In Vitro Antifungal Activity of Naftifine Hydrochloride against Dermatophytes

Abstract

bThe incidence of superficial dermatophytoses is high in developed countries, and there remains a need for effective topical antifungals. In this study, we evaluated the in vitro antifungal activity of naftifine hydrochloride, the active ingredient in naftifine hydrochloride cream and gel 1% and 2%, against dermatophytes. The MICs and minimum fungicidal concentrations (MFCs) of naftifine hydrochloride against 350 clinical strains, including Trichophyton rubrum, T. mentagrophytes, T. tonsurans, Epidermophyton floccosum, and Microsporum canis, were determined using the CLSI methodology. Subsets from this test panel were subsequently tested in a time-kill assay at 0.125؋, 0.25؋, 0.5؋, and 1؋ the MFC for each isolate. CFU counts were performed over a period of 48 h of incubation. Additionally, in order to determine the potential for resistance development, six strains were subjected to 15 serial passages in concentrations higher than the MIC for each strain. MICs were determined following each passage. The MIC range against the dermatophyte isolates tested was 0.015 to 1.0 g/ml, with naftifine hydrochloride being fungicidal against 85% of the Trichophyton species. The time-kill assay showed dose-dependent activity, with the greatest reduction in the numbers of CFU corresponding to the highest drug concentration. There was no increase in MIC for any strains following repeated exposure to naftifine hydrochloride. Naftifine hydrochloride demonstrated potent activity against all dermatophytes tested, and none of the isolates within this test panel demonstrated the potential for the development of resistance. Thus, future clinical studies of naftifine hydrochloride against dermatophytes may be warranted for the treatment of superficial dermatophytoses.

Imidazolium salts with antifungal potential against multidrug-resistant dermatophytes

“…At these concentrations, especially C 16 MImMeS promoted a quick (complete fungal death in 1 h) and long-lasting fungal death (48 h) for all studied dermatophytes. The performance presented by this IMS is far superior to those presented in recent studies in the literature, using Melaleuca alternifolia oil, naftifine hydrochloride and a synthetic analogue of protegrin peptide, as fungicides against dermatophytes (Hammer et al 2002;Ghannoum et al 2013;Simonetti et al 2014). The IMS C 16 MImCl, C 16 MImMeS and C 16 MImNTf 2 cause micromorphological damage on the dermatophytes cells, which seems to be originated from a type of osmotic stress, followed by de-structuring of the TME hyphae.…”

Rapid tools to gain insights into the interaction dynamics of new 8‐hydroxyquinolines with few fungal lines

“…So, the dynamic changes in growth and susceptibility over the studied time period are not taken into account (Nielsen & Friberg, 2013;Treyaprasert, Schmidt, Rand, Suvanakoot, & Derendorf, 2007). On the other hand, time-kill curves are increasingly used to offer detailed information about antimicrobial efficacy as a function of both time and concentration (Ghannoum et al, 2013;Gupta, Paquet, & Simpson, 2013). In addition, pharmacokinetic/pharmacodynamic (PK/PD) modeling has become a powerful tool to evaluate the antimicrobial effect (Bulitta et al, 2010;Nielsen et al, 2007;Treyaprasert et al, 2007).…”

Rationale for selection of a topical antimycotic agent

“…Изучению чувстви-тельности дерматофитов к нафтифину посвящено исследование M. Ghannoum и соавт. [39], в котором показано отсутствие формирования устойчивости к препарату. Для получения резистентных штаммов было проведено длительное культивирование 6 наи-более распространенных в мире штаммов дермато-фитов в присутствии высокой дозы нафтифина.…”

“…(к 81% штаммов T. mentagrophytes, к 74% -T. tonsurans и к 96% штаммов T. rubrum). Фунгиста-тическая активность сохранялась в отношении 72% штаммов E. floccosum и 83% протестированных штаммов M. canis [39].…”