article
Design and characterization of chitosan nanoformulations for the delivery of antifungal agents
Autor
Calvo, Natalia Lorena
Sreekumar, Sruthi
Svetaz, Laura
Lamas, María Celina
Moerschbacher, Bruno M.
Leonardi, Darío
Institución
Resumen
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. Para citar este articulo: 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. https://doi.org/10.3390/ijms20153686 Fil: Calvo, Natalia Lorena. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR -CONICET); Argentina. Fil: Calvo, Natalia Lorena. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área Análisis de Medicamentos; Argentina. Fil: Sreekumar, Sruthi. Westfälische Wilhelms-Universität Münster. Institute for Biology and Biotechnology of Plants (IBBP); Germany. Fil: Svetaz, Laura. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área Farmacognosia; Argentina. Fil: Lamas, María Celina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR -CONICET); Argentina. Fil: Lamas, María Celina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia. Área Técnica Farmacéutica; Argentina. Fil: Moerschbacher, Bruno M. Westfälische Wilhelms-Universität Münster. Institute for Biology and Biotechnology of Plants (IBBP); Germany. Fil: Leonardi, Darío. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR -CONICET); Argentina. Fil: Leonardi, Darío. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia. Área Técnica Farmacéutica; Argentina.