Synergistic Combination Chemotherapy of Camptothecin and Floxuridine through Self-Assembly of Amphiphilic Drug鈥揇rug Conjugate

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• 作者：Minxi Hu ; Ping Huang ; Yao Wang ; Yue Su ; Linzhu Zhou ; Xinyuan Zhu ; Deyue Yan
• 刊名：Bioconjugate Chemistry
• 出版年：2015
• 出版时间：December 16, 2015
• 年：2015
• 卷：26
• 期：12
• 页码：2497-2506
• 全文大小：544K
• ISSN：1520-4812

文摘

Combination chemotherapy has been widely applied in cancer treatment; however, the cocktail administration of combination chemotherapy could cause the nonuniform biodistribution of anticancer agents, thus impairing the therapeutic efficacy. In the present study, to address this concern, we proposed a novel strategy of preparing self-assembled nanoparticles from amphiphilic drug鈥揹rug conjugate for synergistic combination chemotherapy. The conjugate was synthesized by two-step esterification of hydrophobic camptothecin (CPT) and hydrophilic floxuridine (FUDR) through a linker compound. Because of its amphiphilic nature, the CPT-FUDR conjugate self-assembled into stable nanoparticles which could simultaneously release fixed dosage of the two drugs in cancer cells. In vitro studies demonstrated synergistic anticancer efficacy of the CPT-FUDR nanoparticles including improved cell apoptosis, varied cell cycle arrest, as well as effective inhibition of cancer cell proliferation.