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Antimicrobial Agents and Chemotherapy, October 2003, p. 3339-3342, Vol. 47, No. 10
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.10.3339-3342.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

Effects of Lipid-Based Oral Formulations on Plasma and Tissue Amphotericin B Concentrations and Renal Toxicity in Male Rats

Verica Risovic,1 Michael Boyd,2 Eugene Choo,1 and Kishor M. Wasan1*

Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences,1 Acute Care Animal Unit, University of British Columbia, Vancouver, British Columbia, Canada V6T 1Z32

Received 3 January 2003/ Returned for modification 4 June 2003/ Accepted 23 June 2003

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.

* Corresponding author. Mailing address: Division of Pharmaceutics & Biopharmaceutics, Faculty of Pharmaceutical Sciences, The University of British Columbia, 2146 East Mall Ave., Vancouver, British Columbia, Canada V6T 1Z3. Phone: (604) 822-4889. Fax: (604) 822-3035. E-mail: Kwasan{at}interchange.ubc.ca.

Antimicrobial Agents and Chemotherapy, October 2003, p. 3339-3342, Vol. 47, No. 10
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.10.3339-3342.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Gershkovich, P., Wasan, E. K., Lin, M., Sivak, O., Leon, C. G., Clement, J. G., Wasan, K. M. (2009). Pharmacokinetics and biodistribution of amphotericin B in rats following oral administration in a novel lipid-based formulation. J Antimicrob Chemother 64: 101-108 [Abstract] [Full Text]  


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