Formulation and antifungal performance of natamycin-loaded liposomal suspensions: the benefits of sterol-enrichment.

Autor: Bouaoud C; a DSM Food Specialties, DSM Biotechnology Center , Delft , The Netherlands .; b Faculty of Chemical Engineering , Delft University of Technology , Delft , The Netherlands , and., Lebouille JG; c DSM Biomedical , Chemelot, Geleen , The Netherlands., Mendes E; b Faculty of Chemical Engineering , Delft University of Technology , Delft , The Netherlands , and., De Braal HE; a DSM Food Specialties, DSM Biotechnology Center , Delft , The Netherlands ., Meesters GM; a DSM Food Specialties, DSM Biotechnology Center , Delft , The Netherlands .; b Faculty of Chemical Engineering , Delft University of Technology , Delft , The Netherlands , and.
Jazyk: angličtina
Zdroj: Journal of liposome research [J Liposome Res] 2016; Vol. 26 (2), pp. 103-12. Date of Electronic Publication: 2015 May 26.
DOI: 10.3109/08982104.2015.1046079
Abstrakt: The aim of this study is to develop and evaluate food-grade liposomal delivery systems for the antifungal compound natamycin. Liposomes made of various soybean lecithins are prepared by solvent injection, leading to small unilamellar vesicles (<130 nm) with controlled polydispersity, able to encapsulate natamycin without significant modification of their size characteristics. Presence of charged phospholipids and reduced content of phosphatidylcholine in the lecithin mixture are found to be beneficial for natamycin encapsulation, indicating electrostatic interactions of the preservative with the polar head of the phospholipids. The chemical instability of natamycin upon storage in these formulations is however significant and proves that uncontrolled leakage out of the liposomes occurs. Efficient prevention of natamycin degradation is obtained by incorporation of sterols (cholesterol, ergosterol) in the lipid mixture and is linked to higher entrapment levels and reduced permeability of the phospholipid membrane provided by the ordering effect of sterols. Comparable action of ergosterol is observed at concentrations 2.5-fold lower than cholesterol and attributed to a preferential interaction of natamycin-ergosterol as well as a higher control of membrane permeability. Fine-tuning of sterol concentration allows preparation of liposomal suspensions presenting modulated in vitro release kinetics rates and enhanced antifungal activity against the model yeast Saccharomyces cerevisiae.
Databáze: MEDLINE
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