title: Triclosan: release from transdermal adhesive formulations and in vitro permeation across human epidermal membranes.
abstract: 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 microg x cm(-2) x h(-1) (S.E.M. 1.29), 2516:15.05 microg x cm(-2) x h(-1) (S.E.M. 1.00), 2287 12.83 microg x cm(-2) x 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.
authors.affiliation: Welsh School of Pharmacy, Cardiff University, CF10 3XF, Cardiff, UK.
authors.forename: Paula
authors.initials: P
authors.lastname: Chedgzoy
authors.forename: Gareth
authors.initials: G
authors.lastname: Winckle
authors.forename: Charles M
authors.initials: CM
authors.lastname: Heard
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000279:Administration, Cutaneous; D000328:Adult; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D004817:Epidermis / Q000378:metabolism*; D005260:Female; D006801:Humans; D010539:Permeability / Q000187:drug effects; D014260:Triclosan / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D000269:Adhesives; D000891:Anti-Infective Agents, Local; D014260:Triclosan