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Oleic Acid Vesicles as a new Approach for Transdermal Delivery of Econazole Nitrate: Development, Characterization,
Shivani Verma1,2, Puneet Utreja3,4
1Department of Pharmaceutics, Rayat-Bahra College of Pharmacy, Hoshiarpur, Punjab 146001, India;
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 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, therefore, in present research work we developed and evaluated econazole nitrate loaded oleic acid vesicles 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), 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, 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 (EcodermR) of econazole nitrate for a prolonged period of 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.
Insights
Novel oleic acid vesicles effectively treat cutaneous candidiasis, a deep fungal skin infection. This econazole nitrate delivery system enhances therapeutic efficacy and reduces side effects compared to conventional creams.
Area of Science:
- Dermatology
- Pharmaceutics
- Nanotechnology
Background:
- Cutaneous candidiasis is a deep fungal skin infection, often affecting immunocompromised individuals.
- Conventional treatments like gels and creams have limited efficacy and side effects.
- Novel drug delivery systems are needed for improved treatment of this infection.
Purpose of the Study:
- To develop and evaluate econazole nitrate-loaded oleic acid vesicles for transdermal treatment of cutaneous candidiasis.
- To assess the potential of this novel formulation for enhanced therapeutic efficacy and reduced side effects.
Main Methods:
- Econazole nitrate-loaded oleic acid vesicles were prepared using thin-film hydration.
- Characterization included drug entrapment, vesicle size, zeta potential, PDI, FT-IR, DSC, and XRD.
- Ex-vivo skin permeation/retention and in-vitro/in-vivo antifungal activity were evaluated.
Main Results:
- Vesicles demonstrated high drug encapsulation (74.76%) and suitable colloidal properties (size: 373.4 nm, PDI: 0.231, zeta potential: -13.27 mV).
- The vesicular gel exhibited significant skin permeation (61.98 μg/cm²/h) and retention (35.90%).
- Both in-vitro and in-vivo antifungal activity were superior to a marketed econazole nitrate cream over 4 days.
Conclusions:
- Econazole nitrate-loaded oleic acid vesicles offer an effective treatment for cutaneous candidiasis.
- This novel system has the potential to minimize side effects and increase therapeutic efficacy.
- The transdermal delivery of econazole nitrate via oleic acid vesicles shows promise for managing deep fungal skin infections.
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