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Open AccessArticle

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

1
Instituto de Química Rosario (IQUIR, CONICET-UNR), Suipacha 531, Rosario S2002LRK, Argentina
2
Área Análisis de Medicamentos, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario S2002LRK, Argentina
3
Institute for Biology and Biotechnology of Plants (IBBP), Westfälische Wilhelms-Universität Münster, Schlossplatz 8, 48143 Münster, Germany
4
Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario S2002LRK, Argentina
5
Área Técnica Farmacéutica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario S2002LRK, Argentina
*
Authors to whom correspondence should be addressed.
N.L.C. and S.S. contributed equally to this work.
Int. J. Mol. Sci. 2019, 20(15), 3686; https://doi.org/10.3390/ijms20153686
Received: 11 June 2019 / Revised: 25 July 2019 / Accepted: 25 July 2019 / Published: 27 July 2019
(This article belongs to the Special Issue Chitosan-Based Nanoparticles)
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. View Full-Text
Keywords: chitosan nanocapsules; drug delivery; anti-fungal; biological activity; vaginal candidiasis; econazole nitrate; tioconazole chitosan nanocapsules; drug delivery; anti-fungal; biological activity; vaginal candidiasis; econazole nitrate; tioconazole
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Calvo, N.L.; Sreekumar, S.; Svetaz, L.A.; Lamas, M.C.; Moerschbacher, B.M.; Leonardi, D. Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents. Int. J. Mol. Sci. 2019, 20, 3686.

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