pH/Reductant Dual-Responsive Core-Cross-Linked Micelles via Facile in Situ ATRP for Tumor-Targeted Delivery of Anticancer Drug with Enhanced Anticancer Efficiency

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• 作者：Kun Tian ; Xu Jia ; Xubo Zhao ; Peng Liu
• 刊名：Molecular Pharmaceutics
• 出版年：2016
• 出版时间：August 1, 2016
• 年：2016
• 卷：13
• 期：8
• 页码：2683-2690
• 全文大小：454K
• 年卷期：0
• ISSN：1543-8392

文摘

Anticancer drugs cause severe side effects on normal tissues and organs due to their nonspecific delivery. Thus, tumor-targeting delivery of anticancer drugs remains a serious challenge in chemotherapy. Here a facile strategy was established for the pH/reductant dual-responsive core-cross-linked (CCL) micelles for tumor-targeted delivery of anticancer drug, via in situ atom transfer radical polymerization (ATRP). In the in vitro controlled release experiments with doxorubicin (DOX) as a model drug, the premature drug leakage rate was only 13.4% in the physiological medium within 36 h, while the cumulative release rate in the stimulated tumor microenvironment reached 78.7%, demonstrating the excellent tumor microenvironment responsive controlled release behavior upon acidic medium with high GSH level. As a folate receptor (FR) mediated targeting drug delivery system (DDS), the micelles showed excellent cytocompatibility, and enhanced anticancer efficiency after loading of DOX, compared with free DOX.