Polymer assisted entrapment of netilmicin in PLGA nanoparticles for sustained antibacterial activity

Abstract

This study was aimed to develop poly(dl-lactide-co-glycolide) (PLGA) nanoparticle of highly water soluble antibiotic drug, netilmicin sulfate (NS) with improved entrapment efficiency (EE) and antibacterial activity. Dextran sulfate was introduced as helper polymer to form electrostatic complex with NS. Nanoparticles were prepared by double emulsification method and optimized using 2^5-1 fractional factorial design. EE was mainly influenced by dextran sulfate: NS charge ratio and PLGA concentration, whereas particle size (PS) was affected by all factors examined. The optimized NS-loaded-NPs had EE and PS of 93.23 ± 2.7% and 140.83 ± 2.4 nm respectively. NS-loaded-NPs effectively inhibited bacterial growth compared to free NS. Sustained release protected its inactivation and reduced the decline in its killing activity over time even in presence of bronchial cells. A MIC value of 18 μg/mL was observed for NPs on P. aeruginosa. Therefore, NPs with sustained bactericidal efficiency against P. aeruginosa may provide therapeutic benefit in chronic pulmonary infection, like cystic fibrosis.

• Antibiotic
• antimicrobial effect
• nanoparticle
• PLGA
• Pseudomonas aeruginosa, sustained release

Acknowledgements

Authors would also thanks to TIFAC CORE in NDDS for laboratory facilities for the work.

Declaration of interest

The authors report no conflict of interest. We are grateful to financial support from Indian council of Medical Research (ICMR), New Delhi, India and Department of Foreign Affairs and International Trade (DFAIT) Canadian Commonwealth Scholarship Program (CCSP) by the Canadian Bureau of International Education (CBIE).