Abstract
The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN.
Highlights
Topical preparations containing different penetration enhancers were formulated to facilitate toenail delivery of EFN, and permeation profiles through the bovine hoof slice were evaluated in a Franz diffusion cell model
hydroalcoholic solutions (HSs) formulations containing different L-HSs were assessed for EFN delivery (Table 1)
Saner et al (2014) reported that these lipophilic ingredients altered the microstructure of the nail plate by interacting with its lipid components, promoting drug penetration and increasing the efficacy of topical therapies [16]
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Onychomycosis is one of the most chronic and prevalent nail disorders, caused by fungal infection. Epidemiological studies suggest about 19% of the global population is affected by onychomycosis caused by dermatophytes (Trichophyton rubrum and Trichophyton mentagrophytes), non-dermatophyte molds, and yeasts (Candida albicans) [1,2]. Efinaconazole (EFN, Figure 1), the first topical triazole derivative, is prescribed for the treatment of toenail onychomycosis. This antifungal agent has been demonstrated to be potent against
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