Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents

Among different Candida species triggering vaginal candidiasis, Candida albicans is the most predominant yeast. It is commonly treated using azole drugs such as Tioconazole (TIO) and Econazole (ECO). However, their low water solubility may affect their therapeutic efficiency. Therefore, the aim of t...

Authors: Calvo, Natalia L.
Sreekumar, Sruthi
Svetaz, Laura A.
Lamas, María C.
Moerschbacher, Bruno
Leonardi, Darío
Division/Institute:FB 13: Biologie
Document types:Article
Media types:Text
Publication date:2019
Date of publication on miami:01.07.2020
Modification date:21.08.2020
Edition statement:[Electronic ed.]
Source:International Journal of Molecular Sciences 20 (2019) 15, 3686, 1-16
Subjects:chitosan nanocapsules; drug delivery; anti-fungal; biological activity; vaginal candidiasis; econazole nitrate; tioconazole
DDC Subject:570: Biowissenschaften; Biologie
License:CC BY 4.0
Language:English
Funding:Finanziert durch den Open-Access-Publikationsfonds der Westfälischen Wilhelms-Universität Münster (WWU Münster).
Format:PDF document
URN:urn:nbn:de:hbz:6-50189603888
Permalink:http://nbn-resolving.de/urn:nbn:de:hbz:6-50189603888
Other Identifiers:DOI: 10.3390/ijms20153686
Digital documents:artikel_moerschbacher_2019.pdf
zusatzmaterial_moerschbacher_2019.pdf
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Among different Candida species triggering vaginal candidiasis, Candida albicans is the most predominant yeast. It is commonly treated using azole drugs such as Tioconazole (TIO) and Econazole (ECO). However, their low water solubility may affect their therapeutic efficiency. Therefore, the aim of this research was to produce a novel chitosan nanocapsule based delivery system comprising of TIO or ECO and to study their suitability in vaginal application. These systems were characterized by their physicochemical properties, encapsulation efficiency, in vitro release, storage stability, cytotoxicity, and in vitro biological activity. Both nanocapsules loaded with TIO (average hydrodynamic size of 146.8 ± 0.8 nm, zeta potential of +24.7 ± 1.1 mV) or ECO (average hydrodynamic size of 127.1 ± 1.5 nm, zeta potential of +33.0 ± 1.0 mV) showed excellent association efficiency (99% for TIO and 87% for ECO). The analysis of size, polydispersity index, and zeta potential of the systems at 4, 25, and 37 °C (over a period of two months) showed the stability of the systems. Finally, the developed nanosystems presented fungicidal activity against C. albicans at non-toxic concentrations (studied on model human skin cells). The results obtained from this study are the first step in the development of a pharmaceutical dosage form suitable for the treatment of vaginal candidiasis.