Optimization of Preparation Technology of Celastrol Nanostructured Lipid Carrier and Its Characterization / 中国药房

ABSTRACT

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.