Green synthesis and characterization of an orally bioactive artemisinin-zinc nanoparticle with enhanced bactericidal activity.

The occurrence of multidrug-resistant bacteria necessitates the development of new antibacterial agents. This study synthesized artemisinin-zinc nanoparticles (AZ NPs) using a simple green method and investigated their physicochemical properties, antibacterial activity, and oral biological activity. A spherical shape morphology of AZ NPs was observed by scanning and transmission electron microscopy, with a particle size of 73 ± 2.604 nm. Energy dispersive spectrometry analysis showed that the AZ NPs consisted mainly of Zn, C, N, and O elements. According to differential scanning calorimeter analysis, the AZ NPs were stable up to 450 °C. Fourier-transform infrared spectroscopy revealed that artemisinin successfully bound to zinc acetate. The AZ NPs showed antibacterial activity against Salmonella and Escherichia coli, with a minimum inhibitory concentration of 0.056 mg/mL for both and minimum bactericidal concentrations of 0.21 and 0.11 mg/mL, respectively. The mechanisms by which AZ NPs mediate membrane damage were revealed by the downregulation of gene expression, and potassium ion and protein leakage. In vivo safety trials of these drugs revealed low toxicity. After AZ NPs were administered to infected mice, the intestinal bacteria decreased significantly, liver and kidney function were restored, histopathological damage to the liver and spleen were reduced, and the expression of inflammatory cytokines decreased. Therefore, AZ NPs have the potential as an oral antibacterial agent and can be used in antibiotic development and in the pharmaceutical industry.