In-vitro evaluation of the antifungal activity of amphotericin B entrapped into liposomes during storage for one year

The stability of the antifungal activity of amphotericin B entrapped in small sonicated liposomes (ampholiposomes) was studied in vitro over a one-year period. Preparations of ampholiposomes stored at −20°C or at 4°C were compared monthly with freshly-prepared ampholiposomes and a commercial prepara...

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Veröffentlicht in:Journal of antimicrobial chemotherapy 1990-03, Vol.25 (3), p.361-366
Hauptverfasser: Heymans, C., Van der Auwera, P., Sculier, J. P., Coune, A., Brassinne, C., Laduron, C., Hollaert, C., Meunier, F.
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container_end_page 366
container_issue 3
container_start_page 361
container_title Journal of antimicrobial chemotherapy
container_volume 25
creator Heymans, C.
Van der Auwera, P.
Sculier, J. P.
Coune, A.
Brassinne, C.
Laduron, C.
Hollaert, C.
Meunier, F.
description The stability of the antifungal activity of amphotericin B entrapped in small sonicated liposomes (ampholiposomes) was studied in vitro over a one-year period. Preparations of ampholiposomes stored at −20°C or at 4°C were compared monthly with freshly-prepared ampholiposomes and a commercial preparation of amphotericin B-deoxycholate (Fungizone; Squibb) by a killing curve method with Candida albicans. The bioactivity of the four preparations, each containing 1·5 or 2 mg/l of amphotericin B, was measured as the initial rate of killing and the ‘relative bioactivity’. Relative bioactivity was calculated as the percentage reduction of the area under the growth curve compared with control growth. Storage of ampholiposomes for one year did not decrease their antifungal activity. Storage of ampholiposomes containing 1·5 mg/l amphotericin B for one year at −20°C, but not at 4°C, gave a significant increase in relative bioactivity and killing rate in comparison with freshly-prepared ampholiposomes. This was probably due to modifications in the spatial configuration of phospholipids and amphotericin B. The persisting antifungal activity of ampholiposomes stored for one year should allow the preparation of large batches to perform comparative clinical studies.
doi_str_mv 10.1093/jac/25.3.361
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subjects Amphotericin B - administration & dosage
Amphotericin B - pharmacology
Biological and medical sciences
Candida albicans
Drug Carriers
Drug Stability
Drug Storage
General pharmacology
Liposomes
Medical sciences
Microbial Sensitivity Tests
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Time Factors
title In-vitro evaluation of the antifungal activity of amphotericin B entrapped into liposomes during storage for one year
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