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.

The potential role of plant secondary metabolites on antifungal and immunomodulatory effect

“…Currently, antifungal targets have been identified for drugs that treat superficial or systemic fungal infections. Acrylamide targets the fungal enzyme squalene cyclooxylate and then blocks the synthesis of ergosterol, so that squalene accumulates on the cell membrane, increases the cell membrane brittleness, and leads to the rupture and death of fungal cells (Thapa et al 2015 ). Although triazole drugs are the most widely used antifungal drugs, with low hepatorenal toxicity, there is widespread triazole resistance among pathogenic fungi.…”

Penentuan Terbinafine Hidroklorida dalam Kosmetik Sediaan Pemutih Secara Kromatografi Cair Kinerja Tingg

“…Zat tersebut hanya diperbolehkan penggunaannya untuk tujuan pengobatan anti jamur, sehingga hanya dapat diperoleh dengan resep dokter. Saat ini ada beberapa produk kosmetika yang mengandung Terbinafine hidroklorida beredar di masyarakat [5] [6]. Pada Peraturan Menteri Kesehatan Republik Indonesia Nomor 3 Tahun 2021 yang telah ditetapkan tentang perubahan penggolongan, pembatasan dan kategori obat bahwa Terbinafine merupakan golongan obat bebas terbatas dengan pembatasan sebagai sediaan topikal anti jamur sistemik untuk kulit dengan kadar ≤ 1% [7].…”

Photostability of Terbinafine Under UVA Irradiation: The Effect of UV Absorbers

“…Terbinafine hydrochloride (TBF) is a synthetic allylamine antifungal agent which, due to its broad‐spectrum activity, is commonly used against dermatophytes, such as Trichophyton, Microsporum and Epidermophyton spp., and yeasts—especially Candida albicans and nondermatophyte molds . TBF is used orally, but extensive first‐pass metabolism and plasma protein binding at around 99% make the topical routes of administration (skin, fingernail or toenail) appear to be more attractive .…”