Ciclopirox and Efinaconazole Transungual Permeation, Antifungal Activity, and Proficiency To Induce Resistance in Trichophyton rubrum.
Onychomycosis is a nail fungal infection, mostly caused by dermatophytes. The treatment efficacy is impaired by difficulties of reaching effective drug levels at the site of infection; frequent relapses occur after cessation of antifungal therapy. The aim of the study was to compare two commercial products containing ciclopirox or efinaconazole for antimycotic activity and antifungal drug resistance. A study of permeation and penetration through bovine hoof membranes, as a nail model, was performed to evaluate the antimycotic activity of permeates against clinical isolates of selected fungi, and the frequency of spontaneous in vitro Trichophyton rubrum-resistant strains was assessed by broth microdilution assays. The results suggest that ciclopirox creates a depot in the nail, leading to a gradual release of the drug over time with action on both the nail plate and bed. Conversely, efinaconazole, mildly interacting with nail keratin, mainly exerts its antifungal activity in the nail bed. However, in the case of T. rubrum, the antifungal activities of the drugs in the nail plate seem comparable. Finally, efinaconazole showed a potential for induction of resistance in T. rubrum, which may limit its efficacy over time. Ciclopirox did not show any potential to induce resistance in T. rubrum and appears endowed with a more complete activity than efinaconazole in the management of onychomycosis as the nail keratin is a substrate for the growth of fungal cells, and the availability of drug in large concentration just in the nail bed may not be sufficient to guarantee the complete eradication of pathogens.
['Monti|Daniela|D|', 'Mazzantini|Diletta|D|', 'Tampucci|Silvia|S|0000-0002-8927-6083', 'Vecchione|Alessandra|A|', 'Celandroni|Francesco|F|', 'Burgalassi|Susi|S|', 'Ghelardi|Emilia|E|']
D000818:Animals D000935:Antifungal Agents D001692:Biological Transport D002417:Cattle D000077768:Ciclopirox D025141:Drug Resistance, Fungal D006724:Hoof and Claw D006801:Humans D007633:Keratins D008826:Microbial Sensitivity Tests D008867:Microtomy D008954:Models, Biological D009154:Mutation D009262:Nails D010539:Permeability D011485:Protein Binding D014005:Tinea D014230:Triazoles D014249:Trichophyton
ciclopirox efinaconazole transungual permeation Trichophyton rubrum bovine hoof membranes antifungal resistance