In the present study, we have improvised a biogenic method to fabricate zinc oxide nanoparticles (ZnO NPs) using chitosan and an aqueous extract of the leaves of Elsholtzia blanda. Characterization of the fabricated products was carried out with the help of ultraviolet−visible, Fourier transform infrared, X-ray diffraction, field emission scanning electron microscopy, highresolution transmission electron microscopy, selected area electron diffraction, and energy-dispersive X-ray analyses. The size of the improvised ZnO NP measured between 20 and 70 nm and had a spherical and hexagonal shape. The ZnO NPs proved to be highly effective in the antidiabetic test as the sample showed the highest percentage of enzyme inhibition at 74% ± 3.7, while in the antioxidant test, 78% was the maximum percentage of 2,2-diphenyl-1picrylhydrazyl hydrate scavenging activity. The cytotoxic effect was investigated against the human osteosarcoma (MG-63) cell line, and the IC 50 value was 62.61 μg/mL. Photocatalytic efficiency was studied by the degradation of Congo red where 91% of dye degradation was observed. From the various analyses, it can be concluded that the as-synthesized NPs may be suitable for various biomedical applications as well as for environmental remediation.