FORMULATION AND OPTIMIZATION OF NANOSUSPENSION FOR IMPROVING SOLUBILITY AND DISSOLUTION OF GEMFIBROZIL

  • Sanjeevani S Deshkar Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.
  • Kiran G Sonkamble Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.
  • Jayashri G Mahore Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.

Abstract

Objective: The study aims at the formulation and optimization of gemfibrozil (Gem) nanosuspension (NS) for improving its solubility and dissolution rate.

Method: Gem NS was prepared by precipitation-ultrasonication method using ethanol as solvent, water as anti-solvent, and polyvinyl alcohol (PVA) as a stabilizer. A Box–Behnken design was employed to study the effect of the independent variables, Gem concentration in the organic phase (X1), PVA concentration (X2) and sonication time (X3) on the dependent variable, drug release after 90 min (Y). The resulting data were statistically analyzed and subjected to 3D response surface methodology to study the influence of variables on the response. NS was evaluated for particle size, zeta potential, solubility and in vitro drug release and characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD).

Results: On the basis of the evaluation, NS4 formulation (with 80 mg/ml Gem, 0.5% PVA concentration, and 20 min of sonication time) demonstrated highest drug content with a particle size of 191.0 nm and zeta potential of −12.0 mV. Dissolution profiles of NS indicated 2.5-fold increase in drug release than pure drug. NS demonstrated 5- and 9-fold increase in solubility, in water, and phosphate buffer (pH 7.5), respectively, pure drug. DSC and XRD studies indicated changes in the crystallinity of Gem during NS formulation. No chemical change was evident in NS as indicated by FTIR.

Conclusion: Gem NS formulation could serve as a promising approach for improving its solubility and dissolution rate.

Keywords: Gemfibrozil, Nanosuspension, Precipitation-ultrasonication method, Solubility enhancement, Dissolution.

Author Biographies

Sanjeevani S Deshkar, Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.
Associate professor, Department of Pharmaceutics
Kiran G Sonkamble, Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.
Student department of Pharmaceutics
Jayashri G Mahore, Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411 018, Maharashtra, India.
Assistant professor, Department of Pharmaceutics

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How to Cite
Deshkar, S. S., K. G. Sonkamble, and J. G. Mahore. “FORMULATION AND OPTIMIZATION OF NANOSUSPENSION FOR IMPROVING SOLUBILITY AND DISSOLUTION OF GEMFIBROZIL”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 1, Jan. 2019, pp. 157-63, doi:10.22159/ajpcr.2019.v12i1.26724.
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