Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs.

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 Sci

authors

Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb AL

doi

10.1002/jps.22083

subject

Has Abstract

pub_date

2010-07-01 00:00:00

pages

3072-80

issue

7

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)32576-4

journal_volume

99

pub_type

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