title: Terbinafine hydrochloride loaded liposome film formulation for treatment of onychomycosis: in vitro and in vivo evaluation.
abstract: Onychomycosis is a fungal infection of nail unit that is caused by dermatophytes. Oral Terbinafine hydrochloride (TBF-HCl) is being used for the treatment of onychomycosis since 24 years. The side effects caused by the systemic application and limitations of topical administration of this drug regarding the diffusion through nail lead to the development of a new formulation based on, TBF-HCl-loaded liposome. The newly obtained film formulations were prepared and characterized via several parameters, such as physical appearance, drug content, thickness, bioadhesive properties and tensile strength. In vitro and ex vivo permeation studies were performed to select an optimum film formulation for antifungal activity to show the efficiency of formulations regarding the treatment of onychomycosis. The in vitro release percentages of drug were found 71.6 ± 3.28, 54.4 ± 4.26, 56.1 ± 7.48 and 46.0 ± 2.43 for liposome loaded pullulan films (LI-P, LII-P) and liposome loaded Eudragit films (LI-E, LII-E), respectively. The accumulated drug in the nail plates were found 31.16 ± 4.22, 24.81 ± 5.35, 8.17 ± 1.81 and 8.92 ± 3.37 for LI-P, LII-P, LI-E and LII-E, respectively, which within therapeutic range for all film formulations. The accumulated drug in the nail plate was found within therapeutic range for all film formulations. The efficacy of the selected TBF-HCl-loaded liposome film formulation was compared with TBF-HCl-loaded liposome, ethosome, liposome poloxamer gel and ethosome chitosan gel formulations. It was found that TBF-HCl-loaded liposome film formulation had better antifungal activity on fungal nails which make this liposome film formulation promising for ungual therapy of fungal nail infection.
authors.affiliation: a Department of Pharmaceutical Technology, Faculty of Pharmacy , Ege University , Bornova , Turkey .
authors.forename: Sakine Tuncay
authors.initials: ST
authors.lastname: Tanrıverdi
authors.affiliation: b Department of Microbiology and Clinical Microbiology and.
authors.forename: Süleyha
authors.initials: S
authors.lastname: Hilmioğlu Polat
authors.affiliation: b Department of Microbiology and Clinical Microbiology and.
authors.forename: Dilek
authors.initials: D
authors.lastname: Yeşim Metin
authors.affiliation: c Department of Medical Pathology, Faculty of Medicine , Ege University , Bornova , Turkey.
authors.forename: Gülşen
authors.initials: G
authors.lastname: Kandiloğlu
authors.affiliation: a Department of Pharmaceutical Technology, Faculty of Pharmacy , Ege University , Bornova , Turkey .
authors.forename: Özgen
authors.initials: Ö
authors.lastname: Özer
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D005533:Foot Dermatoses / Q000188:drug therapy* / Q000473:pathology; D008081:Liposomes; D008297:Male; D008826:Microbial Sensitivity Tests; D009281:Naphthalenes / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D014009:Onychomycosis / Q000188:drug therapy* / Q000473:pathology; D011817:Rabbits; D000077291:Terbinafine; D014249:Trichophyton / Q000187:drug effects
chemical_list: D000935:Antifungal Agents; D008081:Liposomes; D009281:Naphthalenes; D000077291:Terbinafine
keywords: Film formulation; liposome; nail; onychomycosis; terbinafine hydrochloride; ungual delivery