This study presents a facile synthesis strategy for magnetic field-responsive PEGylated iron-supplement-coated rutile titanium dioxide (TiO) nanoparticles (NPs) for stimulus-responsive drug delivery. Imatinib, an anticancer drug, was successfully loaded into NPs, and its release was investigated under different pH conditions. XRD analysis confirmed the successful synthesis of PEGylated iron supplement-coated rutile titania NPs. HR-TEM studies revealed an increased NP size due to the coating, PEGylation, and drug loading, which was corroborated by FTIR spectra, confirming the drug loading into the NPs. DLS provided a hydrodynamic diameter of 642.2 nm and polydispersity index of 0.277 for PEGylated NPs, indicating their enhanced biodistribution and narrow size distribution. PEGylated NPs exhibited a negative zeta potential of -32.89 mV, indicating high stability. drug-release studies demonstrated controlled release with maximum efficiency under acidic conditions. Hemolysis assay confirmed the safety and biocompatibility of PEGylated NPs. All drug-loaded nanoformulations followed the Peppas-Sahlin model, suggesting Fickian diffusion and Case II relaxation mechanism of drug release. These NPs have the potential for the targeted delivery and controlled release of chemotherapeutics, thereby minimizing side effects.