pH梯度法结合逆向蒸发法制备氟尿嘧啶脂质体

Preparation of Fluorouracil Liposomes by pH-gradients Method Coupled with Reverse Evaporation Technique

目的:以pH梯度法结合逆向蒸发法制备氟尿嘧啶脂质体,并评价其质量。方法:采用pH梯度法结合逆相蒸发制备氟尿嘧啶脂质体,以包封率为指标进行处方优化;用Sephadex G-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;以激光散射粒径分析仪测定脂质体的平均粒径及Zeta电位,透射电镜观测形态,并初步考察脂质体在室温和4℃冷藏条件下的稳定性。结果:制得的氟尿嘧啶脂质体外观形态圆整,平均粒径为282 nm,Zeta电位为-25.9mV,平均包封率为75.39%,4℃冷藏条件下贮存脂质体的稳定性要明显优于室温贮存。结论:运用pH梯度法结合逆向蒸发法能制备包封率较高的氟尿嘧啶脂质体。

Objective： To prepare fluorouracil liposomes by pH-gradients method coupled with reverse evaporation technique and evaluate its quality. Method： The liposomes carried fluorouracil was prepared by pH-gradients method coupled with reverse evaporation technique; Orthogonal design was used to select the optimum formulation; Unloaded fluorouracil were separated by Sephadex-G50 chromatography and HPLC method was used to determine the entrapment efficiency of fluorouracil liposomes; The shape, particle size and zeta-potential of fluorouracil liposomes were investigated with transmission electron microscope and laser scatter; The stability of fluorouracil liposomes was investigated at room temperature and low temperature of 4℃. Reset： The obtained fluorouracil liposomes were round, smooth particles with average size of 282 nm, zeta potential was -25.9mV and entrapment efficiency 75.39%. The fluorouraeil liposomes at low temperature of 4℃ was more stable than that at room temperature. Conclusion： The higher entrapment efficiency of fluorouracil liposomes can he obtained by pH-gradients method coupled with reverse evaporation technique.