Transdermal Delivery of Naltrexol and Skin Permeability Lifetime after Microneedle Treatment in Hairless Guinea Pigs |
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| Authors: | Stan L Banks Raghotham R Pinninti Harvinder S Gill Kalpana S Paudel Peter A Crooks Nicole K Brogden Mark R Prausnitz Audra L Stinchcomb |
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| Institution: | 1. Department of Pharmaceutical Sciences, University of Kentucky College of Pharmacy, Lexington, Kentucky 40536-0082;2. The Wallance Coulter School of Biomedical Engineering at Georgia Tech and Emory University, Georgia Institute of Technology, Atlanta, 30332-0363 Georgia;3. School of Chemical and Biomolecular Engineering, Georgia Institute of Technology, Atlanta, 30332-0100 Georgia |
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| Abstract: | Controlled-release delivery of 6-β-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeation enhancement of NTXOL’s hydrochloride salt in hairless guinea pigs. Specifically, these studies were designed to determine the lifetime of MN-created aqueous pore pathways. MN pore lifetime was estimated by pharmacokinetic evaluation, transepidermal water loss (TEWL) and visualization of MN-treated skin pore diameters using light microscopy. A 3.6-fold enhancement in steady-state plasma concentration was observed in vivo with MN treated skin with NTXOL HCl, as compared to NTXOL base. TEWL measurements and microscopic evaluation of stained MN-treated guinea pig skin indicated the presence of pores, suggesting a feasible nonlipid bilayer pathway for enhanced transdermal delivery. Overall, MN-assisted transdermal delivery appears viable for at least 48 h after MN-application. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:3072-3080, 2010 |
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