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

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...

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Bibliographic Details
Published in:International journal of pharmaceutics 2012-07, Vol.431 (1-2), p.161-175
Main Authors: Villar, Ana Maria Sierra, Naveros, Beatriz Clares, Campmany, Ana Cristina Calpena, Trenchs, Monserrat Aróztegui, Rocabert, Coloma Barbé, Bellowa, Lyda Halbaut
Format: Article
Language:English
Subjects:
Box–Behnken design
Calorimetry, Differential Scanning
Capsules
Chemistry, Pharmaceutical
Drug Delivery Systems - methods
Emulsions
Gelatin
Gemfibrozil
Gemfibrozil - chemistry
Microscopy, Electron, Transmission
Nanostructures - chemistry
Nanostructures - ultrastructure
Plant Oils - chemistry
Pseudoternary phase diagrams
Self-nanoemulsifying drug delivery systems
SNEDDS
Solubility
Spectrometry, Fluorescence
Surface-Active Agents - chemistry
Tablets
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Summary: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® EL), X2 (Capmul® 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 td 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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2012.04.001