A comparison of in vitro toxicity and antifungal efficacy of membrane-active drugs after liposome encapsulation.
The membrane-active ionophores were observed to possess antifungal activity against Candida albicans 336 and were toxic to human erythrocytes. Liposome encapsulation of these drugs significantly reduced their toxicity to erythrocytes but resulted in the loss of their antifungal potency. These results are compared with membrane-active polyenes which maintained their antifungal activity after encapsulation into liposomes. Liposomal-ionophores, however, showed antifungal activity along with low concentrations of Amphotericin B indicating the presence of synergism between these drugs.
Mehta
R T
RT
Department of Pharmacology, University of Texas Medical, Houston.
Hopfer
R L
RL
Juliano
R L
RL
Lopez-Berestein
G
G
D000935:Antifungal Agents / Q000592:standards / Q000633:toxicity; D002462:Cell Membrane / Q000187:drug effects; D004337:Drug Carriers; D004339:Drug Compounding; D004912:Erythrocytes / Q000187:drug effects; D006096:Gramicidin / Q000633:toxicity; D006801:Humans; D007476:Ionophores / Q000008:administration & dosage / Q000494:pharmacology / Q000633:toxicity*; D008081:Liposomes; D011090:Polyenes / Q000633:toxicity
D000935:Antifungal Agents; D004337:Drug Carriers; D007476:Ionophores; D008081:Liposomes; D011090:Polyenes; D006096:Gramicidin