This research was designed to develop and characterize citric acid-coated superparamagnetic nanoparticles (CA-SPIONs) and nintedanib esylate (NE) loaded CA-SPIONs (NE-CA-SPIONs) for their ability as cancer theranostics. The synthesis of SPIONs involved a chemical co-precipitation method. The XPS analysis confirmed the development of iron oxide (Fe3O4) nanoparticles by the presence of photoelectron lines ascribed to C 1 s, O 1 s, and Fe 2p. The CA-SPIONs and NE-CA-SPIONs had particle size of 21.30±2.3 nm and 30.65±3.2 nm, respectively. The zeta potential was found to be −42.7±1.8 mV for CA-SPIONs and −32.3±2.4 mV for NE-CA-SPIONs. The magnetic properties of CA-SPIONs and NE-CA-SPIONs was found to be 65.64 emu/g and 22.09 emu/g, respectively. The particles were spherical-shape and selective area electron diffraction pattern exhibited semi-crystalline nature of NE-CA-SPIONs. The NE-CA-SPIONs showed drug release of 98.85±3.7 % in 29 h. In vitro hemolysis assay demonstrated hemocompatibility of CA-SPIONs and NE-CA-SPIONs. The NE-CA-SPIONs were more cytotoxic compared to free NE across the A549 cells. The CA-SPIONs were proven to be safe with less percentage cell inhibition even at high concentration. The X-ray imaging of CA-SPIONs displayed their use as a contrast agent in diagnosis. Overall, the research suggested the use of CA-SPIONs and NE-CA-SPIONs in diagnosis and cancer treatment.