星点设计效应面法优化吴茱萸次碱固体脂质纳米粒处方

Optimization of rutaecarpine solid lipid nanoparticles by central composite design and response surface methodology

目的优化吴茱萸次碱固体脂质纳米粒(Rut-SLN)的处方。方法以薄膜-超声法制备Rut-SLN,以包封率、平均粒径、Zeta电位为评价指标,采用星点设计考察单硬脂酸甘油酯/主药质量比(A)、卵磷脂/单硬脂酸甘油酯质量比(B)、泊洛沙姆188质量(C)3因素对包封率、平均粒径、Zeta电位的影响,以效应面法选取最佳处方条件进行预测分析。结果根据优化处方制得Rut-SLN的包封率、平均粒径、Zeta电位分别为84.27%、122.6 nm、-20.7mV。结论优选的Rut-SLN处方稳定可行,包封率高,稳定性好,可用于生产。

Objective To optimize the prescription of rutaecarpine solid lipid nanoparticles （Rut-SLN）. Methods Using the film-ultrasound method to lining-up the Rut-SLN, with the entrapment efficiency （EE）, Zeta potential, and the average particle size as the evaluation indexes, using central composite design to inspect the effects of glYCerol monostearate/drug quality ratio （A）, soybean lecithin for injection/glycerol monostearate mass ratio （B）, Poloxamer 188 （C） on three factors of the EE, Zeta potential, and average particle size. Prediction and analysis for selecting the best prescription condition were carried out by using the response surface method. Results According to the optimized prescription, the EE, Zeta potential, and the average particle size of Rut-SLN was respectively 84.27%, 122.6 nm, and -20.7 mV. Conclusion The optimal prescription of Rut-SLN has better stability, feasibility, and high EE, which is suitable for the production.