In-vitro and in-vivo studies of the decrease of amphotericin B toxicity upon association with a triglyceride-rich...

The effects of amphotericin B associated with a triglyceride-rich emulsion (AB-emulsion), shown previously to behave like lymph chylomicrons, were evaluated in vitro and in vivo. Incorporation of amphotericin B to the emulsion was monitored by UV-visible spectrophotometry. Whilst conventional amphotericin B induced a considerable K+ efflux from erythrocytes, AB-emulsion had essentially no effect. In contrast, the K+ efflux from Candida albicans was similar upon incubation either with AB-emulsion or with conventional amphotericin B. Administration to rats showed reduced mortality due to AB-emulsion compared with conventional amphotericin B. Renal toxicity was also decreased upon AB-emulsion treatment, as evaluated by serum urea and creatinine levels. These data suggest that chylomicron-like emulsions could be utilized as vehicles for amphotericin B in antifungal therapy.