The oral delivery of amphotericin B

摘要

Amphotericin B (AmB) is a broad-spectrum antifungal agent with a low incidence of clinical resistances and is also indicated in the treatment of leishmaniasis. AmB is a zwitterionic amphiphilic molecule characterized by its low oral bioavailability. Therefore, in clinical practice, AmB oral administration is restricted to situations in which local action is desired; that is, in order to prevent nosocomial infections in the oesophageol and GI tract. With oral dosing, the systemic toxicity of AmB is usually avoided due to its low oral absorption. After oral administration of AmB lozenges at a dose of 40 mg per day or following oral rinsing with suspensions at a dose of 500 mg four-times a day, a maximum AmB plasma concentration of between 0.136 and 0.5 ug ml~(-1) has been reported [1,2].