Paclitaxel–Paclitaxel Prodrug Nanoassembly as a Versatile Nanoplatform for Combinational Cancer Therapy

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• 作者：Xiangfei Han ; Jinling Chen ; Mengjuan Jiang ; Na Zhang ; Kexin Na ; Cong Luo ; Ruoshi Zhang ; Mengchi Sun ; Guimei Lin ; Rong Zhang ; Yan Ma ; Dan Liu ; Yongjun Wang
• 刊名：ACS Applied Materials & Interfaces
• 出版年：2016
• 出版时间：December 14, 2016
• 年：2016
• 卷：8
• 期：49
• 页码：33506-33513
• 全文大小：421K
• ISSN：1944-8252

文摘

Recently, nanomedicine without drug carriers has attracted many pharmacists’ attention. A novel paclitaxel–s–s–paclitaxel (PTX–s–s–PTX) conjugate with high drug loading (∼78%, w/w) was synthesized by conjugating paclitaxel to paclitaxel by using disulfide linkage. The conjugate could self-assemble into uniform nanoparticles (NPs) with 1,1-dioctadecyl-3,3,3,3-tetramethylindotricarbocyanine iodide (DiR) encapsulated within the core of PTX–s–s–PTX NPs for photothermal therapy (PTT). The DiR-loaded self-assembled nanoparticles (DSNs) had a mean diameter of about 150 nm and high stability in biological condition. A disulfide bond is utilized as a redox-responsive linkage to facilitate a rapid release of paclitaxel in tumor cells. DSNs indicated significant cytotoxicity as a result of the synergetic chemo-thermal therapy. DSNs were featured with excellent advantages, including high drug loading, redox-responsive releasing behavior of paclitaxel, capability of loading with photothermal agents, and combinational therapy with PTT. In such a potent nanosystem, prodrug and photothermal strategy are integrated into one system to facilitate the therapy efficiency.