Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil

作者：Sierra Villar Ana Maria; Clares Naveros Beatriz; Calpena Campmany Ana Cristina; Aroztegui Trenchs Monserrat; Barbe Rocabert Coloma; Halbaut Bellowa Lyda

来源：International Journal of Pharmaceutics, 2012, 431(1-2): 161-175.

DOI：10.1016/j.ijpharm.2012.04.001

• Gemfibrozil
• Self-nanoemulsifying drug delivery systems
• SNEDDS
• Pseudoternary phase diagrams
• Box-Behnken design

Self-nanoemulsifying drug delivery systems of gemfibrozil were developed under Quality by Design approach for improvement of dissolution and oral absorption. Preliminary screening was performed to select proper components combination. Box-Behnken experimental design was employed as statistical tool to optimize the formulation variables, X-1 (Cremophor (R) EL), X-2 (Capmul (R) MCM-C8), and X-3 (lemon essential oil). Systems were assessed for visual characteristics (emulsification efficacy), turbidity, droplet size, polydispersity index and drug release. Different pH media were also assayed for optimization. Following optimization, the values of formulation components (X-1, X-2, and X-3) were 32.43%, 29.73% and 21.62%, respectively (16.22% of gemfibrozil). Transmission electron microscopy demonstrated spherical droplet morphology. SNEEDS release study was compared to commercial tablets. Optimized SNEDDS formulation of gemfibrozil showed a significant increase in dissolution rate compared to conventional tablets. Both formulations followed Weibull mathematical model release with a significant difference in t(d) parameter in favor of the SNEDDS. Equally amodelistic parameters were calculated being the dissolution efficiency significantly higher for SNEDDS, confirming that the developed SNEDDS formulation was superior to commercial formulation with respect to in vitro dissolution profile. This paper provides an overview of the SNEDDS of the gemfibrozil as a promising alternative to improve oral absorption.

• 出版日期2012-7-15