Effect of surfactants on the in vitro and in vivo properties of amphotericin B liposome.
- Author:
Xiao-bin ZHANG
1
;
Jie-qiong XIE
;
Xin-pu HOU
Author Information
- Publication Type:Journal Article
- MeSH: Amphotericin B; administration & dosage; pharmacokinetics; Animals; Antifungal Agents; administration & dosage; pharmacokinetics; Brain; metabolism; Drug Carriers; Drug Delivery Systems; Drug Interactions; Liposomes; chemistry; Particle Size; Phosphatidylethanolamines; pharmacology; Polyethylene Glycols; pharmacology; Polysorbates; pharmacology; Rats; Rats, Sprague-Dawley; Surface-Active Agents; pharmacology; Tissue Distribution
- From: Acta Pharmaceutica Sinica 2003;38(6):471-474
- CountryChina
- Language:Chinese
-
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 Tween 80 could facilitate the transporting of amphotericin B liposome into the brain.
