白藜芦醇胶束的制备及初步质量评价

Preparation and Preliminary Quality Evaluation of Resveratrol Micelles

目的:制备白藜芦醇聚合物胶束(RES-M)并对其进行初步的质量评价。方法:采用薄膜分散法,以普朗尼克F127(pluronic F127)作为载体材料,制备RES-M;以包封率和载药量为指标,通过单因素考察对RES-M的处方及工艺进行优化,并对最优处方制剂进行质量评价。结果:最优处方为pluronic F127与RES投料量比例为8∶1,旋蒸温度为45℃,旋蒸时间为25 min,水化介质为超纯水,水化体积为10 ml。最优处方的RES-M粒径为21.79 nm,多分散系数(PDI)为0.049,Zeta电位为-6.26 mV,包封率为(99.96±0.57)%,载药量为(10.67±0.37)%;RES-M的抗氧化能力与RES本身相当。结论:本试验成功制备RES-M,制备工艺简单,包封率与载药量均较高,为白藜芦醇制剂的研发提供了一定的理论基础。

Objective:To prepare stable polymeric micelles of resveratrol(RES-M)and to evaluate the quality.Methods:The polymeric micelles of resveratrol were prepared by a thin film dispersion method using Pluronic F127 as the carrier material.The formulation and technology of RES micelles were optimized by single factor investigation,and the quality of the optimal formulation was evaluated.Results:The optimal formulation and technology were as follows:the ratio of Pluronic F127 to RES was 8∶1,the spinning temperature was 45℃,the spinning time was 25 min,the hydration medium was super pure water and the hydration volume was 10 ml.The optimal size of RES micelles was 21.79 nm,the PDI was 0.049,the Zeta potential was-6.26 mV,and the average encapsulation rate was(99.96±0.57)%.The average drug loading was(10.67±0.37)%.The antioxidant capacity of RES-M was comparable to that of RES itself.Conclusion:Resveratrol micelles were successfully prepared in this experiment.The preparation process of the micelles is simple.The micelles have small particle size,good dispersion,uniform particle size distribution,and high entrapment efficiency and drug loading,which provide certain theoretical basis for the research and development of resveratrol preparations.