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

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• 作者：Ana Maria Sierra Villar^a ; Beatriz Clares Naveros^b ; ^{beatrizclares@ugr.es} ; Ana Cristina Calpena Campmany^c ; Monserrat Aró ; ztegui Trenchs^a ; Coloma Barbé ; Rocabert^a ; Lyda Halbaut Bellowa^a
• 关键词：Gemfibrozil ; Self-nanoemulsifying drug delivery systems ; SNEDDS ; Pseudoternary phase diagrams ; Box&ndash ; Behnken design
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：15 July, 2012
• 卷：431
• 期：1-2
• 页码：161-175
• 文件大小：2019 K

摘要

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, X₁ (Cremophor^庐 EL), X₂ (Capmul^庐 MCM-C8), and X₃ (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 (X₁, X₂, and X₃) 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.