A novel method for predicting the efficacy of topical drugs on onychomycosis: A comparison of efinaconazole and luliconazole

Masumoto, Akane; Takagi, Masashi; Sugiura, Keita; Matsuda, Yoshiki; Nakamura, Saki; Tatsumi, Yoshiyuki

doi:10.1016/j.mycmed.2022.101259

Cited by 2 publications

(4 citation statements)

References 17 publications

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“…A broadspectrum antifungal drug called econazole nitrate is used to treat skin infections brought on by different pathogenic dermatophyte species. It is applied to treat candidiasis [4]. Fungal infections typically affect the mucous membranes, skin, hair, and nails, but they can also infect the lungs or other sections of your body.…”

Section: Introductionmentioning

confidence: 99%

Development and Characterization of Econazole Topical Gel

Bayan,

Chandrasekaran,

Alyami

2023

Gels

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The purpose of this work was to develop a novel topical formulation of econazole nitrate based on gel that can be easily scaled up in one pot for the potential treatment of fungal and yeast infections. Econazole nitrate, a topical antifungal, is used to treat tinea versicolor, tinea pedis, and tinea cruris. Compared to applying cream or ointment, topical gels offer numerous advantages, one of which is that the drug is released more quickly to the intended site of action. A viscous mixture of propylene glycol, Capmul® MCM C8, methyl and propyl paraben, and econazole nitrate were mixed together before being formulated into the optimized Carbopol® gel bases. The gel’s color, appearance, and homogeneity were assessed visually. For every formulation, the drug content, pH, viscosity, spreadability, and gel strength were characterized. The cup plate diffusion method was used to evaluate the anti-fungal activity of the prepared formulations. To assess the behavior of the developed system, studies on in vitro release and mechanism were conducted. The manufactured formulations were transparent, pale yellow, and exhibited excellent homogeneity. The pH of each formulation was roughly 6.0, making them suitable for topical use. The concentration of Carbopol® 940 resulted in a significant increase in viscosity and gel strength but a significant decrease in spreadability. It was demonstrated that the prepared formulations inhibited the growth of Candida albicans and Aspergillus fumigatus. In contrast, the standard blank gel showed no signs of antifungal action. By increasing the concentration of Carbopol® 940, the in vitro release profile of econazole nitrate significantly decreased. Following the Korsmeyer–Peppas model fitting, all formulations exhibited n values greater than 0.5 and less than 1, indicating that diffusion and gel swelling control econazole nitrate release.

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Section: Introductionmentioning

confidence: 99%

Development and Characterization of Econazole Topical Gel

Bayan,

Chandrasekaran,

Alyami

2023

Gels

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“…The drug’s therapeutic efficacy is determined by its permeability and antifungal activity in the nails [ 16 , 27 ]. In this study, luliconazole showed equal or higher nail concentrations than efinaconazole, presumably because of its higher keratin affinity.…”

Section: Discussionmentioning

confidence: 99%

“…Conversely, efinaconazole 10% solution was highly effective in reducing the nail fungal burden, whereas luliconazole 5% solution showed no 99% efficacy rate. Therefore, the effectiveness of efinaconazole was thought to be due to their different characteristics because efinaconazole has a lower keratin affinity and higher human nail permeability than luliconazole [ 16 , 27 ]. In addition, our recent study showed that there was a drug concentration gradient from the superficial to the internal part of the treated nails, and in the deeper nail layer, the antifungal activity and the amount of permeated efinaconazole were higher than those of permeated luliconazole [ 27 ].…”

Section: Discussionmentioning

confidence: 99%

“…Therefore, the effectiveness of efinaconazole was thought to be due to their different characteristics because efinaconazole has a lower keratin affinity and higher human nail permeability than luliconazole [ 16 , 27 ]. In addition, our recent study showed that there was a drug concentration gradient from the superficial to the internal part of the treated nails, and in the deeper nail layer, the antifungal activity and the amount of permeated efinaconazole were higher than those of permeated luliconazole [ 27 ]. Considering these, it was believed that efinaconazole 10% solution was more effective than luliconazole 5% solution in reducing the nail fungal burden and its therapeutic efficacy was less influenced by the duration of infection, which is unlikely with that of luliconazole 5% solution, presumably because efinaconazole reached the nail’s deep layer and killed the infecting fungi.…”

Section: Discussionmentioning

confidence: 99%

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Evaluation of Topical Antifungals Using a New Predictive Animal Model for Efficacy against Severe Tinea Unguium: A Comparison of Efinaconazole and Luliconazole

et al. 2022

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Development of new topical drugs requires an animal onychomycosis model that can predict the drug efficacy against moderate to severe human onychomycosis because the severity of onychomycosis varies and affects the drug efficacy. This study established a non-immunosuppressive guinea pig tinea unguium model under 8-week infection condition in addition to a previously reported model under 4-week infection condition. In the tinea unguium model, most fungi were tightly present in the arthrospore form, like in human onychomycosis. The topical formulations of efinaconazole and luliconazole, two azole class anti-onychomycosis drugs, were evaluated for their efficacy in these models. In the untreated group, the nail fungal burden in the 8-week model was higher than that in the 4-week model and the stronger infection intensity affected the efficacy of the drugs, suggesting that the 8-week model was more severe. The 90% efficacy rate (42%) of luliconazole in the 8-week model was significantly lowered than that (83%) in the 4-week model, and its 99% efficacy rates were 0% in both models. Conversely, the 90% and 99% efficacy rates of efinaconazole (92% and 50% in the 4-week model, and 75% and 25% in the 8-week model, respectively) were not significantly different between the two infection durations. In addition, efinaconazole was more effective than luliconazole in reducing the nail fungal burden. Considering the relevance of clinical reports of the effectiveness of efinaconazole on severe onychomycosis, the new severe tinea unguium model would predict drug efficacy against moderate to severe onychomycosis.

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A novel method for predicting the efficacy of topical drugs on onychomycosis: A comparison of efinaconazole and luliconazole

Cited by 2 publications

References 17 publications

Development and Characterization of Econazole Topical Gel

Development and Characterization of Econazole Topical Gel

Evaluation of Topical Antifungals Using a New Predictive Animal Model for Efficacy against Severe Tinea Unguium: A Comparison of Efinaconazole and Luliconazole

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