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Open AccessArticle

Preparation, Characterisation, and Topical Delivery of Terbinafine

1
UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UK
2
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka-1000, Bangladesh
3
Department of Pharmaceutical Science and Pharmacology, London Metropolitan University, 166–220 Holloway Road, London N7 8DB, UK
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(10), 548; https://doi.org/10.3390/pharmaceutics11100548
Received: 17 September 2019 / Revised: 15 October 2019 / Accepted: 16 October 2019 / Published: 22 October 2019
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. View Full-Text
Keywords: TBF; fungal infections; topical delivery; in vitro; porcine skin TBF; fungal infections; topical delivery; in vitro; porcine skin
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MDPI and ACS Style

Hossain, A.S.M.M.A.; Sil, B.C.; Iliopoulos, F.; Lever, R.; Hadgraft, J.; Lane, M.E. Preparation, Characterisation, and Topical Delivery of Terbinafine. Pharmaceutics 2019, 11, 548.

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