Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate

Patel, Ashok R.; Vavia, Pradeep R.

doi:10.1208/aapsj0903041

Cited by 220 publications

(142 citation statements)

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“…In the gastrointestinal tract environment (fluids 100 and motility) this systems spontaneously emulsify (Nazzal et al, 2002;Devani et al, 2004;Patel et al, 2007). They can improve oral bioavailability by the increase in the drug solubilization (the water-insoluble drug is usually dissolved in the oil phase), enhancing permeation across the intestinal membrane through a wide distribution in the GIT (due to the small droplet size), and decreasing food effect (Wang et al, 2010;Ke et al, 2005).…”

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confidence: 99%

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

Villar

Naveros

Campmany

et al. 2012

International Journal of Pharmaceutics

143

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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 favour 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. She is an expert in nanotechnology (colloids and nanoparticles) with a wide experience. She has extensive curriculum of published paper about this subject Jose Luis Arias Mediano Ph. D. Professor reseracher, Pharmacy and Pharmaceutical Technology , University of Granada jlarias@ugr.es He is an expert in nanotechnology (colloids and nanoparticles) with a wide experience in this type of investigation. Also is reviewer in specialized pharmaceutical journal. He is an expert in nanotechnology (colloids and nanoparticles) with a wide experience in this type of investigation. Also is reviewer of Pharmaceutical science journals. IJP AUTHOR CHECKLISTDear Author, It frequently happens that on receipt of an article for publication, we find that certain elements of the manuscript, or related information, is missing. This is regrettable of course since it means there will be a delay in processing the article while we obtain the missing details.In order to avoid such delays in the publication of your article, if accepted, could you please run through the list of items below and make sure you have completed the items. Overall Manuscript Electronic artwork format? ---------------------------------------------------TIFF

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mentioning

confidence: 99%

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

Villar

Naveros

Campmany

et al. 2012

International Journal of Pharmaceutics

143

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“…Domperidone was dissolved in a glass test tube containing Transcutol at 60°C in a water bath to facilitate solubilization. Oil and surfactant were added and the final mixture was mixed by vortexing until a clear solution was obtained (12,13). The mixture was stored at room temperature until used.…”

Section: Methodsmentioning

confidence: 99%

“…-Evaluation of the self-microemulsifying properties of SMEDDS formulations was performed by visual assessment (13). The time taken for the microemulsion formation (until a transparent system was obtained) was noticed upon dropwise addition of 100 µL of SMEDDS into 100 mL of distilled water in a glass beaker at 37°C, and the contents were stirred magnetically at 100 rpm (17).…”

Section: ) (13)mentioning

confidence: 99%

Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

et al. 2013

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Domperidone, a dopamine D2 receptor antagonist, is used as a prokinetic and antiemetic agent for the treatment of gastroparesis, nausea and vomiting (1). It is a poor water soluble drug and is rapidly absorbed from the gastrointestinal (GI) tract. Its oral bioavailability was reported in a range of 13-17 % (2). Poor aqueous solubility and extensive first pass metabolism are the reasons for its low oral bioavailability. The approaches used to improve oral bioavailability were: incorporation of the active lipophilic component The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000) and freeze-thaw stability. The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol ® , 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats.The AUC 0-24 and c max values were 3.38 ± 0.81 µg h mL -1 and 0.44 ± 0.03 µg mL -1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 µg h mL -1 and 0.24 ± 0.02 µg mL -1 for domperidone suspension, suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDSS.

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“…In addition, since the microemulsion with the weight ratio of Miglyol 812/Capmul MCM (65:22, w/w) to Tween 80 at 40:55 (#7 in Fig. 7a) or lower exhibited similar dilution properties of self-microemulsifying drug delivery systems (29,30), these microemulsions might find applications to enhance oral absorption of poorly watersoluble and/or poorly permeable drugs, which is beyond the scope of the current study.…”

Section: Phase Inversion Behavior Of W/o Microemulsionsmentioning

confidence: 97%

In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

Liu

Russo

et al. 2012

AAPS J

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Abstract. Peptide and protein drugs have become the new generation of therapeutics, yet most of them are only available as injections, and reports on oral local intestinal delivery of peptides and proteins are quite limited. The aim of this work was to develop and evaluate a water-in-oil (w/o) microemulsion system in vitro and in vivo for local intestinal delivery of water-soluble peptides after oral administration. A fluorescent labeled peptide, 5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT (TAMRA-TAT), was used as a model peptide. Water-in-oil microemulsions consisting of Miglyol 812, Capmul MCM, Tween 80, and water were developed and characterized in terms of appearance, viscosity, conductivity, morphology, and particle size analysis. TAMRA-TAT was loaded and its enzymatic stability was assessed in modified simulated intestinal fluid (MSIF) in vitro. In in vivo studies, TAMRA-TAT intestinal distribution was evaluated using fluorescence microscopy after TAMRA-TAT microemulsion, TAMRA-TAT solution, and placebo microemulsion were orally gavaged to mice. The half-life of TAMRA-TAT in microemulsion was enhanced nearly three-fold compared to that in the water solution when challenged by MSIF. The treatment with TAMRA-TAT microemulsion after oral administration resulted in greater fluorescence intensity in all intestine sections (duodenum, jejunum, ileum, and colon) compared to TAMRA-TAT solution or placebo microemulsion. The in vitro and in vivo studies together suggested TAMRA-TAT was better protected in the w/o microemulsion in an enzyme-containing environment, suggesting that the w/o microemulsions developed in this study may serve as a potential delivery vehicle for local intestinal delivery of peptides or proteins after oral administration.

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Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate

Cited by 220 publications

References 20 publications

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

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

Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

In Vitro and In Vivo Evaluation of a Water-in-Oil Microemulsion System for Enhanced Peptide Intestinal Delivery

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