Iron oxide nanoparticles are widely used for biological applications thanks to their outstanding balance between magnetic properties, surface-to-volume ratio suitable for efficient functionalization and proven biocompatibility. Their development for MRI or magnetic particle hyperthermia concentrates much of the attention as these nanomaterials are already used within the health system as contrast agents and heating mediators. As such, the constant improvement and development for better and more reliable materials is of key importance. On this basis, this review aims to cover the rational design of iron oxide nanoparticles to be used as MRI contrast agents or heating mediators in magnetic hyperthermia, and reviews the state of the art of their use as nanomedicine tools.