Self nanoemulsifying drug delivery systems

The aims of this study were to prepare SNEDDS containing aceclofenac and to evaluate its in vivo efficacy. Pseudo-ternary phase diagrams were constructed to optimize the percentage of oil, surfactant and cosurfactant. The efficiency of the emulsification was good when Km was 8:1. An optimized formulation consisting of Labrafac? Lipophile WL1349 (oil,7.4%), Labrasol? (surfactant,82.2%) and Capmul? MCM C8 (cosurfactant,10.4%) was selected for digestible SNEDDS; Maisine? 35-1 (oil,7.4%), Cremophor? RH40 (surfactant,82.2%) and Brij? O10 (cosurfactant,10.4%) for nondigestable SNEDDS. Nanoemulsions formed with water showed good properties with droplet size of 12.9±0.1 and 10.7±0.1 nm; polydispersity index of 0.123±0.006 and 0.075±0.005 for digestable and nondigestable SNEDDS, respectively. The effects of dilution and pH on the droplet size were examined using pH 1.2; 4.5; 6.8, FaSSIF and FeSSIF simulated media. The nondigestable SNEDDS remained stable for up to four months. In vivo pharmacodynamic studies were carried out using carrageenan-induced rat-paw-edema-model (10mg/kg aceclofenac). The results indicate that dilution and pH had no real effect on the droplet size. The release of aceclofenac in FaSSIF and FeSSIF media showed that was independent of fed and fasted states. With developed SNEDDS, the antiinflammatory activity started earlier and took a long time than the nanoemulsion system. The studies on ternary phase diagrams, lipolysis, pH and dilution rate offered a valuable and efficient strategy for developing and optimizing SNEDDS to obtain optimal formulations. The data suggest that the use of SNEDDS can provide a potential way to enhance the bioavailability of poorly water soluble drugs such as aceclofenac.