Preparation, characterisation, and topical delivery of Terbinafine
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 proper...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI
2019
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| Online Access: | https://repository.londonmet.ac.uk/5225/1/pharmaceutics-11-00548.pdf |
| _version_ | 1824446417389748224 |
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| author | Hossain, Monjur Sil dos Santos, Bruno Iliopoulos, Fotis Lever, Rebecca Hadgraft, Jonathan Lane, Majella E. |
| author_facet | Hossain, Monjur Sil dos Santos, Bruno Iliopoulos, Fotis Lever, Rebecca Hadgraft, Jonathan Lane, Majella E. |
| author_sort | Hossain, Monjur |
| collection | LMU |
| 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. |
| first_indexed | 2024-07-09T03:59:05Z |
| format | Article |
| id | oai:repository.londonmet.ac.uk:5225 |
| institution | London Metropolitan University |
| language | English |
| last_indexed | 2024-07-09T03:59:05Z |
| publishDate | 2019 |
| publisher | MDPI |
| record_format | eprints |
| spelling | oai:repository.londonmet.ac.uk:52252019-12-02T11:04:48Z http://repository.londonmet.ac.uk/5225/ Preparation, characterisation, and topical delivery of Terbinafine Hossain, Monjur Sil dos Santos, Bruno Iliopoulos, Fotis Lever, Rebecca Hadgraft, Jonathan Lane, Majella E. 540 Chemistry & allied sciences 610 Medicine & health 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. MDPI 2019-10-21 Article PeerReviewed text en https://repository.londonmet.ac.uk/5225/1/pharmaceutics-11-00548.pdf 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 10.3390/pharmaceutics11100548 |
| spellingShingle | 540 Chemistry & allied sciences 610 Medicine & health Hossain, Monjur Sil dos Santos, Bruno Iliopoulos, Fotis Lever, Rebecca Hadgraft, Jonathan Lane, Majella E. Preparation, characterisation, and topical delivery of Terbinafine |
| title | Preparation, characterisation, and topical delivery of Terbinafine |
| title_full | Preparation, characterisation, and topical delivery of Terbinafine |
| title_fullStr | Preparation, characterisation, and topical delivery of Terbinafine |
| title_full_unstemmed | Preparation, characterisation, and topical delivery of Terbinafine |
| title_short | Preparation, characterisation, and topical delivery of Terbinafine |
| title_sort | preparation characterisation and topical delivery of terbinafine |
| topic | 540 Chemistry & allied sciences 610 Medicine & health |
| url | https://repository.londonmet.ac.uk/5225/1/pharmaceutics-11-00548.pdf |
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