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Diclofenac Sodium-Loaded Eudragit® Microspheres: Optimization Using Statistical Experimental Design

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Abstract

Purpose

In this study, polymeric microspheres containing diclofenac sodium were prepared by single emulsion (oil-in-water) solvent evaporation method and evaluated for their size, morphology, encapsulation efficiency, drug loading, and in vitro drug release.

Methods

Two nonbiodegradable polymers, Eudragit® RS100 and RL100 were used in combination. Microspheres were prepared by varying the amount of polyvinyl alcohol as a surfactant (0.05, 0.125, and 2.0 %, w/v) to the external phase; varying the amount of polymer (1:1, 2:1, and 3:1, w/w) to the drug by employing 32 full factorial design using the Design Expert (Version 8.0.7.1). The drug polymer interactions were investigated by Fourier transform infrared spectroscopy (FTIR) and X-ray powder diffractometry (XRPD). Imaging of particles was performed by field emission scanning electron microscopy.

Results

Graphical and mathematical analysis of the design showed a quadratic model was significant for the responses. Low magnitude of error and significant values of R 2 proves the high prognostic ability of the RSM. Encapsulation efficiency of microspheres (41.13 to 65.33 %) increases with an increase in surfactant concentration but decreases with an increase in polymer concentration. The microspheres were found to be discrete, spherical with smooth surface. The absence of drug polymer interactions was confirmed by FTIR spectroscopy. XRPD revealed the dispersion of drug within microspheres formulation. The Perfect pH-independent release profile was achieved from Eudragit® microspheres by anomalous transport mechanism.

Conclusions

In conclusion, Eudragit® microspheres containing diclofenac sodium can be successfully prepared, and seem to be promising for sustained release application.

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Acknowledgment

Authors are very much thankful to University Grants Commission, New Delhi for providing financial assistance (project reference no. F. no. 37-276/2009 (SR)) to carry out this research work. The authors gratefully acknowledge Natco Pharma Limited, (Hyderabad, India) and Evonik Degussa India Pvt. Ltd. (Mumbai, India) for providing the gift sample of DS and Eudragit (RS 100 and RL 100), respectively.

Declaration of Interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.

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  1. Department of Pharmaceutical Technology, University Institute of Chemical Technology, North Maharashtra University, Umavi Nagar, Post Box No. 80, Jalgaon, 425 001, Maharashtra, India

    Rameshwar K. Deshmukh & Jitendra B. Naik

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Correspondence to Jitendra B. Naik.

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Deshmukh, R.K., Naik, J.B. Diclofenac Sodium-Loaded Eudragit® Microspheres: Optimization Using Statistical Experimental Design. J Pharm Innov 8, 276–287 (2013). https://doi.org/10.1007/s12247-013-9167-9

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