赵亮 崔文禹 王永峰 (1. 辽宁医学院 辽宁锦州 121001；2. 沈阳药科大学；3. 阿斯顿大学)
摘 要 目的：研究维生素E琥珀酸聚乙二醇酯 (Vit E TPGS) 作为一种新型乳化剂在聚酸酐紫杉醇微球中的应用，以提高微球质量。方法：以熔解浓缩聚合法制备聚［1，3-双(对羧基苯氧基)丙烷-癸二酸］，利用Vit E TPGS和聚乙烯醇(PVA)分别作乳化剂，通过单乳化方法制备紫杉醇微球。结果： Vit E TPGS作为微球乳化剂的用量只有0.1%,低于传统乳化剂PVA的10%，载药量和包封产率提高到8.51%，89.1%，在体外释药实验中，无明显突释现象，累积释药率达到85%。结论：相比于传统的乳化剂PVA， 无论是在微球的制备还是在药物的包封产率上，Vit E TPGS都是一种更加有效安全的乳化剂。
关键词 维生素E琥珀酸聚乙二醇酯；聚酸酐；乳化剂; 聚［1，3-双(对羧基苯氧基)丙烷-癸二酸］
中图分类号：R944.9
文献标识码：A
文章编号：1008-049X(2007)05-0433-03
d-α-tocopheryl Polyethylene Glycol 1 000 Succinate(Vitamin E TPGS) Used as Emulsifier for Fabrication of Paclitaxelloaded Polyanhydride Microspheres
Zhao Liang(Liaoning Medical University, Liaoning，Jinzhou 121001, China); Cui Wenyu (Shenyang Pharmaceutical University, Shenyang Liaoning 110016, China); Wang Yongfeng (Aston Univeristy, Birmingham, UK)
ABSTRACT Objective: To study the effect of d-α-tocopheryl polyethylene glycol 1000 succinate(Vitamin E TPGS) as a new emulsifier on polyanhydride microspheres for improving the quality of microspheres.Method: Poly1,3-bis(p-carboxyphenoxy) propanesebacic acid was prepared by the melt condensation. By using Vitamin E TPGS and PVA as emulsifiers microspheres were obtained by single emulsion solvent evaporation technique.Result: The required amount of TPGS was only 0.1%, an amount 10 times less than PVA. The drug content and encapsulation efficiency for paclitaxel containing microspheres were increased to 8.51%，89.1%，respectively. There was no burst release happening in vitro drugrelease experiment and the drug accumulative release rate was 85%.Conclusion: Vitamin E TPGS could be a more effective and safer emulsifier in fabrication and characterization of microspheres for drug delivery compared with traditional emulsifiers.
KEY WORDS d-α-tocopheryl polyethylene glycol 1 000 succinate; Polyanydride; emulsifier; Poly1,3-bis(p-carboxyphenoxy) propanesebacic acid
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