Effect of ion-pairing on the permeation of glibenclamide through rat skin

The purpose of the present study was to investigate the effect of ion-pairing on the permeation of glibenclamide through rat skin. Diethylamine, triethylamine, ethanolamine, diethanolamine and triethanolamine were used as counter-ions. The steady-state flux of glibenclamide markedly increased in the presence of counterions (P < 0.05). These results suggest that it is possible to enhance the permeation of glibenclamide by using an ion-pair approach. Moreover, the extent of enhancement possibly depends on the alkalinity, molecular weight, structure of the counter-ions and the dielectric constant of the donor solution. The influence of penetration enhancers on the permeation of glibenclamide was also determined. All the penetration enhancers studied increased the flux of glibenclamide compared with the control. Among these enhancers, menthol and N-methyl-2-pyrrolidone showed the greatest enhancing activity.