title: Comparison of Characteristics of Two Topical Therapeutic Agents for Onychomycosis.
abstract: Two topical therapeutic agents were approved in Japan from 2015 to 2016, adding new options for onychomycosis therapy in the clinical field. In order to confirm the differences of formulation properties and nail pharmacokinetics between 5% luliconazole solution and 10% efinaconazole solution, drug concentration and antifungal activity in the nail were measured after topical treatment using human nail plates. In the in vitro permeation study, concentration of each drug was measured in the transversely sliced nail after single treatment with the two topical therapeutic agents. The results showed that concentration of luliconazole is higher than that of efinaconazole at all nail layers, differing by 1.7-8.4 times at each measurement point. Next, we examined antifungal activities of each drug in sliced nail after 14-day topical treatment. Mean rates of formation of inhibition zones for 5% luliconazole solution and 10% efinaconazole solution were 71.0% and 12.6%, respectively, and were statistically different. These results show that the two topical therapeutic agents have different properties, and suggest that 5% luliconazole solution has good nail permeation and retention characteristics. Moreover, luliconazole was found to retain enough antifungal activity in the nail plate against Trichophyton spp. after treatment with the topical agent.
authors.affiliation: R&D Laboratories, POLA PHARMA INC.
authors.forename: Tsuyoshi
authors.initials: T
authors.lastname: Shimamura
authors.forename: Akiko
authors.initials: A
authors.lastname: Miyamae
authors.forename: Ami
authors.initials: A
authors.lastname: Imai
authors.forename: Kozue
authors.initials: K
authors.lastname: Hirayanagi
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Iwanaga
authors.forename: Nobuo
authors.initials: N
authors.lastname: Kubota
authors.forename: Kazutoshi
authors.initials: K
authors.lastname: Shibuya
mesh_terms: D000287:Administration, Topical; D000935:Antifungal Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery / Q000639:trends; D025141:Drug Resistance, Fungal; D006801:Humans; D007093:Imidazoles / Q000493:pharmacokinetics* / Q000494:pharmacology*; D066298:In Vitro Techniques; D009262:Nails / Q000378:metabolism*; D014009:Onychomycosis / Q000188:drug therapy* / Q000382:microbiology; D012996:Solutions; D014230:Triazoles / Q000493:pharmacokinetics* / Q000494:pharmacology*; D014249:Trichophyton / Q000187:drug effects*
chemical_list: D000935:Antifungal Agents; D007093:Imidazoles; D012996:Solutions; D014230:Triazoles; C431707:efinaconazole; C112528:luliconazole