The potent bacterial infections serve as the primary cause of mortality due to the absence of novel antibacterial therapy. The present investigation synthesized citric acid dendrimers through the divergent method that serves as a suitable platform in fulfilling the prerequisites of drug delivery. The cytotoxicity studies revealed 5.4 ± 0.3% of cell viability at 0.5 μg/ml and 35±0.3% at 300 μg/ml after 36 h. The IC50 values on Human Alveolar Epithelial (HAE) cells for unmodified dendrimers were 1.36±0.06 mg ml−1while for PEG CZ G5 dendrimers were 35.19±0.15 mg/mlwith 9 ± 0.18% hemolysis. The significant differences were due to the variations in drug content and PEG shield density at the terminal surface. The Reactive Oxygen Species (ROS) uptake and dichlorofluorescein intensity for PEG CZ G2 dendrimers was 24.15 ± 1.24% and 42.3 ± 0.12%whichincreased significantly with the degree of pegylation and revealed 72.5 ± 1.03% and 79.2 ± 0.24%for PEG CZ G5 dendrimers. The increased ROS concentrations altered the mitochondrial functioning and served as a proof for antibacterial effect. Drug release pattern when heuristically fitted into various kinetic models specified zero-order release with non-fickian diffusion. Antibacterial investigations and pharmacokinetic studies revealed that the synthesized generations were quite effective against various bacterial pathogens with optimized concentrations. © 2020 Taiwan Institute of Chemical Engineers