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Galantamine Delivery on Buccal Mucosa: Permeation Enhancement and Design of Matrix Tablets

V. De Caro1*, G. Giandalia1, M.G. Siragusa1, G. Campisi2§, L.I. Giannola1§
1Dipartimento di Chimica e Tecnologie Farmaceutiche, Università di Palermo, Italy
2Dipartimento di Scienze Stomatologiche, Università di Palermo, Italy
§IntelliDrug Consortium supported by the European Commission under the Sixth Framework (IST-FP6 n° 002243)
*Corresponding author: Dr. V. De Caro, Dipartimento di Chimica e Tecnologie Farmaceutiche,
Università degli Studi di Palermo,
Via Archirafi 32-90123, Palermo, Italy,
Tel       : +39 091 6236126,
Fax      : +39 091 6236124,
E-mail : vdecaro@unipa.it
Received October 07, 2009; Accepted December 18, 2009; Published December 18, 2009
Citation: De Caro V, Giandalia G, Siragusa MG, Campisi G, Giannola LI (2009) Galantamine Delivery on Buccal Mucosa: Permeation Enhancement and Design of Matrix Tablets. J Bioequiv Availab 1: 127-134. doi:10.4172/jbb.1000020
Copyright: © 2009 De Caro V, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Abstract

The most important feature in transbuccal drug delivery is the low drug passage through the buccal mucosa. In our previous work we demonstrated the aptitude of Galantamine to penetrate the buccal tissue. The collected data suggested that Galantamine passively crosses the membrane, but the calculated Js and Kp values showed that the drug amount that crosses the membrane wasn’t sufficient to assure blood therapeutic level. So, in this study, ex vivo permeation tests, using porcine buccal mucosa, were performed in presence of physical or chemical enhancers. No significant differences in penetration rate were observed using chemical enhancers as sodium dehydrocholate, EDTA disodium salt and trisodium citrate dihydrate; while, Js and Kp were extensively affected by application of electric fields. Tablets, designed for Galantamine administration on buccal mucosa, were prepared by direct compression of drug loaded Eudragit® RS 100 matrices. When the tablets were coated with lipophilic material, Galantamine is slowly discharged from buccal tablets, following the Higuchian kinetic. Buccal tablets containing Galantamine may represent a potential alternative dosage form in Alzheimer management.

 
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