[Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposome].
OBJECTIVE
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.


CONCLUSIONS
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.
D000666:Amphotericin B / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004347:Drug Interactions; D008081:Liposomes / Q000737:chemistry; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000494:pharmacology; D000077423:Polidocanol; D011092:Polyethylene Glycols / Q000494:pharmacology; D011136:Polysorbates / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013501:Surface-Active Agents / Q000494:pharmacology*; D014018:Tissue Distribution
D000935:Antifungal Agents; D004337:Drug Carriers; D008081:Liposomes; D010714:Phosphatidylethanolamines; D011136:Polysorbates; D013501:Surface-Active Agents; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D000077423:Polidocanol; D011092:Polyethylene Glycols; D000666:Amphotericin B