Journal article
Permeation and Systemic Absorption of R- and S-baclofen Across the Nasal Mucosa
Journal of pharmaceutical sciences, Vol.100(7), pp.2717-2723
07/01/2011
DOI: 10.1002/jps.22499
PMCID: PMC4315361
PMID: 21283988
Abstract
Baclofen, an antispasmodic agent that acts as a GABA(B) agonist, resembles phenylalanine in structure and has been reported to be a substrate of the large amino acid transporter 1 (LAT-1). The objective of this study was to investigate the absorption of baclofen across the nasal mucosa both in vitro and in vivo. Baclofen transport was measured across excised bovine olfactory and respiratory mucosae to investigate site-specific uptake of baclofen, and the intranasal bioavailability of R- and S-baclofen was determined in rats. Increasing flux with increasing baclofen donor concentration and the absence of polarized transport was observed in vitro, and similar distribution profiles were observed for both enantiomers following intranasal administration in rats. The absence of stereospecificity in nasal absorption indicates limited involvement of the amino acid or other transporters in the nasal absorption of baclofen. (C) 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100: 2717-2723, 2011
Details
- Title: Subtitle
- Permeation and Systemic Absorption of R- and S-baclofen Across the Nasal Mucosa
- Creators
- Hefei Zhang - University of IowaMark Schmidt - University of IowaDaryl J. Murry - University of IowaMaureen D. Donovan - University of Iowa
- Resource Type
- Journal article
- Publication Details
- Journal of pharmaceutical sciences, Vol.100(7), pp.2717-2723
- DOI
- 10.1002/jps.22499
- PMID
- 21283988
- PMCID
- PMC4315361
- NLM abbreviation
- J Pharm Sci
- ISSN
- 0022-3549
- eISSN
- 1520-6017
- Publisher
- Elsevier
- Number of pages
- 7
- Grant note
- R01DC008374 / NATIONAL INSTITUTE ON DEAFNESS AND OTHER COMMUNICATION DISORDERS; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA; NIH National Institute on Deafness & Other Communication Disorders (NIDCD) DC 008374 / National Institutes of Health; United States Department of Health & Human Services; National Institutes of Health (NIH) - USA
- Language
- English
- Date published
- 07/01/2011
- Academic Unit
- Pharmaceutical Sciences and Experimental Therapeutics; Biochemistry and Molecular Biology; Holden Comprehensive Cancer Center
- Record Identifier
- 9984365885002771
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