星点设计法优化地喹氯铵修饰紫杉醇与和厚朴酚共聚物胶束制备工艺

Optimizing Prescription of Dequalinium Modified Paclitaxel and Honokiol Polymeric Micelles by Central Composite Design-Response Surface Methodology

目的:制备地喹氯铵修饰紫杉醇与和厚朴酚Soluplus/TPGS共聚物胶束,并通过星点设计-响应面法优选出最佳处方,提高难溶性药物紫杉醇与和厚朴酚的包封率。方法:采用薄膜水化法制备地喹氯铵修饰紫杉醇与和厚朴酚Soluplus/TPGS共聚物胶束。采用星点设计-响应面法并使用Design-Expert 8.0.6.1统计学软件对试验组的响应值进行回归分析,优化共聚物胶束的制备工艺条件。结果:共聚物胶束最佳制备工艺为Soluplus/紫杉醇=150:1(质量比),Soluplus/TPGS=8:1(质量比),水化温度25℃。胶束中紫杉醇与和厚朴酚含量的综合评分为96.11%。结论:星点设计-响应面法优选出的地喹氯铵修饰紫杉醇与和厚朴酚Soluplus/TPGS共聚物胶束的制备工艺条件的重复性良好,操作简便,所建模型具有较好的实用性和预测性。

Objective:Dequalinium modified paclitaxel and honokiol Soluplus/TPGS polymeric micelles were prepared and the best prescription was optimized by central composite design-response surface methodology to increase the encapsulation efficiency of paclitaxel and honokiol.Methods:Dequalinium modified paclitaxel and honokiol Soluplus/TPGS polymeric micelles were prepared by film hydration method.The regression analysis of each experimental group was evaluated by central composite design-response surface methodology and the Design-Expert 8.0.6.1 software.Results:The best prescription was as following:Soluplus/paclitaxel=150:1(mass ratio);Soluplus/TPGS=8:1(mass ratio);the hydration temperature was 25 ℃ and the comprehensive score of encapsulation efficiencies was 96.11%.Conclusion:The preparation process optimized by central composite design-response surface methodology had a good repeatability and simple preparation,which indicated that this model possessed a good practicability and predictability.