Comparative in vitro studies on liposomal formulations of amphotericin B and its derivative, N-methyl-N-D-fructosyl amphotericin B methyl ester [MFAME]

• Autorzy: Cybulska B. , Kupczyk K. , Szlinder-Richert J. , Borowski E.
• Języki publikacji: EN

Abstrakty

EN

N-Methyl-W-D-fructosyl amphotericin B methyl ester (MFAME) is a semisynthetic de­rivative of the antifungal antibiotic amphotericin B (AMB). In contrast to the parent antibiotic, the derivative is characterised by low toxicity to mammalian cells and good solubility in water of its salts. Comparative studies on biological properties of free MFAME, AMB and their liposomal formulations were performed. To obtain liposomal forms, the antibiotics were incorporated into small unilamellar vesicles composed of dimyristoyl phos- phatidylcholine (DMPC) and DMPC: cholesterol or ergosterol, 8:2 molar ratio. The effectivity of the liposomal and free forms of AMB and MFAME were compared by de­termination of fungistatic and fungicidal activity against Candida albicans ATCC 10261, potassium release from erythrocytes, and haemolysis. The results obtained indicate that in contrast to AMB, incorporation of MFAME into liposomes did not further improve its selective toxicity. Studies on the antagonistic effect of ergosterol and cholesterol on the antifungal ac­tivity of the antibiotics indicated that sterol interference was definitely less pro­nounced in the case of MFAME than in the case of AMB.

Słowa kluczowe

EN

fungicidal activity; amphotericin B derivative; fungistatic activity; treatment; dimyristoyl phosphatidylcholine; antibiotic; non-toxic drug; Candida albicans; in vitro; liposomal formulation

• Wydawca: -
• Czasopismo: Acta Biochimica Polonica
• Rocznik: 2002
• Tom: 49
• Numer: 1
• Opis fizyczny: p.67-75,fig.

Twórcy

autor

Cybulska B.

• Technical University of Gdansk, Gdansk, Poland

autor

Kupczyk K.

autor

Szlinder-Richert J.

autor

Borowski E.

Bibliografia

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