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TRANSDERMAL AND BUCCAL DELIVERY OF METHYLXANTHINES THROUGH HUMAN TISSUE IN VITRO.

Thakur1, R.A., Michniak1, B.B., Meidan2, V.M. 1Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ, 2Department of Pharmaceutical Sciences, University of Strathclyde, Glasgow, Scotland, UK.
Abstract

This study by researchers at Rutgers University (USA) and the University of Strathclyde (Scotland) demonstrated that MatTek’s EpiOral in vitro human buccal (inner cheek) tissue equivalent is an excellent in vitro substitute for testing the buccal permeability of a number of central nervous system stimulants. Researchers examined the in vitro permeation of central nervous system stimulants – caffeine, theophylline, and theobromine – across human skin with the aid of six chemical enhancers. It was found that oleic acid was the most potent enhancer for all three methylxanthines. Further optimization studies with different solvents showed that caffeine transport could be enhanced to give flux values up to 585 ìg/cm2.hr-1. Theobromine and theophylline delivery rates proved insufficient. An additional study involving a buccal tissue equivalent (EpiOral™, MatTek Corp.) showed that this membrane was more permeable than skin for all model actives tested and would offer an alternate way of delivery.

Keywords

Buccal delivery, Chemical enhancers, EpiOral, Methylxanthines, ORL-200, Permeation enhancers

Materials Tested

Caffeine, Oleic acid, Theobromine, Theophylline

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