To improve the poor activity of hydrophobic antibiotics in eradicating bacterial biofilms

a nano-antibiotic was constructed

via

the inclusion complexation between an azobenzene-conjugated norfloxacin prodrug and oligo-

α

-cyclodextrin. The enzyme-responsive degradation and biofilm eradication properties were characterized by nuclear magnetic resonance (NMR)

dynamic light scattering (DLS)

ultraviolet-visible spectrometer (UV-Vis spectrometer)

and scanning electron microscope (SEM). The nano-antibiotics showed excellent broad-spectrum antibacterial activity against the planktonic Gram-negative bacteria

Escherichia coli

and Gram-positive bacteria

Staphylococcus aureus

as well as effective deep penetration in bacterial biofilms due to the good water solubility. In the presence of overexpressed azoreductase in bacterial microenvironment

the azobenzene motif could be responsively degraded

leading the high efficiency in biofilm eradication of norfloxacin

which significantly reduced antibiotic dose. The enzyme responsive nanomedicine reported in this report provided a promising insight to combat the bacterial infection-related diseases.