Iron oxide nanoparticles have unique magnetic properties and therefore readily respond to applied magnetic fields. Moreover, their surfaces can be used to attach active molecules via various covalent or noncovalent interactions. Thus, they can be used as drug carriers for magnetically controlled delivery to specific biological sites of interest. In the present study, we have synthesized aqueous dispersed samples of citric acid-capped iron oxide nanoparticles, and the anticancer drug doxorubicin was then linked with these superparamagnetic iron oxide nanoparticles via a simple noncovalent interaction. Our results show that the conjugated drug releases from the nanoparticles in a sustained manner. The cellular uptake of these nanoparticles was found to be substantial, although it can be further enhanced using magnetic guidance. These nanoparticles (drug free) were found to be nontoxic to cells; however, upon drug conjugation, drug-induced toxicity was observed, owing to the slow release of drug from the nanoparticles.