materials that can facilitate drug entrance into bacteria, enable penetration into biofilms, and exhibit synergism with their own functional characteristics. One method of slowing the development of antimicrobial resistance is to encapsulate antibacterial drugs in nanomaterial. By increasing the absorption of antimicrobial medications and thereby halting the development of resistant mutations, antibiotic-loaded nanoparticles may lessen antimicrobial resistance. Additionally, antibiotics at the nanoscale may be able to prevent efflux pumps. A New ciprofloxacin derivative 2 was synthesized and characterized. The newly synthesized compound 2 loaded nanoparticles evaluated as antibacterial agents against Staphylococcus aureus as Gram-positive bacteria and Escherichia coli and Pseudomonas aeruginosa as Gram-negative bacteria using ciprofloxacin as reference. The in vitro antibacterial screening revealed the higher potency of compound 2 loaded nanoparticles against Staphylococcus aureus with MIC value of 0.68 µg/mL than parent ciprofloxacin with MIC value of 3.24 µg/mL and lower activity against Escherichia coli and Pseudomonas aeruginosa (MIC range 0.85-1.17, µg/mL) compared to ciprofloxacin (MIC range 0.17-0.23, µg/mL). Molecular docking studies showed that compound 2 loaded nanoparticles exerts an additional significant binding towards topoisomerase II (gyrase) enzyme (PDB: 2XCT) active.