Effect of surface charge of nanohybrids on the intracellular bacterial killing efficiency

Abstract Background : Lipid polymer hybrid nanoparticles (LPHNPs) are widely investigated nanohybrid system in drug and gene delivery and also medical imaging. A knowledge of lipids-based surface engineering and its effects on the physicochemical properties of LPHNPs affect the cell – NPs interaction, consequently, influence the cytological response is in high demand.Methods and Results : Herein, we developed a cationic and zwitterionic lipids-based surface engineering approach with antibiotics (Doxycycline or Vancomycin) loaded LPHNPs and examined the surface charge influence on the physiochemical characteristics, antibiotic entrapment, and intracellular release behaviors. Importantly, we examined the intracellular antibacterial activity of drug-loaded LPHNPs against Mycobacterium smegmatis or Staphylococcus aureus infected macrophages. Furthermore, cationic or zwitterionic lipids in LPHNP formulations improved the antibiotic loading efficiency and extended the duration of antibiotic release. In vitro particle uptake studies indicated that the cationic LPHNPs and bare nanoparticles (BNPs) were more efficiently internalized into macrophages than zwitterionic LPHNPs.Conclusion : A play in surface charge in the formulation of the macrophage uptake and intracellular bacterial killing efficiency of LPHNPs loaded with clinical antibiotics on macrophages infected with bacteria, provided a basis for optimizing their use in biomedical applications.