Formulation of sustained-release microspheres of cefixime with enhanced oral bioavailability and antibacterial potential.
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.
['Razdan|Karan|K|', 'Sahajpal|Nikhil S|NS|', 'Singh|Kuldeep|K|', 'Singh|Harmanpreet|H|', 'Singh|Harjeet|H|', 'Jain|Subheet K|SK|']
D000284:Administration, Oral D000818:Animals D000900:Anti-Bacterial Agents D020682:Cefixime D004337:Drug Carriers D004339:Drug Compounding D065546:Drug Liberation D004926:Escherichia coli D006207:Half-Life D007711:Klebsiella pneumoniae D008863:Microspheres D010316:Particle Size D051381:Rats D012485:Salmonella typhi
microspheres cefixime bioavailability in vivo sustained release resistance