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Transdermal Delivery of Naltrexol and Skin Permeability Lifetime after Microneedle Treatment in Hairless Guinea Pigs
Journal article   Peer reviewed

Transdermal Delivery of Naltrexol and Skin Permeability Lifetime after Microneedle Treatment in Hairless Guinea Pigs

Stan L Banks, Raghotham R Pinninti, Harvinder S Gill, Kalpana S Paudel, Peter A Crooks, Nicole K Brogden, Mark R Prausnitz and Audra L Stinchcomb
Journal of pharmaceutical sciences, Vol.99(7), pp.3072-3080
07/2010
DOI: 10.1002/jps.22083
PMCID: PMC2862091
PMID: 20166200

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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 48h after MN-application. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:3072-3080, 2010
microneedle 6-β-naltrexol addiction therapy transdermal hairless guinea pig

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