Formulation of sustained-release Microspheres of Cefixime With Enhanced Oral Bioavailability and Antibacterial Potential

Abstract

Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 μm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC₉₀ value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.

Keywords:

• in vivo sustained release
• bioavailability
• cefixime
• microspheres
• resistance

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgments

One of the authors K Razdan is thankful to AICTE for research scholarship. The authors are thankful to RK Manhas, GNDU for microbiology support.

Financial & competing interests disclosure

The authors are grateful to University grants commission (UGC), New Delhi for granting potential for excellence (UPE) status to Guru Nanak Dev University, Amritsar, Punjab, India and providing the grant for establishment of Centre of Emerging Life Sciences (equipped with sophisticated instruments). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.