Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs.
Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs.
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DOI:
10.1002/jps.22083
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发表时间:
2010-07
影响因子:
3.8
通讯作者:
Stinchcomb, Audra L.
中科院分区:
文献类型:
--
作者:
Banks, Stan L.;Pinninti, Raghotham R.;Gill, Harvinder S.;Paudel, Kalpana S.;Crooks, Peter A.;Brogden, Nicole K.;Prausnitz, Mark R.;Stinchcomb, Audra L.
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. Microneedle 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 non-lipid bilayer pathway for enhanced transdermal delivery. Overall, MN-assisted transdermal delivery appears viable for at least 48 h after MN-application.
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DOI:
10.1073/pnas.2331316100
发表时间:
2003-11-25
影响因子:
11.1
作者:
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通讯作者:
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影响因子:
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DOI:
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发表时间:
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影响因子:
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作者:
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通讯作者:
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