快速膜乳化-溶剂萃取/挥发法制备水飞蓟宾PLGA微球的工艺优选

Optimization of Preparation Technology of Silybin PLGA Microspheres by Premix Membrane Emulsification-Solvent Extraction/Evaporation Method

摘要:

目的: 制备粒径均一的水飞蓟宾PLGA微球,并优选其制备工艺。 方法: 采用快速膜乳化-溶剂萃取/挥发法制备水飞蓟宾PLGA微球,以平均粒径和径距为指标,通过单因素试验考察油相溶剂、膜孔径、过膜压力、油水相体积比4个影响因素,正交试验考察药辅比、PVA质量分数及油水相体积比对制备工艺的影响;考察水飞蓟宾PLGA微球的平均粒径、粒径分布、载药量、包封率及形貌等理化性质。 结果: SPG膜孔径2.8 μm,过膜压力1.0 MPa,离心20 min,固化液为生理盐水;水飞蓟宾PLGA微球的最佳制备工艺为药辅比1:4,PVA质量分数3%,油水相体积比1:19。制备的微球圆整度好、表面光滑,平均粒径(2.634±0.35) μm,径距(13.326±3.06),载药量(14.84±0.76)%,包封率(56.16±3.77)%。 结论: 快速膜乳化法可用于制备中药难溶性成分水飞蓟宾PLGA微球,且制备的微球粒径均一可控。

Abstract:

Objective:To prepare uniform-sized silybin loaded poly (lactic-co-glycolic acid) (PLGA) microspheres and optimize its preparation technology. Method: Silybin PLGA microspheres was prepared by premix membrane emulsification-solvent extraction/evaporation method,with the average particle size and span as indexes,oil phase solvent,membrane pore size,membrane pressure and volume ratio of oil-water phase were investigated by single factor test,influence of pharmaceutical-accessories ratio,the mass fraction of PVA and volume ratio of oil-water phase on preparation technology was investigated by orthogonal test;The mean particle size,particle size distribution,drug loading,entrapment efficiency,morphology and other physical-chemical properties were evaluated. Result: Pore size of SPG membrane was 2.8 μm,membrane pressure was 1.0 MPa,centrifuged time of 20 min,physiological saline as hardening liquid;Optimum preparation technology of silybin PLGA microspheres was as following:pharmaceutical-accessories ratio of 1:4,the mass fraction of PVA of 3%,volume ratio of oil-water phase of 1:19.Prepared microspheres were round with smooth surface,the mean diameter was (2.634±0.35) μm,span was (13.326±3.06),drug loading was (14.84±0.76)% and entrapment efficiency was (56.16±3.77)%. Conclusion: Premix membrane emulsification method could be used to prepare silybin PLGA microspheres,which was an insoluble component from Chinese meteria medica,and particle size of prepared silybin PLGA microspheres was uniform and controllable.