二次乳化-冻融法制备5-氟尿嘧啶脂质体及其包封率的测定  

Preparation of 5-FU liposomes by double emulsification and freeze-thawing method

作　　者：顾吉晋[1] 邓英杰[1] 董晓东[1] 

机构地区：[1]沈阳药科大学药学院

出　　处：《中国药剂学杂志（网络版）》2009年第2期44-51,共8页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的结合二次乳化法和冻融法制备5-氟尿嘧啶脂质体来提高5-氟尿嘧啶脂质体的包封率(encapsulation efficiency,En)。方法采用二次乳化法制备5-氟尿嘧啶脂质体,建立超滤-HPLC法测定冻融前后5-氟尿嘧啶脂质体的包封率,并考察了二次乳化过程中温度、乳化时间对包封率的影响。结果最终确定第一次乳化温度和时间分别为25℃、3min,第二次乳化温度和时间分别为25℃、10min。冻融前后的包封率分别为(23.60±0.87)%和(30.90±2.59)%。结论二次乳化法和冻融法结合能显著提高5-氟尿嘧啶脂质体的包封率。Objective To prepare 5-FU liposomes by double emulsification and freeze-thawing method in order to improve the encapsulation efficiency of 5-FU in liposomes. Methods 5-FU liposomes were prepared by double emulsification method and the encapsulation efficiency was determined by ultrafiltration-HPLC method before and after freeze-thawing. Also, the influence of temperature, emulsifying time during the emulsification process on the encapsulation efficiency was investigated. Results Temperature and time had significant influence and the encapsulation efficiency of 5-FU could be improved when keeping both the first emulsion and the second emulsion temperature at 25 ℃, and emulsified for 3 and 10 min, respectively. Before and after freeze-thawing, the encapsulation rates were (23.6±0.87)% and (30.9±2.59)%, respectively. Conclusion Double emulsification and freeze-thawing method can significantly increase the encapsulation efficiency 5-FU in liposomes.

关 键 词：药剂学 5-氟尿嘧啶脂质体 二次乳化法 冻融法 超滤法 包封率 

分 类 号：R94[医药卫生—药剂学]