title: DA 5505: a novel topical formulation of terbinafine that enhances skin penetration and retention.
abstract: Topical fungal infections can become severe if left untreated. Efficient treatment modalities for topical fungal infections aid the penetration of antifungal agents deep into viable skin layers. Terbinafine is a fungicidal agent that inhibits ergosterol, an essential fungal component. The main objective of this study was to evaluate skin permeation and retention of a terbinafine-loaded solution containing chitosan as a film former. Comparative assessment of skin permeation and retention was performed using a prepared formulation (DA 5505) and marketed formulations of terbinafine in murine and porcine skin. To mimic fungal infection of skin, keratinized skin was induced in NC/Nga mice. In comparison with the marketed formulations, DA 5505 exhibited significantly better skin permeation. The flux, permeation coefficient, and enhancement ratio of terbinafine were remarkably increased by DA 5505 in comparison with the marketed formulations, and lag time was dramatically reduced. DA 5505 significantly increased cumulative terbinafine retention in viable skin layers in comparison with the marketed solution, suggesting enhanced efficacy. Furthermore, DA 5505 exhibited superior skin permeation in normal skin and keratinized skin. Thus, the DA 5505 formulation has the potential to effectively deliver terbinafine to superficial and deep cutaneous fungal infections.
authors.affiliation: College of Pharmacy, Yeungnam University.
authors.forename: Raj Kumar
authors.initials: RK
authors.lastname: Thapa
authors.forename: Sang-Duk
authors.initials: SD
authors.lastname: Han
authors.forename: Hyoung Geun
authors.initials: HG
authors.lastname: Park
authors.forename: Miwon
authors.initials: M
authors.lastname: Son
authors.forename: Joon Ho
authors.initials: JH
authors.lastname: Jun
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical; D004355:Drug Stability; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009281:Naphthalenes / Q000737:chemistry* / Q000494:pharmacology; D012867:Skin / Q000187:drug effects / Q000378:metabolism* / Q000473:pathology; D013552:Swine; D000077291:Terbinafine
chemical_list: D000935:Antifungal Agents; D009281:Naphthalenes; D000077291:Terbinafine