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Comparative in vitro Antifungal Activity of Amphotericin B Lipid Complex, Amphotericin B and Fluconazole

2000; Karger Publishers; Volume: 46; Issue: 4 Linguagem: Inglês

10.1159/000007295

1421-9794

Alfonso-Javier Carrillo-Muñoz, Guillermo Quindós, Cristina Tur Tur, Maite Ruesga, R. Rosas Alonso, Oscar del Valle, Virginia Rodríguez, María Pilar Arévalo, Javier Salgado, Estrella Martín‐Mazuelos, Fernando Jorge Bornay-Llinares, Amalia del Palacio, Marisol Cuétara, I Gasser, Juan Manuel Hernández-Molina, Javier Pemán,

Insects and Parasite Interactions

Amphotericin B (AMB) is considered the gold standard in the treatment of serious systemic mycoses in spite of its nephrotoxicity and adverse effects. Association with lipids enables larger doses of AMB to be given with a longer t_½ and C_max, without the toxic effects at lower concentrations. Liposome-encapsulated AMB shows a lower affinity for mammalian cells and improves V_d, thus decreasing toxicity. Amphotericin B lipid complex (ABLC) is an AMB formulation associated with a biodegradable phospholipid matrix (5% molar) from which the drug is released by cell phospholipases. ABLC is recommended for serious mycoses refractory to conventional antifungal therapy or when AMB is contraindicated. We compared the in vitro antifungal activity of ABLC, AMB and fluconazole (FLZ) against 328 strains of clinically significant opportunistic fungi using a microdilution method (NCCLS, M-27A). 64.9% of the yeasts were inhibited by MIC of ABLC ≤ AMB resulting in a similar or slightly superior efficacy compared to AMB when tested against <i>Candida albicans, C. glabrata, C. guilliermondii, C. parapsilosis</i> and <i>C. tropicalis.</i> Effectiveness against <i>C. krusei</i> was lower for ABLC (5.99 μg/ml for ABLC, 1.58 μg/ml for AMB). However, for <i>Aspergillus fumigatus,</i> the activities of AMB and ABLC were 1.62 and 2.46 μg/ml, respectively; <i>A. niger</i> 0.72 μg/ml, 0.76 μg/ml (ABLC and AMB, respectively); <i>A. clavatus, A. candidus, A. tenuissima, A. corymbifera</i> and <i>Exophiala jeanselmei, Scedosporium</i> spp. and <i>Miceliophtora</i> spp. showed a low susceptibility to both AMB formulations. ABLC is a useful alternative to AMB or FLZ for the treatment of severe fungal infections, due to the broad spectrum of antifungal actions observed in this study.