DEVELOPMENT AND OPTIMIZATION OF TRANSDERMAL MICROEMUSION FORMULATION OF BCS CLASS II ANTIDIABETIC DRUG BY DOE

The main aim of present investigation was to examine the potential of a microemulsion formulation developed through simplex lattice design  as well as desirability function approach for transdermal delivery of BCS class II anti diabetic drug Glibenclamide. Pseudo-ternary phase diagrams were plotted by water titration method for multiple microemulsion formulations using oleic acid (oil), tween 80 (surfactant) ethanol (cosurfactant) mixture and water. The area of Pseudo ternary phase diagram was the basis of selecting surfactant cosurfactant ratio (i.e. 1:2).Simplex lattice design for microemulsion preparation was used to identify the effect of independent variables oil concentration (X₁), scs concentration (X₂) and water (X₃) with response variables like percentage transmittance (Y₁) as well as cumulative % drug permeation (Y₂). Polynomial equations as well as model graphs obtained by performing simplex lattice design experiments were used to evaluate the effect of independent variables on responses. The concentration of surfactant cosurfactant mixture was directly related to transmittance and hydration of skin also affected the permeation. So there was significant effect on the responses (p<0.05). Using desirability function, the optimized formulation with desirability value (0.998) was developed with oleic acid (4.06%), surfactant cosurfactant(1:2) concentration (44.3%) and water 51.52% showed the transmittance value 99.87± 2.35% and permeation value 86.17±2.79%. The %permeation from optimized microemulsion was found  2.73 times more that of the control suspension formulation through excised rat skins in franz diffusion cell . The other parameters of optimized formulation like globule size was uniform, stable and showed same observed and predicted responses.