葛根素纳米结构脂质载体的制备及理化性质考察

目的:制备用于脑靶向给药的葛根素纳米结构脂质载体(Pue-NLC)并考察其理化性质.方法:采用乳化-超声分散法制备Pue-NLC；以包封率为指标,通过正交试验考察固体脂质材料用量、豆磷脂与泊洛沙姆-188的比例、脂质材料与乳化剂的比例及药物用量对处方工艺的影响,确定最佳制备工艺；通过透射电镜观察粒子形态,分别用Zeta电位及粒度分析仪测定表面电位和粒径,离心超滤法测定包封率,透析法考察其体外释药特性,HPLC测定葛根素含量.结果:最佳制备工艺为脂质材料用量400 mg,豆磷脂与泊洛沙姆-188的比例1:3,脂质材料与乳化剂的比例为1:2,药物用量10 mg.制备的Pue-NLC外形呈类圆球状,粒径分布均匀,平均粒径(89±7)nm,包封率(91.33±1.2)％,平均Zeta电位(-22±0.4)mV；Pue-NLC中葛根素在24 h累积释放率69.25％,且无突释效应.结论:采用乳化-超声分散法制备的Pue-NLC粒径大小分布均匀,药物包封率高,具有明显的缓释效果.

Preparation and Physico-chemical Properties Investigation of Puerarin Nanostructured Lipid Carriers

Objective: To prepare an appropriate puerarin-loaded nanostructured lipid carriers(Pue-NLC) for brain targeted drug delivery,and investigate its physicochemical properties and in vitro release. Method: Pue-NLC was prepared by emulsion-ultrasonic dispersion method.With encapsulation efficiency as index,single factor test and orthogonal test was adopted to optimize preparation technology with the amount of solid lipid material,ratio of soybean lecithin and poloxamer-188,ratio of lipid material and emulsifier,the amount of drug as factors;Particle morphology of dispersion was observed by transmission electron microscopy,surface potential and particle size were determined by Zeta potential and particle size analyzer,entrapment efficiency was determined by centrifugation ultrafiltration method.In vitro drug release behavior was studied by dialysis,the content of puerarin was determined by HPLC. Result: Optimum preparation technology was as following:the dosage of solid lipid material 400 mg,ratio of soybean lecithin and poloxamer-188=1:3,ratio of lipid material and emulsifier 1:2,the amount of drug 10 mg.Under transmission electronic microscope, Pue-NLC assumed spherical shape. Its distribution of particle size was even with the average value of (89±7) nm.Entrapment efficiency was (91.33±1.2)%.The average Zeta potential was (-22±0.4) mV;Cumulative release of puerarin was 69.25% in 24 h without burst effect. Conclusion: These prepared Pue-NLC had uniform particle size distribution,high encapsulation efficiency,sustained release effect.