Academy of Chinese Medical Sciences, Zhejiang Chinese Medical University, Hangzhou, 310053, China.
Department of Pharmacy, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, China.
Curr Med Sci. 2020 Apr;40(2):218-231. doi: 10.1007/s11596-020-2185-1. Epub 2020 Apr 26.
D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) is a pharmaceutical excipient approved by Chinese NMPA and FDA of USA. It's widely applied as a multifunctional drug carrier for nanomedicine. The advantages of TPGS include P-glycoprotein (P-gp) inhibition, penetration promotion, apoptosis induction via mitochondrial-associated apoptotic pathways, multidrug resistant (MDR) reversion, metastasis inhibition and so on. TPGS-based drug delivery systems which are responding to external stimulus can combine the inhibitory functions of TPGS towards P-gp with the environmentally responsive controlled release property and thus exerts a synergistic anti-cancer effect, through increased intracellular drug concentration in tumors cells and well-controlled drug release behavior. In this review, TPGS-based nano-sized delivery systems responsive to different stimuli were summarized and discussed, including pH-responsive, redoxresponsive and multi-responsive systems in various formulations. The achievements, mechanisms and different characteristics of TPGS-based stimuli-responsive drug-delivery systems in tumor therapy were also outlined.
D-α-生育酚聚乙二醇 1000 琥珀酸酯（TPGS）是一种经中国 NMPA 和美国 FDA 批准的药用辅料。它被广泛用作纳米医学的多功能药物载体。TPGS 的优点包括抑制 P-糖蛋白（P-gp）、促进渗透、通过线粒体相关凋亡途径诱导细胞凋亡、逆转多药耐药（MDR）、抑制转移等。基于 TPGS 的药物传递系统对外界刺激的响应可以将 TPGS 对 P-gp 的抑制功能与环境响应的控制释放特性相结合，从而通过增加肿瘤细胞内的药物浓度和良好控制的药物释放行为发挥协同抗癌作用。在这篇综述中，总结和讨论了基于 TPGS 的对不同刺激响应的纳米级给药系统，包括各种制剂中的 pH 响应、氧化还原响应和多响应系统。还概述了基于 TPGS 的刺激响应药物传递系统在肿瘤治疗中的成就、机制和不同特点。
