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Accumulation of Topical Naproxen by Cultured Oral Epithelium

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

^* corresponding author, walters.2{at}osu.edu

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 µg/mL and 0.94 ng/min/µg 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.

KEY WORDS: analgesic • inflammatory periodontitis