Preparation, characterisation, and topical delivery of Terbinafine

Hossain, Monjur, Sil dos Santos, Bruno, Iliopoulos, Fotis, Lever, Rebecca, Hadgraft, Jonathan and Lane, Majella E. (2019) Preparation, characterisation, and topical delivery of Terbinafine. Pharmaceutics, 11 (548). pp. 1-14. ISSN 1999-4923

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Abstract / Description

Terbinafine (TBF) is commonly used in the management of fungal infections of the skin because of its broad spectrum of activity. Currently, formulations containing the free base and salt form are available. However, there is only limited information in the literature about the physicochemical properties of this drug and its uptake by the skin. In this work, we conducted a comprehensive characterisation of TBF, and we also examined its percutaneous absorption in vitro in porcine skin. TBF-free base was synthesised from the hydrochloride salt by a simple proton displacement reaction. Both the free base and salt form were further analysed using Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). Delivery of TBF-free base in excised porcine skin was investigated from the following solvents: Isopropyl myristate (IPM), propylene glycol monolaurate (PGML), Transcutol® (TC), propylene glycol (PG), polyethylene glycol 200 (PEG 200), oleic acid (OL), ethanol (EtOH), and isopropyl alcohol (IPA). Permeation and mass balance studies confirmed that PG and TC were the most efficacious vehicles, delivering higher amounts of TBF-free base to the skin compared with a commercial gel (p < 0.05). These preliminary results are promising and will inform the development of more complex formulations in future work.

Item Type: Article
Uncontrolled Keywords: TBF; fungal infections; topical delivery; in vitro; porcine skin
Subjects: 500 Natural Sciences and Mathematics > 540 Chemistry & allied sciences
600 Technology > 610 Medicine & health
Department: School of Human Sciences
Depositing User: Bruno Da Silva sil dos santos
Date Deposited: 23 Oct 2019 08:18
Last Modified: 23 Oct 2019 08:18
URI: http://repository.londonmet.ac.uk/id/eprint/5225

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