雷公藤红素纳米结构脂质载体的制备工艺优化及其表征

Optimization of Preparation Technology of Celastrol Nanostructured Lipid Carrier and Its Characterization

目的:优化雷公藤红素(Cel)纳米结构脂质载体(Cel-NLC)的制备工艺,并对其进行表征。方法:采用熔融乳化超声法制备Cel-NLC。在单因素试验基础上,以Cel包封率为指标,采用星点设计-响应面法优化液态脂质比例(占总质量的比例)、复合乳化剂用量及主药用量,并进行验证试验。利用纳米粒度及Zeta电位分析仪测定最优处方下制备的Cel-NLC的粒径及Zeta电位,在透射电镜下观察其形态。结果:最优处方的液态脂质比例为39%,复合乳化剂用量为196 mg,主药用量为8 mg。所制3批Cel-NLC的平均包封率为87.22%、平均粒径为(41.2±1.1)nm、平均Zeta电位为(-18.4±0.2)mV(n=3),电镜下观察其外观呈类球形。结论:优化的处方工艺方法简便、稳定可行,适用于Cel-NLC的制备。

OBJECTIVE:To optimize the preparation technology of Celastrol nanostructured lipid carriers(Cel-NLC),and to characterize it. METHODS:Cel-NLC was prepared by melt-emulsification ultrasonic method. Based on single factor test,using encapsulation rate of Cel as index,the ratio of liquid lipid(the ratio of total mass),the amount of compound emulsifier and the dose of main drug were optimized by central composite design-response surface methodology. Validation test was conducted. Zeta potential and particle size of Cel-NLC that prepared by optimal prescription were determined by using granularity and Zeta potential analyzer. The morphology of liposome was observed by TEM. RESULTS:The optimal prescription included that the ratio of liquid lipid was 39%;the amount of compound emulsifier was 196 mg;the dose of main drug was 8 mg. The average encapsulation efficiency of 3 batches of Cel-NLC was 87.22%;average particle size was (41.2 ± 1.1) nm,and average Zeta potential was (-18.4±0.2)mV(n=3). It was spherical under electron microscopy. CONCLUSIONS:The optimized technology is simple, stable and feasible,and it is suitable for the preparation of Cel-NLC.