DA 5505: A Novel Topical Formulation of Terbinafine That Enhances Skin Penetration and Retention
| Autor: | Miwon Son, Hyoung Geun Park, Joon Ho Jun, Jong Oh Kim, Raj Kumar Thapa, Sang-Duk Han |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Antifungal
Antifungal Agents Swine medicine.drug_class Chemistry Pharmaceutical Mice Nude Naphthalenes Pharmacology Administration Cutaneous Chitosan Mice chemistry.chemical_compound Lag time Drug Stability Drug Discovery medicine Animals Terbinafine Skin Mice Inbred BALB C Ergosterol integumentary system General Chemistry General Medicine Penetration (firestop) Permeation chemistry Skin penetration medicine.drug |
| Zdroj: | CHEMICAL & PHARMACEUTICAL BULLETIN. 63:525-530 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.c15-00108 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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