冻干保护剂和复水溶液对HB-Ⅰa脂质体包封率的影响

Effects of lyoprotectents and rehydrated solutions on the encapsulation of HB-Ⅰa liposomes

目的：研究不同保护剂种类与浓度、不同复水溶液对HB-Ⅰa脂质体冻干前后包封率的影响。方法：按不同配方进行了18组对比实验，通过比较各组脂质体冻干前后包封率，优选较好的HB-Ⅰa脂质体冻干工艺。结果：在对HB-Ⅰa脂质体包封率的提高与冻干保护方面，蔗糖及甘氨酸所组成的二元保护剂显示了较好的效果；在保护剂使用过程中，过高或过低的蔗糖浓度对提高冻干HB-Ⅰa脂质体的包封率不利；在复水溶液的使用方面，当保护剂蔗糖存在时，冻干后缓冲液复水较纯水复水包封率高。结论：以蔗糖-甘氨酸-卵磷脂-胆固醇-HB-Ⅰa(4：0．8：1：0．5：0．2)的配方配制的HB-Ⅰa脂质体包封率冻干前可达91．1％，冻干后可达85．6％。

Objective: To study the effects of freeze-drying on the encapsulation of HB-Ⅰa lipo some with different kinds of lyoprotectents at various concentrations and different rehydrated solutions. Methods: Eighteen formulations of HB-Ⅰ a liposome were designed and their comparison studieswere performed. The optimized freeze-drying technique was selected based upon the encapsulation rate prior to and post freeze-drying. Results:The use of sucrose as a primary lyoprotectent and glycine as a supporting lyoprotectents provided a highest encapsulation rate and minimal change of HB-Ⅰa lipo somes. Sucrose at too high or too low concentrations failed to increase the encapsulation rate. At the presence of sucrose, the buffer solution showed a superior rehydration of freeze-dried HB-Ⅰa liposome to water. Conclusion: With an appropriate mass ratio of sucrose: glycine:phosphatidylcholine: cholesterol: HB-Ⅰ a( 4:0.8:1: 0.5: 0.2 ) the encapsulation rate of HB-Ⅰa liposome solution can be enhanced to 91.1% and 85.6% prior to and post the freeze-drying,respectively.