Amphotericin B microspheres: a therapeutic approach to minimize toxicity while maintaining antifungal efficacy.
Amphotericin B microsphere formulations with and without addition of polyethylene glycol 2000 in cross-linked bovine serum albumin were prepared. Amphotericin B microspheres were characterized for particle size (<5 microm), zeta potential (approximately 30 mV) and drug interaction by DSC and FTIR and were found to be stable formulations. Drug release profiles for these microspheres revealed that the release was primarily by diffusion. In vitro toxicity as assessed by release of haemoglobin and potassium demonstrated no toxic effect as compared with conventional solution formulation. Antifungal activity in vitro was comparable to solution formulation when tested by broth dilution method.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
Pawan K
PK
Angra
Carl
C
Oettinger
S
S
Balakrishna Pai
Martin J
MJ
D'Souza
D000666:Amphotericin B / Q000008:administration & dosage / Q000627:therapeutic use* / Q000633:toxicity; D000935:Antifungal Agents / Q000008:administration & dosage / Q000627:therapeutic use* / Q000633:toxicity; D002152:Calorimetry, Differential Scanning; D004912:Erythrocytes / Q000187:drug effects; D006801:Humans; D008863:Microspheres; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared
D000935:Antifungal Agents; D011092:Polyethylene Glycols; D000666:Amphotericin B