均匀设计法考察不同制备方法对氟尿嘧啶脂质体包封率的影响

The Effects of Preparation Methods on Entrapment Efficiency of Fluorouracil Liposomes by Applying Uniform Design

目的考察不同制备方法对氟尿嘧啶脂质体包封率的影响,从而优选较好的制备方法。方法分别以薄膜分散法、逆向蒸发法、pH梯度法、以及硫酸铵梯度法制备氟尿嘧啶脂质体,用SephadexG-50葡聚糖凝胶柱分离-高效液相色谱法测定氟尿嘧啶脂质体的包封率,以包封率为指标运用均匀设计法优选制备方法和处方。结果主动载药法尤其是pH梯度法制得的氟尿嘧啶脂质体包封率明显优于被动载药法,包封率顺序为pH梯度法>硫酸铵梯度法>逆向蒸发法>薄膜分散法。采用最优工艺制备氟尿嘧啶脂质体,平均包封率可达60.67%。结论制备方法对氟尿嘧啶脂质体包封率影响显著;pH梯度法能制得包封率较高的氟尿嘧啶脂质体。

Objective To study the effects of various preparation methods on the entrapment efficiency of fluorouracil liposomes in order to select the optimum one. Methods Different preparation methods, including film dispersing, reverse phase evaporation, pH-gradients and ammonium sulfate gradients were used to prepare the fluorouracil liposomes. Unloaded fluorouracil was separated by Sephadex-G50 chromatography and detected by HPLC. Uniform design was used to optimize the preparation method and formulation by entrapment efficiency of fluorouracil liposomes. Results The entrapment efficiency of fluorouracil liposomes by active loading method was obviously higher than that by passive loading method. The order of entrapment efficiency was pH-gradients method 〉 ammonium sulfate gradients 〉 reverse phase evaporation 〉 film dispersing method. Using the optimum preparation method and formulation, the average entrapment efficiency could reach at 60.67%. Conclusion Preparation method has the remarkable influence on the entrapment efficiency of fluorouracil liposomes. The higher entrapment efficiency of fluorouracil liposomes can be obtained by pH-gradicnts method.