α-生育酚琥珀酸酯抗肿瘤新剂型研究进展  

Research Advance in Novel Dosage Forms of α-Tocopheryl Succinate for Anti-tumor

作　　者：郑益萍[1] 鲁春青 纪宏宇[1,2] 唐景玲[1] Zheng Yiping;Lu Chunqing;Ji Hongyu;Tang Jingling(College of Pharmacy, Harbin Medical University, Harbin 150086, China;Department of Pharmacy, the Second Affiliated Hospital of Harbin Medical University)

机构地区：[1]哈尔滨医科大学药学院,哈尔滨150086 [2]哈尔滨医科大学附属第二医院药学部

出　　处：《中国药师》2018年第7期1275-1277,共3页China Pharmacist

摘　　要：α-生育酚琥珀酸酯(α-TOS)是维生素E(VE)的衍生物,具有广泛的抗肿瘤活性,能选择性抑制乳腺癌、肺癌、前列腺癌和结肠癌等多种肿瘤细胞生长。α-TOS口服易被胃肠道酯酶水解为无抗肿瘤活性的VE,为避免α-TOS被胃肠道酯酶水解,需将其通过腹腔或静脉注射给药,然而α-TOS在水溶液中溶解度差,因此极大地限制了其临床应用。随着新剂型的开发,纳米粒、脂质体、纳米乳、纳米囊泡和胶束等纳米技术的应用可改善α-TOS的溶解度,增强其抗肿瘤疗效。本文通过文献检索,对国内外α-TOS抗肿瘤新剂型的研究概况进行综述,为其新剂型的开发提供参考。α-Tocopheryl succinate（ α-TOS） is a derivative of vitamin E（ VE）. Researches indicated that α-TOS can selectively inhibit the growth of various types of cancer cells including breast,lung,prostate and colon cancers. α-TOS is easily hydrolyzed into vitamin E without antitumor activity by gastrointestinal esterase after oral administration,therefore,it depends on intraperitoneal or intravenous injection in order to protect α-TOS from being hydrolyzed by intestinal esterases. However,α-TOS has low solubility in aqueous solution,which greatly limits its application in cancer chemotherapy. With the development of new dosage forms,such as nanoparticles,liposomes,nanoemulsions,nanovesicles and micelles,the solubility of α-TOS can be improved and its antitumor efficacy can be enhanced. The research progress in the new dosage forms of α-TOS at home and abroad was reviewed through searching literatures in order to provide reference for the development of the new dosage forms of α-TOS.

关 键 词：α-生育酚琥珀酸酯 抗肿瘤活性 纳米粒 脂质体 纳米乳 

分 类 号：R944.9[医药卫生—药剂学]