Formulation of Tioconazole and Melaleuca alternifolia Essential Oil Pickering Emulsions for Onychomycosis Topical Treatment.

Barbara Vörös-Horváth,Sándor Nagy,Sourav Das,Ala’ Salem,Szilárd Pál,Tamás Kőszegi,Andrea Böszörményi,Aleksandar Széchenyi

doi:10.3390/molecules25235544

Barbara Vörös-Horváth, Sándor Nagy + Show 6 more

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https://doi.org/10.3390/molecules25235544

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Abstract

Onychomycosis is a disease that affects many adults, whose treatment includes both oral and topical therapies with low cure rates. The topical therapy is less effective but causes fewer side effects. This is why the development of an effective, easy to apply formulation for topical treatment is of high importance. We have used a nanotechnological approach to formulate Pickering emulsions (PEs) with well-defined properties to achieve site-specific delivery for antifungal drug combination of tioconazole and Melaleuca alternifolia essential oil. Silica nanoparticles with tailored size and partially hydrophobic surface have been synthesized and used for the stabilization of PEs. In vitro diffusion studies have been performed to evaluate the drug delivery properties of PEs. Ethanolic solution (ES) and conventional emulsions (CE) have been used as reference drug formulations. The examination of the antifungal effect of PEs has been performed on Candida albicans and Trichophyton rubrum as main pathogens. In vitro microbiological experimental results suggest that PEs are better candidates for onychomycosis topical treatment than CE or ES of the examined drugs. The used drugs have shown a significant synergistic effect, and the combination with an effective drug delivery system can result in a promising drug form for the topical treatment of onychomycosis.

Highlights

Onychomycosis is a fungal infection of nails and nail bed and occurs on both finger and toenails.This fungal infection affects about 11.4% [1] of the adult population and is responsible for more than50% of nail diseases [2]
The TIO was chosen as a drug with high antifungal activity but low water solubility and permeability through the nail plate
The combination of the drugs applied in this study showed a significant synergistic effect

Summary

Introduction

Onychomycosis is a fungal infection of nails and nail bed and occurs on both finger and toenails.This fungal infection affects about 11.4% [1] of the adult population and is responsible for more than50% of nail diseases [2]. Onychomycosis is a fungal infection of nails and nail bed and occurs on both finger and toenails. This fungal infection affects about 11.4% [1] of the adult population and is responsible for more than. 50% of nail diseases [2]. For the treatment of onychomycosis, oral, topical, mechanical, and chemical therapies or a combination of these methods are used in practice [3]. The therapy is a long process (10–12 months) and has a poor cure rate [4]. Oral therapy is the most effective, but in the case of prolonged use, orally administered drugs can cause severe side effects because of their high toxicity [5].

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