Box-Behnken效应面法优化长春西汀长循环脂质体处方

目的通过优化手段筛选最佳处方,制备长春西汀长循环脂质体。方法采用薄膜分散法制备长循环脂质体,分别以磷脂质量浓度(1ρ)、Tween80质量浓度(ρ2)、磷脂-药质量比(ms∶md)为考察对象,以包封率(Y1)、载药量(Y2)和粒径(d)为评价指标,利用三因素三水平Box-Behnken效应面设计法筛选长循环脂质体的最佳处方;透射电子显微镜考察其形态与粒径。结果长循环脂质体的包封率为85.9%;载药量18.5 mg.g-1;粒径为213.4 nm,与理论值偏差均小于10%。结论长春西汀长循环脂质体采用Box-Behnken实验设计法优化是可行的。

Optimization of vinpocetine long-circulation liposome formulation by Box-Behnken experimental design

Abstract: Objective To develop and optimize vinpocetine long-circulation liposome. Method Long-circulation liposome was prepared by the membrane hydration method. A three factor, three-level Box–Behnken design was used for the optimization procedure, with the soybean phosphatidylcholine concentration (ρ₁), Tween80 concentration (ρ₂) and soybean phosphatidylcholine to drug (m_s∶m_d) as the independent variables, and the entrapment efficiency(Y₁), the loading content(Y₂), the particle diameter (d) as the response variable; the particle shape was measured by transmission electrical microscope. Results In the optimized vinpocetine long-circulation liposome formulation, the entrapment efficiency was 85.9 %, the drug content was 18.5 mg.g^-1, and the particle diameter was 213.4 nm. The observed responses were coincident with the predicted values of the optimized formulation, and the deviations of the measured values from the predicted ones were less than 10 %. Conclusion The Box-Behnken experimental design facilitates the formulation and optimization of vinpocetine long-circulation liposome.