The aim of the current study is to design the radiolabeled and drug-loaded nanocarrier with high loading capacity and pH-dependent drug release characteristics that could effectively transport loaded compounds to various organs for efficient diagnostic imaging and chemotherapeutic drug delivery. The aqueous extract of green tea leaves was used to synthesize the small-sized iron oxide nanoparticles (IONPs). The nanoparticles were characterized with UV-visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and energy-dispersive X-ray analysis (EDX). Iron oxide nanoparticles with sizes smaller than 50 nm were successfully synthesized, making them suitable for in vivo studies. In drug loading trials, 94% of the drug was loaded onto the active surface of iron oxide nanoparticles from the solution. The in vitro drug release study revealed that an acidic environment (pH 4.5) effectively triggers the release of doxorubicin (DOX) from the nanoparticles as compared to a neutral environment (pH 7.4). The gamma-emitting radionuclide Tc was successfully labeled with IONPs for biodistribution and imaging studies. The efficiency of radiolabeling was observed to be ≥ 99%. Furthermore, the in vivo biodistribution study of radiolabeled IONPs in rabbit model showed rapid accumulation in various organs such as heart, liver, and kidneys. This work suggested that green synthesized iron oxide nanoparticles are potential nanocarriers for diagnostic imaging and efficiently distributing DOX to specific organs. The aqueous extract of green tea leaves was used for the facile green synthesis of iron oxide nanoparticles (IONPs). Furthermore, the chemotherapeutic drug doxorubicin (DOX) and gamma-emitting radionuclide Tc were loaded on these iron oxide nanoparticles to evaluate the in vivo biodistribution and drug delivery studies in the rabbit models.