Background: Cutaneous candidiasis is a deep-seated skin fungal infection that
is most commonly observed in immunocompromised patients. This fungal infection is
conventionally treated with various formulations like gels and creams which are having
different side effects and the least therapeutic efficacy. Hence, it becomes necessary to
develop a novel carrier system for the treatment of this deep-seated skin fungal infection.
Econazole nitrate is the most widely used antifungal for the treatment of cutaneous candidiasis
and many patents have been granted by various pharmaceutical scientists around
the globe related to nanocarrier systems for transdermal delivery of antifungal drugs like
econazole nitrate (ECN) therefore, we developed and evaluated econazole nitrate loaded
oleic acid vesicles in the present research work for treatment of cutaneous candidiasis
through transdermal route.
Methods: Econazole nitrate loaded oleic acid vesicles were prepared by thin-film hydration
and characterized for drug entrapment, vesicle size, zeta potential, polydispersity index
(PDI), Fourier Transform-infrared spectroscopy (FT-IR), differential scanning
calorimetry (DSC), and X-ray diffraction (XRD) analysis. Furthermore, the oleic acid
vesicular gel was evaluated for ex-vivo skin permeation/retention and in-vitro and in-vivo
antifungal activity in Wistar rats.
Results: Econazole nitrate loaded oleic acid vesicles showed high encapsulation of drug
(74.76 ± 3.0%), acceptable size (373.4 ± 2.9 nm), and colloidal characteristics (PDI =
0.231 ± 0.078, and zeta potential = -13.27 ± 0.80 mV). The oleic acid vesicular gel
showed high skin permeation (Transdermal flux = 61.98 ± 2.45 μg/cm2/h), skin retention
(35.90 ± 2.06%), in-vitro, and in-vivo antifungal activity compared to marketed cream (Ecoderm
R) of econazole nitrate for a prolonged time (4 days).
Conclusion: Developed econazole nitrate loaded oleic acid vesicles could be used effectively
in the treatment of cutaneous candidiasis with minimization of side effects of econazole
nitrate with increased therapeutic efficacy.