烃的阳离子囊泡：用于药物/siRNA 共递送的氧化还原响应系统
DOI：
10.1002/anie.201407272
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发表时间：
2014-11-24
影响因子：
16.6
通讯作者：
Pei, Zhichao
中科院分区：
文献类型：
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作者：
Chang, Yincheng;Yang, Kui;Pei, Zhichao
合成了一种新型的二茂铁包覆两亲性柱[5]芳烃（FCAP），并在水溶液中自组装成阳离子囊泡。由于二茂铁阳离子和二茂铁基之间的氧化还原平衡，阳离子囊泡具有低细胞毒性和显著的氧化还原反应行为，可以构建理想的谷胱甘肽（GSH）反应性药物/siRNA共递送系统，用于在GSH浓度较高的癌细胞中快速释放药物和基因转染。这是首次报道由柱状芳烃组装的氧化还原反应囊泡用于药物/siRNA共递送；除了提高药物对癌细胞的生物利用度和减少对正常细胞的不良副作用外，这些系统还可以克服癌细胞的耐药性。这项工作为有效的刺激反应性药物/siRNA共递送系统的合理设计提供了一个很好的例子。
A novel ferrocenium capped amphiphilic pillar[5]arene (FCAP) was synthesized and self-assembled to cationic vesicles in aqueous solution. The cationic vesicles, displaying low cytotoxicity and significant redox-responsive behavior due to the redox equilibrium between ferrocenium cations and ferrocenyl groups, allow building an ideal glutathione (GSH)-responsive drug/siRNA co-delivery system for rapid drug release and gene transfection in cancer cells in which higher GSH concentration exists. This is the first report of redox-responsive vesicles assembled from pillararenes for drug/siRNA co-delivery; besides enhancing the bioavailability of drugs for cancer cells and reducing the adverse side effects for normal cells, these systems can also overcome the drug resistance of cancer cells. This work presents a good example of rational design for an effective stimuli-responsive drug/siRNA co-delivery system.