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Triclosan: release from transdermal adhesive formulations and in vitro permeation across human epidermal membranes

Chedgzoy, P., Winckle, Gareth and Heard, Charles Martin ORCID: 2002. Triclosan: release from transdermal adhesive formulations and in vitro permeation across human epidermal membranes. International Journal of Pharmaceutics 235 (1-2) , pp. 229-236. 10.1016/S0378-5173(01)00992-9

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Malarial resistance is an escalating global problem and consequently new and more efficacious treatments to combat malaria are urgently needed. The transdermal delivery of anti-malarials may provide an effective alternative or adjunct to conventional regimens. Triclosan is widely used as an anti-bacterial agent and it has recently been demonstrated that this compound has anti-malarial properties. Its high lipophilicity makes it a potential candidate for delivery across the skin and this paper examines in vitro the potential for the transdermal delivery of triclosan from ‘drug-in-glue’ formulations. Model patches were prepared using DuroTak® 2287, 2516 and 2051 acrylic polymer adhesives loaded with 0, 30 and 50 mg per 0.785 cm−2 triclosan and dissolution was measured over a 12-h period. There was no apparent difference between the adhesives at the 30 mg patch loading, but at 50 mg, the trend for increased release was 2051>2516>2287. No significant burst effect was apparent. Patches of 50 mg per 0.785 cm2 were then used to determine the permeation of triclosan across heat-separated human epidermal membranes in Franz diffusion cells, over a period of 48 h. The above general trend was reflected in the steady state flux values obtained: 2051:16.91 μg cm−2 h−1 (S.E.M. 1.29), 2516:15.05 μg cm−2 h−1 (S.E.M. 1.00), 2287 12.83 μg cm−2 h−1 (S.E.M. 2.81). Although pharmacokinetic data are not currently available to permit calculation of an efficacious patch size, the transdermal delivery of triclosan is feasible.

Item Type: Article
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: Elsevier
ISSN: 0378-5173
Last Modified: 27 Oct 2022 09:43

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