Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposome / 药学学报

ABSTRACT

<p><b>AIM</b>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.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>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.</p>