Iron oxide nanoparticles (IONPs) can be applied to targeted drug delivery, targeted diagnosis and treatment of tumors due to their easy preparation, good biocompatibility, low biotoxicity, high imaging quality, high magnetothermal sensitivity and stable targeting after certain surface modifications. However, the complexity of the mechanism of action and their properties has led to there being few clinical applications of IONPs. This review first describes the targeting mechanisms of IONPs and their toxicity issues, then discusses the applications of IONP targeting studies in tumor MRI. Finally, the applications of IONP targeting in tumor therapy are listed. The authors show the advantages of targeting IONPs and hope that the review will increase the possibility of converting IONPs from biomedical applications to clinical applications.