乙醇对盐酸伊立替康脂质体粒径及包封率的影响

目的考察乙醇对盐酸伊立替康脂质体粒径及包封率的影响。方法以阳离子交换树脂分离游离药物和脂质体,并以紫外分光光度法和激光粒度仪分别测定脂质体的包封率和粒径;考察24 h内,空白脂质体、梯度脂质体及盐酸伊立替康载药脂质体在体积分数分别为0%、5%、10%、15%、20%、25%的乙醇溶液中粒径及包封率的变化。结果在乙醇体积分数不超过10%范围内,空白脂质体、梯度脂质体及盐酸伊立替康脂质体的粒径与包封率基本无变化;当乙醇体积分数达到15%及以上时,粒径随时间的延长逐渐增大,而包封率逐渐下降,包封率下降最高可达64.51%。结论在盐酸伊立替康脂质体的制备过程中,一定量的乙醇会对脂质体的粒径及包封率产生严重影响,控制乙醇体积分数不大于10%,脂质体的粒径及包封率基本无变化。

ffects of ethanol on the size and entrapment efficiency of irinotecan hydrochloride liposomes

Objective To evaluate effects of ethanol on the size and entrapment efficiency of irinotecan hydrochloride(CPT-11) liposomes.Methods Free CPT-11 and liposomes were separated by cation exchange resin.Ultraviolet spectrophotometry and laser particle analyzer were applied to determine the entrapment efficiency and the size of liposomes,respectively.In 24 h,the changes of size and entrapment efficiency of blank liposomes,gradient liposomes,and CPT-11 liposomes with 0%,5%,10%,15%,20%,25%(φ) ethanol concentration were detected.Results In the presence of ethanol with the concertration less than 10%,the size and entrapment efficiency of blank liposomes,gradient liposomes,and CPT-11 liposomes had no obvious changes.While ethanol concentration is above 15%(φ),the size of liposomes gradually increased with the extension of time,the entrapment efficiency gradually decreased,and the reduction percentage of entrapment efficiency was up to 64.51%.Conclusions In the preparation of CPT-11 liposomes,the ethanol concentration has significant effect on the size and entrapment efficiency.When ethanol concentration is not higher than 10%,the size and entrapment efficiency of liposomes have no changes.