张小滨, 谢洁琼, 侯新朴. 不同表面活性剂对两性霉素B脂质体体内外性质的影响J. 药学学报, 2003, 38(6): 471-474.
引用本文: 张小滨, 谢洁琼, 侯新朴. 不同表面活性剂对两性霉素B脂质体体内外性质的影响J. 药学学报, 2003, 38(6): 471-474.
ZHANG Xiao-bin, XIE Jie-qiong, HOU Xin-pu. Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposomeJ. Acta Pharmaceutica Sinica, 2003, 38(6): 471-474.
Citation: ZHANG Xiao-bin, XIE Jie-qiong, HOU Xin-pu. Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposomeJ. Acta Pharmaceutica Sinica, 2003, 38(6): 471-474.

不同表面活性剂对两性霉素B脂质体体内外性质的影响

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

  • 摘要: 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。

     

    Abstract: AimSome 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. MethodsThe 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. ResultsThe 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. ConclusionDSPE-PEG and Brij 35 could decrease the clearing of reticuroendothelial systems(RES) to the amphotericin B liposome and Tween80 could facilitate the transporting of amphotericin B liposome into the brain.

     

/

返回文章
返回