Abstract:
:Controlled-release delivery of 6-beta-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.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb ALdoi
10.1002/jps.22083subject
Has Abstractpub_date
2010-07-01 00:00:00pages
3072-80issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)32576-4journal_volume
99pub_type
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