Bile Salts as Skin Permeation Enhancers ThanaaM. Borg Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura (Egypt)
The influence of bile salts (sodium cholate, sodium taurocholate, and sodium chenodeoxycholate) on the permeation of a lipophilic drug (ß-estradiol) and a polar drug (tetraethylammoniumbromide, TEAB) through hairless mouse skin was investigated. Two-tube chamber diffusion cells and bile salt solutions in saline were used to quantify the reversible permeation enhancement effect of the bile salts. An enhancement factor was calculated from the permeability coefficient and the solubility data. Chenodeoxycholate, cholate, and taurocholate increased the permeability for the ionic drug (TEAB) by a factor of 16.42, 13.92 and 6.59, resp. For lipid soluble ß-estradiol by a factor of 3.11, 1.66 and 1.403, resp. The enhancement factor was 28.39, 12.51 and 11.79 for sodium chenocholate, sodium taurocholate, and sodium cholate, resp. It is proposed that the bile salts affect both the pore pathway as well as the lipoidal pathway. Chenodeoxycholate showed the strongest skin penetration enhancement. Key words Bile salts · ß-Estradiol · Sodium chenocholate · Sodium cholate · Sodium tauorcholate · Skin permeation enhancers · Tetraethylammonium |
| © ECV- Editio Cantor Verlag (Germany) 2000 |
pharmind 2000, Nr. 2, Seite 157
