Permeation and systemic absorption of R- and S-baclofen across the nasal mucosa

Hefei Zhang, Mark Schmidt, Daryl J. Murry, Maureen D. Donovan

Research output: Contribution to journalArticle

5 Scopus citations

Abstract

Baclofen, an antispasmodic agent that acts as a GABAB 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.

Original languageEnglish (US)
Pages (from-to)2717-2723
Number of pages7
JournalJournal of Pharmaceutical Sciences
Volume100
Issue number7
DOIs
StatePublished - Jul 2011

Keywords

  • Bioavailability
  • Nasal absorption
  • Nasal drug delivery
  • Permeability
  • Pharmacokinetics
  • Transporters

ASJC Scopus subject areas

  • Pharmaceutical Science

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