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The Strathprints institutional repository is a digital archive of University of Strathclyde research outputs. Strathprints provides access to thousands of Open Access research papers by University of Strathclyde researchers, including those from the School of Psychological Sciences & Health - but also papers by researchers based within the Faculties of Science, Engineering, Humanities & Social Sciences, and from the Strathclyde Business School.

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Enhanced iontophoretic delivery of buspirone hydrochloride across human skin using chemical enhancers

Meidan, V.M. and Al-Khalili, M. and Michniak, B.B. (2003) Enhanced iontophoretic delivery of buspirone hydrochloride across human skin using chemical enhancers. International Journal of Pharmaceutics, 264 (1-2). pp. 73-83. ISSN 0378-5173

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Abstract

Buspirone hydrochloride (BH) is a structurally and pharmacologically unique anxiolytic that is used to treat a variety of different anxiety conditions. The marketed product is named BuSpar®. The in vitro iontophoretic delivery of BH through human skin was investigated in order to evaluate the feasibility of delivering a therapeutic dose of BH by this route. We also examined the influence of co-formulations of chemical enhancers (Azone®, oleic acid, menthone, cineole, and terpineol) on BH permeation, both without iontophoresis and with iontophoresis—to look for possible synergistic effects. By applying iontophoresis at 0.5 mA/cm2, it was possible to achieve a BH steady state flux of approximately 350 μg/cm2 h, which would be therapeutically effective if clinically duplicated. Importantly, 24 h of iontophoresis at 0.5 mA/cm2 did not affect skin morphology and after the current was switched off, the skin’s permeability to BH rapidly reverted to its pre-iontophoretic level. Without iontophoreis, BH transdermal flux was significantly enhanced by the application of 2.5% (v/v) concentrations of Azone®, oleic acid, or menthone but not cineole or terpineol. Furthermore, this paper identified a synergistic transport enhancement effect developing when very low current (0.025 mA/cm2) iontophoresis was applied in conjuction with Azone® treatment.