Evaluation of galantamine transbuccal absorption by reconstituted human oral epithelium and porcine tissue as buccal mucosa models: part I.
Over the last decade, interest in delivering drugs through buccal mucosa has increased. As a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aim of this study was to evaluate the aptitude of galantamine, useful in Alzheimer's disease, to penetrate the buccal mucosa. The evaluation of the ability of galantamine to permeate through the buccal epithelium was investigated using two permeation models. Firstly, in vitro permeation experiments were carried out using reconstituted human oral non-keratinised epithelium and Transwell diffusion cells system. Results were validated by ex vivo experiments using porcine buccal mucosa as membrane and Franz type diffusion cells as permeation model. The entity of buccal permeation was expressed in terms of drug flux (J(s)) and permeability coefficients (K(p)). Data collected by in vitro and ex vivo experiments were in agreement and suggested that buccal mucosa does not block diffusion of galantamine. The effects of drug application on histology of tissue specimens used in every experiment were also studied: no sign of flogosis and no significant cytological or architectural changes were highlighted.
De Caro
Viviana
V
Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli study di Palermo, Italy. vdecaro@unipa.it
Giandalia
Giulia
G
Siragusa
Maria Gabriella
MG
Paderni
Carlo
C
Campisi
Giuseppina
G
Giannola
Libero Italo
LI
D000278:Administration, Buccal; D000818:Animals; D002478:Cells, Cultured; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000378:metabolism*; D004058:Diffusion; D015194:Diffusion Chambers, Culture; D004847:Epithelial Cells / Q000378:metabolism*; D005702:Galantamine / Q000008:administration & dosage / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D009061:Mouth Mucosa / Q000166:cytology / Q000378:metabolism*; D010539:Permeability; D013552:Swine
D002800:Cholinesterase Inhibitors; D005702:Galantamine