山药总多糖脂质体的制备及表征

Preparation and Characterization of Dioscoreae Rhizoma Polysaccharide Liposomes

目的:优选山药总多糖脂质体的处方工艺并对其进行表征,为该有效部位的开发提供参考。方法:采用逆向蒸发-微孔滤膜挤压法制备山药总多糖脂质体。以卵磷脂质量浓度、卵磷脂与胆固醇比例、药脂比为考察因素,包封率为评价指标,采用L9(34)正交试验设计优选处方。利用苯酚-硫酸法测定山药总多糖含量,高速离心法测定山药总多糖脂质体的包封率。结果:山药总多糖脂质体的最佳处方工艺为卵磷脂-胆固醇(6∶1),卵磷脂质量浓度12 g·L^(-1),药脂比1∶15;包封率和载药量分别为83.29%,3.83%,平均粒径121.6 nm,多分散指数平均值0.136,平均Zeta电位-31.8 m V。结论:优选的处方工艺稳定可行、重复性好。制备的山药总多糖脂质体形态圆整、粒径分布均匀、包封率较高。

Objective： To optimize formulation process of Dioscoreae Rhizoma polysaccharide liposomes and investigate its characterization. Method： The liposomes was prepared by the reverse evaporation-microporous membrane extrusion method.Taking lecithin concentration,ratio of lecithin to cholesterol and ratio of drug to lipid as factors,orthogonal test was adopted to optimize formulation process with entrapment efficiency as index.High-speed centrifugation was developed for determination of entrapment efficiency.The content of Dioscoreae Rhizoma polysaccharide was measured by phenol-sulfuric acid method. Result： Optimum formulation of Dioscoreae Rhizoma polysaccharide liposomes was as following：lecithin concentration of 12 g·L^-1,lecithin-cholesterol （6：1）,drug-lipid （1：15）.These average values of particle size,polydispersity index and Zeta potential were 121.6 nm,0.136 and -31.8 mV,entrapment efficiency and drug loading were 83.29%and 3.83%,respectively. Conclusion： This optimized process is stable and feasible.Dioscoreae Rhizoma polysaccharide liposomes has round shape,uniform particle size distribution and high entrapment efficiency.