[表面活性剂对两性霉素B脂质体体外及体内性质的影响]
[Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposome].
作者信息
Zhang Xiao-bin, Xie Jie-qiong, Hou Xin-pu
机构信息
Department of Physical-pharmacy, School of Pharmacy, Peking University, Beijing 100083, China.
出版信息
Yao Xue Xue Bao. 2003 Jun;38(6):471-4.
AIM
Some surfactants such as DSPE-PEG, Tween 80 and Brij 35 were used to modify the amphotericin B liposome, improve the stability, optimize the tissue distribution and decrease the toxicity of amphotericin B liposome.
METHODS
The amphotericin B liposome was prepared by the film-supersound method. The effects of cholesterol and amphotericin B on the encapsulation percentage were studied. The diameter, leakage percentage in phosphate buffer solution(PBS) and calf blood serum, and tissue distributions of amphotericin B liposome in the rat were determined.
RESULTS
The top encapsulation percentage of amphotericin B liposome is (91.2 +/- 1.6)%. After modification with DSPE-PEG, Tween 80 and Brij 35, the encapsulation percentages were improved, the average diameters were decreased and the stabilities were improved, the amphotericin B concentrations in the liver, spleen and kidney were decreased, and the amphotericin B concentrations in the brain were increased, especially in the AmB-L-Tween 80 group.
CONCLUSION
DSPE-PEG and Brij 35 could decrease the clearing of reticuroendothelial systems(RES) to the amphotericin B liposome and Tween 80 could facilitate the transporting of amphotericin B liposome into the brain.
目的
使用一些表面活性剂如二硬脂酰磷脂酰乙醇胺-聚乙二醇（DSPE-PEG）、吐温80和Brij 35修饰两性霉素B脂质体，以提高其稳定性、优化组织分布并降低两性霉素B脂质体的毒性。
方法
采用薄膜超声法制备两性霉素B脂质体。研究胆固醇和两性霉素B对包封率的影响。测定两性霉素B脂质体的粒径、在磷酸盐缓冲液（PBS）和小牛血清中的渗漏率以及在大鼠体内的组织分布。
结果
两性霉素B脂质体的最高包封率为（91.2±1.6）%。经DSPE-PEG、吐温80和Brij 35修饰后，包封率提高，平均粒径减小，稳定性提高，肝脾肾中两性霉素B浓度降低，脑中两性霉素B浓度升高，尤其是在两性霉素B-脂质体-吐温80组。
结论
DSPE-PEG和Brij 35可降低网状内皮系统（RES）对两性霉素B脂质体的清除，吐温80可促进两性霉素B脂质体进入脑内。
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