冻干保护剂对HB有效组分脂质体包封率和粒径的影响

目的研究不同冻干保护剂种类和浓度对HB有效组分脂质体冻干前后包封率和平均粒径的影响。方法按16个处方制备了HB有效组分脂质体,采用荧光分光光度法测定包封率,用显微镜和数码图象分析软件测定了平均粒径,通过冻干前后脂质体包封率和粒径的比较优选出最佳的冻干保护剂。结果最佳冻干保护剂为甘露醇和二元保护剂蔗糖-甘氨酸,包封率达到69.91%和66.70%,外观效果良好,比例分别为,甘露醇:PC:CH:HB=4:1:0.5:0.2;蔗糖:甘氨酸:PC:CH:HB=4:0.8:1:0.5:0.2。结论冻干保护剂可减少脂质体囊泡在冻干过程受到的破坏以及对脂质体包封率和粒径的影响。

Effects of Lyoprotectents on the Encapsulation and Vesicles Size of HB Liposome

Objective To study the effects of freeze-drying on the endcapsulation and vesicles size of HB liposome with different kinds of lyoprotectents at various concentrations.Methods Sixteen formulations of HB liposome were designed.The entrapment ef- ficiency was examined by fluorospectrophotometry.The particle size of the preparation was examined by microscope and digital im- aging analysis software.The optimized lyoprotectent was selected based on the comparison of entrapment efficiency and particle size before and after freeze-drying.Results The use of sucrose as a primary lyoprotectent and glycine as a supporting lyoprotectents and the use of mannitol provided the highest encapsulation rate and minimal change of HB liposomes.The results showed that the optimum formula were Man:PC:CH:HB=4:1:0.5:0.2;Suc:Gly:PC:CH:HB=4:0.8:1:0.5:0.2,theen- capsulation rates were 69.91% and 66.70%.Conclusion The lyoprotectent can protect the liposome vesicles during freeze-dr- ying and mininal the influences of encapsulation and particle size.