An Emulsion Formulation of Amphotericin B Improves the Therapeutic Index When Treating Systemic Murine Candidiasis

The maximal tolerated dose (MTD) in mice was 1 mg of Fungizone/kg; however, the MTD was ^ mg of the Intralipid? emulsion formulation/kg. The emulsion formulation and Fungizone were equipotent for treating systemic candidiasis in mice. Amphotericin B nephrotoxicity, as manifested by polyuria that was resistant to antidiuretic hormone, was markedly diminished when amphotericin B was administered as an emulsion to rats. Loss of potassium from human red blood cells was also reduced by formulating this agent within emulsions. The emulsion formulation extended the survival time of mice that had established Candida albicans infections, when compared with the Fungizone treatment. The efficacy and reduced toxicity of the amphotericin B emulsion are findings suggesting that the emulsion formulation is preferable to Fungizone.