不同表面活性剂对两性霉素B脂质体体内外性质的影响

目的寻找与DSPE-PEG功能相似的表面活性剂修饰两性霉素B脂质体，以增加其在体内的稳定性，改善其体内分布，降低毒副作用。方法用薄膜超声法制备两性霉素B脂质体；比较用DSPE-PEG，Tween 80和Brij 35修饰后两性霉素B脂质体包封率、粒径分布、稳定性及组织分布的变化。结果两性霉素B脂质体的包封率最高为（91.2±1.6）％。修饰后的两性霉素B脂质体包封率提高，粒径减小，稳定性增加，肝、脾和肾中两性霉素B的浓度降低，脑中AmB的浓度提高。结论DSPE-PEG和Brij 35能提高脂质体逃避网状内皮系统吞噬的能力；Tween 80能增加两性霉素B在大鼠脑组织中的分布。

Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposome

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.