title: Accumulation of topical naproxen by cultured oral epithelium.
abstract: Topically administered non-steroidal anti-inflammatory drugs (NSAIDs) inhibit periodontal bone loss, but little is known about the mechanism by which they penetrate oral epithelium. Active transporters could potentially play a role in this process. In this study, we used a cell line derived from oral epithelium to investigate a role for transporters and to characterize conditions that enhance epithelial penetration. Using fluorescence to monitor uptake, we demonstrated that SCC-25 cell monolayers transport naproxen with a Michaelis constant (K(m)) and maximum velocity (V(max)) of 164 microg/mL and 0.94 ng/min/microg protein, respectively. At steady state, the intra-cellular/extracellular concentration ratio was 3.4. Naproxen accumulation was more efficient at acidic pH than under neutral or alkaline conditions. Small proportions of glycerol, Pluronic F-127, and glucosylceramide enhanced naproxen entry. The individual and combined effects of glycerol and Pluronic F-127 were of lesser magnitude than those obtained with glucosylceramide or at pH 6.3. Thus, SCC-25 cells possess transporters for naproxen.
authors.affiliation: Section of Periodontology, College of Dentistry, The Ohio State University Health Sciences Center, 305 West 12th Avenue, P.O. Box 182357, Columbus, OH 43218-2357, USA.
authors.forename: R R
authors.initials: RR
authors.lastname: Fitzgerald
authors.forename: J D
authors.initials: JD
authors.lastname: Walters
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D001693:Biological Transport, Active / Q000187:drug effects; D045744:Cell Line, Tumor; D004847:Epithelial Cells / Q000378:metabolism*; D000431:Ethanol / Q000494:pharmacology; D005963:Glucosylceramides / Q000494:pharmacology; D005990:Glycerol / Q000494:pharmacology; D006801:Humans; D009288:Naproxen / Q000493:pharmacokinetics*; D020442:Poloxamer / Q000494:pharmacology; D013501:Surface-Active Agents / Q000494:pharmacology
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005963:Glucosylceramides; D013501:Surface-Active Agents; D020442:Poloxamer; D000431:Ethanol; D009288:Naproxen; D005990:Glycerol