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

• Authors: Barbara Cybulska , Karolina Kupczyk , Joanna Szlinder-Richter , Edward Borowski
• Languages of publication: EN

Abstracts

EN

N-Methyl-N-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 phosphatidylcholine (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.

Keywords

EN

nontoxic antifungals; liposomal formulation; amphotericin B derivative; amphotericin B

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2002
• Volume: 49
• Issue: 1
• Pages: 67-75

Dates

published

2002

received

2001-09-10

revised

2002-01-20

accepted

2002-02-14

Contributors

author

Barbara Cybulska

• Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, 80-952 Gdańsk, Poland

author

Karolina Kupczyk

• Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, 80-952 Gdańsk, Poland

author

Joanna Szlinder-Richter

• Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, 80-952 Gdańsk, Poland

author

Edward Borowski

• Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, 80-952 Gdańsk, Poland

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