ENHANCEMENT OF TRANSBUCCAL PERMEATION OF MORPHINE-SULFATE BY SODIUM GLYCODEOXYCHOLATE IN-VITRO

In this study, enhancement of transbuccal permeation of morphine sulfa te was studied in the presence of sodium glycodeoxycholate (GDC). The permeability of the bovine buccal mucosa to morphine sulfate was deter mined in vitro in the absence and presence of GDC at 10 mM and 100 mM concentrations. Light and electron microscopy studies were performed t o determine the histological and ultrastructural changes resulting fro m transepithelial permeation enhancement. In addition, infrared spectr oscopy (IR) was used to investigate the interaction of GDC with the ep ithelial lipids of bovine buccal mucosa, The permeation of morphine su lfate across the bovine buccal epithelium was enhanced in the presence of 100 mM GDC by a factor of five whereas at lower concentrations, no significant enhancement was obtained. After 4 h treatment with 100 mM (5% w/v) GDC, significant changes were observed in the epithelium at histological and ultrastructural levels which can be defined as format ion of vacuoles, swelling of the cells and a possible increase in inte rcellular space. Furthermore, by means of IR spectroscopy, it was poss ible to show the effect of GDC on bovine buccal epithelial lipid domai ns which was in good correlation with the permeation results. In the l ight of the results obtained by permeation, histological and IR spectr oscopy studies, it is concluded that GDC at 100 mM concentration signi ficantly enhances the permeation of MS across the buccal epithelium an d the mechanism of this action appears to involve an interaction with the epithelial lipids.