Fabrication of liquid and solid self-double emulsifying drug delivery system of atenolol by response surface methodology

Self Double Emulsifying Drug Delivery System (SDEDDS), a concoction of hydrophilic surfactants and water-in-oil (w/o) emulsions, can spontaneously emulsify to water-in-oil-in-water (w/o/w) double emulsions in gastrointestinal aqueous environment, with hydrophilic drugs present in internal water phase. In this study, we developed SDEDDS of atenolol by response surface methodology. A 32 full factorial design was applied for optimization procedure. Independent variables were oil phase and span 80, whereas, response variables were zeta potential (Y1), % drug release at 300 min (Y2), T85% (Y3), mean dissolution time (Y4) and % dissolution efficiency (Y5). Drug loading capacity (500mg/g-water) was increased by using tartaric acid. Microscopic studies confirmed the formation of double emulsions, besides, SEM, TEM and AFM. Responses Y1, Y2, Y3, Y4 and Y5 as exhibited by optimized formulations OF1 were −42 mv, 96%, 180 min, 86 min and 68%, and OF2 were −45 mv, 98%, 184 min, 79 min and 69% respectively. Formed globules were of size-range 182 ± 6 to 308 ± 3 nm. Optimized formulations were solidified by adsorption technique. Ex vivo intestinal permeability studies revealed that atenolol SDEDDS exhibited better drug permeation compared to atenolol or atenolol-tartaric acid solution. Histopathology studies confirmed SDEDDS exerted no serious local damages.

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