The effects of serum albumin on the aggregation state and toxicity of amphotericin B

摘要

Amphotericin B (AmB), a heptaene macrolide antibiotic, is widely used for treatment of systemic fungal disease. Despite widespread use, especially among immunocompromised patients, serious side effects of this membrane-active drug including nephrotoxicity limit its efficacy. The chemical modification of AmB has not yielded less toxic derivatives. Several lipid-based systems of AmB have shown reduced toxicity and have been approved for use in humans. However, an improved therapeutic index of lipid-based AmB has yet to be firmly established, especially in light of the necessity of higher doses of AmB and the favored disposition of lipid-based AmB at the liver, which could lead to long-term toxicity.