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Amphotericin B lipid preparations: what are the differences?

J P Adler-Moore¹, R T Proffitt

¹Department of Biological Sciences, California State Polytechnic University, Pomona, CA 91768, USA. jpadler@csupomona.edu

Clinical Microbiology and Infection : the Official Publication of the European Society of Clinical Microbiology and Infectious Diseases

|April 24, 2008

Summary

Lipid formulations of amphotericin B reduce toxicity while maintaining antifungal activity. Differences in pharmacokinetics and toxicity impact clinical use, especially in immunocompromised patients.

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Area of Science:

Pharmacology
Mycology
Drug Delivery

Background:

Amphotericin B is a broad-spectrum antifungal agent with significant in-vivo toxicity.
Various lipid formulations (lipid complexes, liposomes) have been developed to mitigate amphotericin B toxicity.
These formulations exhibit distinct pharmacokinetic and toxicity profiles.

Purpose of the Study:

To review the characteristics of different amphotericin B lipid formulations.
To compare their in-vitro and in-vivo antifungal activity, pharmacokinetics, and toxicity.
To discuss their clinical implications and potential in combination therapy.

Main Methods:

Review of preclinical and clinical studies on amphotericin B lipid formulations.
Comparison of pharmacokinetic data, tissue distribution, and toxicity profiles.
Evaluation of antifungal efficacy and therapeutic indices.

Main Results:

Lipid formulations demonstrate reduced toxicity compared to conventional amphotericin B.
Formulations vary in serum pharmacokinetics, tissue localization, and retention.
Despite similar in-vitro and in-vivo antifungal activity at comparable doses, toxicity profiles differ, impacting therapeutic indices.

Conclusions:

Amphotericin B lipid formulations offer improved safety profiles for treating fungal infections, particularly in high-risk patients.
Differences in formulation characteristics necessitate careful consideration for treatment selection and dosing.
These formulations are expected to remain crucial in antifungal therapy and combination regimens.