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目的采用Box-Behnken实验设计法优化奥沙利铂(oxaliplatin,Ox)脂质体的制备工艺。方法以磷脂质量浓度(X1)、磷脂与Ox质量比(X2)和磷脂与胆固醇质量比(X3)为考察对象,以包封率(Y)为评价指标,采用三因素三水平的Box-Behnken实验设计筛选奥沙利铂脂质体最佳的处方。结果最优处方是磷脂质量浓度为10.20 g·L-1,磷脂与药物的质量比为31∶1,脂质体膜材料中磷脂与胆固醇质量比为3.8∶1。包封率的预测值与理论值偏差较小。结论 Box-Behnken实验设计法可用于奥沙利铂脂质体的处方优化。
OBJECTIVE To optimize the preparation of oxaliplatin (Ox) liposomes by Box-Behnken experimental design. Methods The concentration of phospholipid (X1), mass ratio of phospholipid to Ox (X2) and mass ratio of phospholipid to cholesterol (X3) were investigated. The encapsulation efficiency (Y) was used as the evaluation index and the three factors and three levels of Box-Behnken Experimental Design Screening of oxaliplatin liposomes best prescription. Results The optimal prescription was the phospholipid concentration of 10.20 g · L-1, the mass ratio of phospholipid to drug was 31:1, and the mass ratio of phospholipid to cholesterol in liposome membrane material was 3.8:1. The predicted value of the entrapment ratio has a small deviation from the theoretical value. Conclusion Box-Behnken experimental design method can be used to optimize the formulation of oxaliplatin liposomes.