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目的以聚乙二醇单甲醚-聚乳酸-聚组氨酸(mPEG-PLA-PHis)pH敏感嵌段共聚物为载体材料,制备白藜芦醇载药胶束,并对其处方和工艺进行优化和体外评价。方法采用薄膜分散水化法制备白藜芦醇胶束,应用中心复合设计-效应面法优化白藜芦醇胶束的处方和制备工艺;透析法考察载药胶束在不同pH值磷酸盐缓冲液中的释药行为。结果在优化条件下制备的胶束平均粒径为54.13 nm,包封率(90.69±1.87)%,载药量为(10.25±0.64)%,载药胶束的体外释药行为具有pH敏感性。结论中心复合设计-效应面优化法的预测性较好,所制备的pH敏感性白藜芦醇胶束粒径小且均匀,载药量和包封率均较高。
OBJECTIVE To prepare resveratrol-loaded micelles by using polyethylene glycol monomethyl ether-polylactic acid-polyhistidine (mPEG-PLA-PHis) pH sensitive block copolymer as carrier material, Optimization and in vitro evaluation. Methods Resveratrol micelles were prepared by membrane-dispersed hydration method. Central composite design-response surface methodology was used to optimize the preparation and preparation of resveratrol micelles. Dialysis was used to investigate the effects of drug-loaded micelles Liquid release behavior. Results The average diameter of micelles was 54.13 nm, the encapsulation efficiency was (90.69 ± 1.87)% and the drug loading was (10.25 ± 0.64)%. The in vitro drug release behavior of drug-loaded micelles was pH sensitive . Conclusion The center composite design - effect surface optimization method has good predictability. The prepared pH-sensitive resveratrol micelles have small and uniform particle size, high loading capacity and encapsulation efficiency.