Amphotericin B Formulations and Drug Targeting

Amphotericin B is a low-soluble polyene antibiotic which is able to self-aggregate. The aggregation state can modify its activity and pharmacokinetical characteristics. In spite of its high toxicity it is still widely employed for the treatment of systemic fungal infections and parasitic disease and...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2008-07, Vol.97 (7), p.2405-2425
Main Authors: Torrado, J.J., Espada, R., Ballesteros, M.P., Torrado-Santiago, S.
Format: Article
Language:English
Subjects:
aggregation
amphotericin B
Amphotericin B - administration & dosage
Amphotericin B - chemistry
Amphotericin B - pharmacokinetics
Amphotericin B - toxicity
Animals
antifungal
Antifungal Agents - administration & dosage
Antifungal Agents - chemistry
Antifungal Agents - pharmacokinetics
Antifungal Agents - toxicity
Biological and medical sciences
Chemistry, Pharmaceutical
Drug Delivery Systems - methods
drug targeting
efficacy
General pharmacology
Humans
Kidney Diseases - chemically induced
leishmaniasis
Liposomes
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
pharmacokinetics
Pharmacology. Drug treatments
Solubility
toxicity
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Summary:Amphotericin B is a low-soluble polyene antibiotic which is able to self-aggregate. The aggregation state can modify its activity and pharmacokinetical characteristics. In spite of its high toxicity it is still widely employed for the treatment of systemic fungal infections and parasitic disease and different formulations are marketed. Some of these formulations, such as liposomal formulations, can be considered as classical examples of drug targeting. The pharmacokinetics, toxicity and activity are clearly dependent on the type of amphotericin B formulation. New drug delivery systems such as liposomes, nanospheres and microspheres can result in higher concentrations of AMB in the liver and spleen, but lower concentrations in kidney and lungs, so decreasing its toxicity. Moreover, the administration of these drug delivery systems can enhance the drug accessibility to organs and tissues (e.g., bone marrow) otherwise inaccessible to the free drug. During the last few years, new AMB formulations (AmBisome®, Abelcet®, and Amphotec®) with an improved efficacy/toxicity ratio have been marketed. This review compares the different formulations of amphotericin B in terms of pharmacokinetics, toxicity and activity and discusses the possible drug targeting effect of some of these new formulations.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.21179