The aim of current study was the loading of ceftazidime onto the first generation of poly(propyleneimine) dendrimer (PPI-G1) to produce an effective drug delivery system against Pseudomonas aeruginosa.The mechanism of ceftazidime- PPI-G1 dendrimer complexes formation is based on interaction between amine groups of dendrimers and carboxylic groups of ceftazidime.PPI-G1 was dissolved in dry tetrahydrofuran (THF) and ceftazidimewas addedto the solution to prepare the nanodrug. The series of tests including size, zeta potential, drug release, stability and kinetic evaluations as well as scanning electron microscopy (SEM) and Fourier transform infrared (FT-IR) spectroscopy were performed for characterization of the ceftazidime-loaded PPI-G1. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the nanodrug was determined with respect to Pseudomonas aeruginosa asthe test microorganism. Ceftazidime-PPI-G1 complex was synthesized with the size of 156.6 nm and -10.2 mV zeta potential. The value of loaded ceftazidime was determined about 38.46 mol%. A gradual drug release was observed within three days up to 92% of the loaded ceftazidime The macrodilution assay demonstrated that PPI-G1 enhances the antibacterial activity of ceftazidime. A new drug delivery system was improved against P. aeruginosa with sustained release and enhanced antibacterial activity.