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Development and optimization of sustained release polymeric microparticles by screening design

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Abstract

The aim of the present study was to investigate the effect of processing and formulation variables on polymeric microparticles, intended to be used for sustaining drug delivery of ibuprofen. Ibuprofen, polycaprolactone, dichloromethane (DCM), water, stirring speed and polyvinyl alcohol were selected as independent variables during the microparticles preparation. The independent variables influencing encapsulation efficiency (E.E.) and physical characteristics were assessed. The resultant microparticles were characterized for their E.E., surface morphology, and in vitro drug release. Ibuprofen loaded polymeric microparticles were characterized by FESEM, FTIR, DSC, and XRPD analysis. Graphical and mathematical analysis of the design showed that ibuprofen, polycaprolactone and DCM were significant effect on the E.E. of the microparticles. The low magnitudes of error and the significant values of R2 in the present investigation prove the high prognostic ability of the design. The microparticles showed high E.E. (76.11 ± 0.06–104.9 ± 0.46 %) with average particle size of 5–100 μm. The microparticles were found to be discrete, spherical with smooth surface. The FTIR analysis confirmed the compatibility of ibuprofen with the polymers. The XRPD and DSC study revealed the dispersion of drug within microparticles formulation. In vitro study showed sustain drug release over 12 h, thus prolong the drug action to treat the musculoskeletal disorder.

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Acknowledgments

All authors (A. S. Gawali, R. K. Deshmukh, J. B. Naik) declare that they have no conflict of interest. This article does not contain any studies with human and animal subjects performed by any of the authors. The authors want to express their sincere thanks to Technical Education Quality Improvement Program (TEQIP II), MHRD New Delhi, India for financial support. Authors are very much thankful to Natco Pharma Limited (Hyderabad, India), for providing the gift sample of Ibuprofen.

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  1. Department of Pharmaceutical Technology, University Institute of Chemical Technology, North Maharashtra University, Umavi Nagar, Post Box 80, Jalgaon, 425 001, Maharashtra, India

    Amol S. Gawali, Rameshwar K. Deshmukh & Jitendra B. Naik

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  1. Amol S. Gawali
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  2. Rameshwar K. Deshmukh
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  3. Jitendra B. Naik
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Correspondence to Jitendra B. Naik.

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Gawali, A.S., Deshmukh, R.K. & Naik, J.B. Development and optimization of sustained release polymeric microparticles by screening design. Journal of Pharmaceutical Investigation 45, 349–358 (2015). https://doi.org/10.1007/s40005-015-0181-4

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  • DOI: https://doi.org/10.1007/s40005-015-0181-4

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