Pharmacokinetic and biodistribution studies of amphotericin B microspheres.
The pharmacokinetics of Amphotericin B (AmB) from polyethylene glycol 2000 (PEG 2000) entrapped cross-linked bovine serum albumin (BSA) microsphere formulations were investigated and compared with solution formulation. The microsphere preparations were characterized for particle size using electron microscopy, zeta potential and encapsulation efficiency. The microsphere formulations demonstrated a sustained release of AmB for a longer period of time, with no rise in plasma creatinine and potassium levels. The enhanced AmB accumulation in lungs was observed which could be of importance since lungs are the primary target in most fungal infections. The stealth property of submicron cross-linked BSA microspheres in formulations containing PEG 2000 (formulation F-2N) and without PEG 2000 (formulation F-1N) was also evaluated. There was no evidence that microspheres embedded with PEG remained longer in circulation; however, it was noticed that the internalization of formulation F-2N microspheres was delayed when compared with microspheres from formulation F-1N.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
Pawan K
PK
Angra
Aladin
A
Siddig
Henry
H
Nettey
Nishil
N
Desai
Carl
C
Oettinger
Martin J
MJ
D'Souza
D000666:Amphotericin B / Q000493:pharmacokinetics*; D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D008168:Lung / Q000378:metabolism; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D051381:Rats; D014018:Tissue Distribution
D000935:Antifungal Agents; D000666:Amphotericin B