Effect of tissue penetration on AmBisome efficacy.
Amphotericin B reformulated into the liposomal formulation known as AmBisome (amphotericin B, hydrogenated soy phosphatidylcholine, cholesterol and dimyristoyl phosphatidylglycerol) can be safely administered at dosages 15 times higher than the conventional drug with the same broad spectrum of activity. Increased doses demonstrate non-linear clearance with saturation of the reticuloendothelial system (RES) and redistribution of the drug into non-RES tissues. The efficacy of this liposomal amphotericin B formulation appears to be related both to improved tissue penetration in the lungs, brain, kidneys, liver and spleen along with sustained bioactivity of therapeutic drug levels in these target tissues.
Adler-Moore
Jill
J
Department of Biological Sciences, California State Polytechnic University, Pomona, CA 91768, USA. jpadler@csupomona.edu
Proffitt
Richard T
RT
D000666:Amphotericin B / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D001927:Brain Diseases / Q000378:metabolism / Q000382:microbiology; D003881:Dermatomycoses / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D008107:Liver Diseases / Q000378:metabolism / Q000382:microbiology; D008172:Lung Diseases, Fungal / Q000188:drug therapy / Q000378:metabolism; D009181:Mycoses / Q000188:drug therapy / Q000378:metabolism / Q000517:prevention & control; D013158:Splenic Diseases / Q000188:drug therapy / Q000378:metabolism
D000935:Antifungal Agents; C068538:liposomal amphotericin B; D000666:Amphotericin B