Self nano emulsifying solid of clopidogrel - developement, characterization, evaluation and effect on bioavailability

Abstract

The aim of the present study is the development and characterization of self-nano emulsifying drug delivery systems (SNEDDSs) to improve the rate of dissolution of poorly water-soluble anti-platelet agent clopidogrel bisulfate. The solubility was estimated in various vehicles to select proper components and compositions. Cinnamon oil (as oil), Tween 80 (as a surfactant), polyethylene glycol 400 (as co-surfactant) and Water is used to construct pseudo-ternary phase diagrams. Stability, dispersibility and robustness to dilution were performed to optimize formulations by using the phase diagram. Formulations were prepared with different composed of cinnamon oil, Tween 80 and PEG 400 (Smix) ratios. The globule size of the optimized system was less than 200 nm, which could be an accepted nanoemulsion size range. The selected formulation F 7 SNEEDS of z-average size was 140.8 nm, and zeta potential was -28.6. In vitro, drug release studies showed a significantly enhanced rate of dissolution of F 7 SNEDDS when compared to the marketed formulation.