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Journal of Dental Research
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*ETHANOL
*GLYCERIN
*NAPROXEN
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Biological

Accumulation of Topical Naproxen by Cultured Oral Epithelium

R.R. Fitzgerald and J.D. Walters*

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

Correspondence: * 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 (Km) and maximum velocity (Vmax) 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

Journal of Dental Research, Vol. 86, No. 8, 775-779 (2007)
DOI: 10.1177/154405910708600817
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