| Permeation and systemic absorption of R- and S-baclofen across the nasal mucosa. | |
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MedLine Citation:
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PMID: 21283988 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Hefei Zhang; Mark Schmidt; Daryl J Murry; Maureen D Donovan |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, N.I.H., Extramural Date: 2011-01-31 |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 100 ISSN: 1520-6017 ISO Abbreviation: J Pharm Sci Publication Date: 2011 Jul |
Date Detail:
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Created Date: 2011-05-06 Completed Date: 2011-09-12 Revised Date: 2012-10-09 |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: United States |
Other Details:
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Languages: eng Pagination: 2717-23 Citation Subset: IM |
Copyright Information:
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Copyright © 2011 Wiley-Liss, Inc. and the American Pharmacists Association |
Affiliation:
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Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, University of Iowa, Iowa City, Iowa 52242, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Absorption Administration, Intranasal Animals Baclofen / blood, chemistry, pharmacokinetics* Biological Availability Biological Transport Cattle Cell Polarity Electric Impedance Injections, Intra-Arterial Isomerism Male Models, Biological Muscle Relaxants, Central / blood, chemistry, pharmacokinetics* Nasal Mucosa / metabolism* Olfactory Mucosa / metabolism Permeability Rats Rats, Sprague-Dawley |
| Grant Support | |
ID/Acronym/Agency:
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DC 008374/DC/NIDCD NIH HHS; R01 DC008374/DC/NIDCD NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Muscle Relaxants, Central; 1134-47-0/Baclofen |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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