星点设计-效应面法优化紫杉醇自微乳给药系统

Optimization of self-microemulsifying drug delivery system for paclitaxel by central composite design-response surface method

目的紫杉醇自微乳释药系统的制备优化及评价。方法通过溶解度试验、伪三元相图的绘制及星点设计-效应面法,以粒径、平衡溶解度和自乳化时间为指标,筛选最佳处方,并对紫杉醇自微乳的理化性质和体外释药进行测定。结果紫杉醇自微乳最佳处方:十四酸异丙酯为23.93%、聚氧乙烯蓖麻油为57.91%、聚乙二醇400为18.16%;其平均粒径<40 nm,自乳化时间<86 s。结论制得的紫杉醇自微乳给药系统稳定,能显著提高紫杉醇的溶解度。

Objective To optimize and assess the preparation of self-microemulsifying drug delivery system（SMEDDS） for paclitaxel. Methods The optimum formulation of paclitaxel SMEDDS was screened by solubility, tertiary phase diagrams and central composite design-response surface method, with the particle size, the balanced solubility and the time of self-emulsification as parameters. The physic-chemical property and dissolution characters of paclitaxel SMEDDS were also determined. Results The optimum self-microemulsifying drug delivery system was composed of IPM（23.93%）, Cremophor EL（57.91%）, and PEG-400（18.16%）. The average partical size after the emulsification was less than 40 nm, the time of self-microemulsification was less than 86 s. Conclusion The prepared paclitaxel SMEDDS is stable, which can greatly increase the solubility of paclitaxel.