Flux across [corrected] microneedle-treated skin is increased by increasing charge of naltrexone and naltrexol in vitro

S. L. Banks, R. R. Pinninti, Harvinder Gill, P. A. Crooks, M. R. Prausnitz, A. L. Stinchcomb

Research output: Contribution to journalArticlepeer-review

Abstract

PURPOSE: The purpose of this investigation was to evaluate the in vitro microneedle (MN) enhanced percutaneous absorption of naltrexone hydrochloride salt (NTX x HCl) compared to naltrexone base (NTX) in hairless guinea pig skin (GP) and human abdominal skin. In a second set of experiments, permeability of the major active metabolite 6-beta-naltrexol base (NTXOL) in the primarily unionized (unprotonated) form at pH 8.5 was compared to the ionized form (pH 4.5). METHODS: In vitro fluxes of NTX, NTX.HCl and ionized and unionized NTXOL were measured through microneedle treated or intact full thickness human and GP skin using a flow through diffusion apparatus. Solubility and diffusion samples were analyzed by HPLC. RESULTS: Both GP and human skin show significant increases in flux when treated with 100 MN insertions as compared to intact full thickness skin when treated with NTX.HCl or ionized NTXOL (pH 4.5; p < 0.05). MN increased GP skin permeability for the hydrophilic HCL salt of NTX
Original languageEnglish
Pages (from-to)1677-85
JournalPharm Res
StatePublished - 2008

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