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

CALVO, N.; SVETAZ, L.; LAMAS, M. C.; LEONARDI, D.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Lugar: Basel; Año: 2019 vol. 20

1422-0067

Abstract: Among different Candida species triggering vaginal candidiasis, Candida albicans is the mostpredominant 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 aimof this research was to produce a novel chitosan nanocapsule based delivery system comprising of TIOor ECO and to study their suitability in vaginal application. These systems were characterized by theirphysicochemical properties, encapsulation efficiency, in vitro release, storage stability, cytotoxicity,and in vitro biological activity. Both nanocapsules loaded with TIO (average hydrodynamic size of146.8 ± 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% forECO). The analysis of size, polydispersity index, and zeta potential of the systems at 4, 25, and37 ◦C (over a period of two months) showed the stability of the systems. Finally, the developednanosystems presented fungicidal activity against C. albicans at non-toxic concentrations (studied onmodel human skin cells). The results obtained from this study are the first step in the development ofa pharmaceutical dosage form suitable for the treatment of vaginal candidiasis.