Open AccessEffects of Lipid-Based Oral Formulations on Plasma and Tissue Amphotericin B Concentrations and Renal Toxicity in Male Rats
Author(s) -
Verica Risovic,
Michael Boyd,
Eugene Choo,
Kishor M. Wasan
Publication year - 2003
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.47.10.3339-3342.2003
Subject(s) - toxicity , amphotericin b , pharmacology , chemistry , oral administration , pharmacokinetics , triglyceride , micelle , absorption (acoustics) , plasma concentration , chromatography , amphotericin b deoxycholate , kidney , cholesterol , medicine , biochemistry , biology , antifungal , microbiology and biotechnology , materials science , organic chemistry , composite material , aqueous solution , caspofungin
The purpose of this study was to determine the effects of various lipid and mixed-micelle formulations on the oral absorption and renal toxicity of amphotericin B (AMB) in rats. The maximum concentration of AMB in plasma and the area under the concentration-time curve for 0 to 24 h for AMB were elevated in rats administered triglyceride (TG)-rich AMB formulations in comparison to those in rats given (i) AMB preformulated as a micelle containing sodium deoxycholate with sodium phosphate as a buffer (DOC-AMB), (ii) an AMB-lipid complex suspension, or (iii) AMB solubilized in methanol. Furthermore, our findings suggest that AMB incorporated into TG-based oral formulations has less renal toxicity than DOC-AMB.