Antimicrobial Agents and Chemotherapy · 1989 · 46 citations · 11 references
Life SciencesMicrobiologyPharmacologyDrug DeliveryLipid BiochemistryMycologyAntifungal AgentsLipid BilayersLipid ChemistryLiposomal FormulationsMembrane Lipid CompositionOral CandidiasisCandida Albicans InfectionCholesterol Content In LiposomesFatty Acyl Chain LengthFungal Membrane LipidsLipid-based Antifungal FormulationsLiposome CharacterizationLiposomesSmall Unilamellar Vesicles
We compared the anticellular effects of liposomal amphotericin B (AmB) formed from AmB and small unilamellar vesicles. The small unilamellar vesicles with or without cholesterol were prepared from three L-alpha-phosphatidylcholines with saturated acyl chains of different lengths: distearoyl (C18), dipalmitoyl (C16), and dimyristoyl (C14). We found that the anticellular potency of liposomal AmB, compared with that of free AmB, decreased with decreasing length of the acyl chain of the phospholipid and increased with the addition of cholesterol. In a parallel study (S. Jullien, A. Vertut-Croquin, J. Brajtburg, and J. Bolard, Anal. Biochem. 172:197-202, 1988), we found that binding of AmB to vesicles decreased with increasing length of the acyl chain of the phospholipid and decreased with the addition of cholesterol. We conclude that the anticellular effects of liposomal AmB preparations are due to the levels of AmB remaining free (unbound to the lipids) in these preparations.
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