As proven in clinical trials, superficial fungal infections can be effectively treated by single topical application of terbinafine hydrochloride (Ter-HCl) in a film forming system (FFS). Poly(lactic-co-glycolic acid) (PLGA) derivatives, originally synthesized with intention to get carriers with optimized properties for drug delivery, and multifunctional plasticizers - ethyl pyruvate, methyl salicylate, or triacetin - were used for formulation of Ter-HCl loaded FFSs. After spraying, a biodegradable, transparent, adhesive, and occlusive thin layer is formed on the skin, representing drug depot. In situ formed films were characterized by thermal, structural, viscoelastic, and antifungal properties as well as drug release and skin penetration. DSC and SEM showed fully amorphous films with Ter-HCl dissolved in PLGA in high concentration (up to 15%). FFSs are viscoelastic fluids with viscosity which can be easily adjusted by the type of plasticizer used and its concentration. The formulations showed excellent bioadhesion properties, thus ensuring persistence on the skin. In situ film based on branched PLGA/A plasticized with 10% of ethyl pyruvate allowed prolonged release of Ter-HCl by linear kinetics for the first 6 days with a total time of almost 14 days. During ex vivo human skin penetration experiment, Ter-HCl was found to be located only in its target layer, the epidermis. According to our results, plasticized branched PLGA derivatives loaded by Ter-HCl are suitable for the development of FFSs for superficial fungal infections treatment.

Department of Biological and Medical Sciences Charles University Faculty of Pharmacy in Hradec Kralove Akademika Heyrovskeho 1203 Hradec Kralove 500 05 Czech Republic

Department of Organic And Bioorganic Chemistry Charles University Faculty of Pharmacy in Hradec Kralove Akademika Heyrovskeho 1203 Hradec Kralove 500 05 Czech Republic

Department of Pharmaceutical Technology Charles University Faculty of Pharmacy in Hradec Kralove Akademika Heyrovskeho 1203 Hradec Kralove 500 05 Czech Republic

Department of Physics Faculty of Science University of Hradec Kralove Rokitanskeho 62 Hradec Kralove 500 03 Czech Republic

InStar Technologies a s Mrstikova 399 2a 460 07 Liberec Czech Republic

Institute of Pharmaceutical Technology and Regulatory Affairs Faculty of Pharmacy University of Szeged Eötvös u 6 H 6720 Szeged Hungary

Skin Barrier Research Group Charles University Faculty of Pharmacy in Hradec Kralove Akademika Heyrovskeho 1203 Hradec Kralove 500 05 Czech Republic

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