Oral Bioavailability Enhancement of Glibenclamide by Self-Emulsifying Drug Delivery Systems (SEDDS)

The present work was aimed to improve the oral bioavailability of glibenclamide by developing self-emulsifying drug delivery system (SEDDS). Solubility of glibenclamide was determined in oils, surfactant, and cosurfactant. Pseudoternary phase diagrams were constructed to obtain self-nanoemulsifying region. SEDDS were evaluated for thermodynamic stability, droplet size, in vitro dissolution, in vivo pharmacokinetic, and stability studies. Sunflower oil (3.46 +/- 0.32 mg/100 mg), Tween 80 (3.75 +/- 0.37 mg/100 mg) and PEG 600 (2.98 +/- 0.44 mg/100 mg) were selected as oil, surfactant, and cosurfactant, respectively. Surfactant and cosurfactant mix (Smix) of 3:1, 2:1, and 1:1 showed a larger nanoemulsification region and Ba3 (Smix 3:1) showed minimum emulsion globule size of 122.9 nm with PDI of 0.549 and exhibited highest cumulative drug release (97.6 +/- 1.8), as compared to pure glibenclamide (31.2 +/- 2.2) and marketed tablet (90.3 +/- 2.1). Cmax of Ba3 (10.01 +/- 2.14 mu g/mL) was significantly higher than pure drug (7.13 +/- 1.16 mu g/mL) and marketed tablet (9.02 +/- 2.23 mu g/mL) and AUC of Ba3 (140.39 +/- 10.14 mu g.h/mL) was found to be significantly higher than pure glibenclamide (100.12 +/- 11.45 mu g.h/mL), indicating an improvement in the bioavailability of glibenclamide from SEDDS formulation as compared to pure drug.