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Influence of net charge on the aggregation and solubility behaviour of amphotericin B and its derivatives in aqueous media

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Abstract

The poor solubility of polyene antibiotics in aqueous media limits their application in the therapy of systemic fungal infections. In the present paper we have demonstrated that the ionic state (net electrical charge) of the antibiotic molecule is an important factor in determining the aggregation and solubility properties of amphotericin B and its derivatives. A multi-step model of polyene self-association in aqueous media has been proposed as an explanation for the fact that some major differences are observed when aggregation is monitored by different techniques.

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Abbreviations

DMF:

dimethylformamide

DMSO:

dimethylsulphoxide

CD:

circular dichroism

MMC:

maximal monomer concentration

MSC:

maximal solute concentration

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Authors and Affiliations

  1. Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdańsk, PL-80-952, Gdańsk, Poland

    J. Mazerski, J. Grzybowska & E. Borowski

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  1. J. Mazerski
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  2. J. Grzybowska
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  3. E. Borowski
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Mazerski, J., Grzybowska, J. & Borowski, E. Influence of net charge on the aggregation and solubility behaviour of amphotericin B and its derivatives in aqueous media. Eur Biophys J 18, 159–164 (1990). https://doi.org/10.1007/BF02427375

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  • DOI: https://doi.org/10.1007/BF02427375

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