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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。
Objective: To study the application of Vitamin E TPGS as a new emulsifier in paclitaxel microspheres to improve the microsphere quality. Methods: Poly [1,3-bis (p-carboxyphenoxy) propane-sebacic acid] was prepared by melt-condensation polymerization. VitE TPGS and polyvinyl alcohol (PVA) Paclitaxel microspheres. Results: The dosage of Vit E TPGS as microsphere emulsifier was only 0.1%, lower than that of traditional emulsifier PVA by 10%, and the drug loading and entrapment yield increased to 8.51% and 89.1% respectively. In in vitro drug release experiments, Obvious burst phenomenon, the cumulative release rate reached 85%. Conclusion: Compared with the traditional emulsifier PVA, Vit E TPGS is a more effective and safe emulsifier both in the preparation of microspheres and in the encapsulation yield of drugs.