Abstract: Traditional chemotherapeutic drugs act on targeted organs through intravenous administration, causing irreversible damage to human liver and kidney while attacking tumor tissues. In recent years, researches on magnetic nanomaterials develop rapidly. After surface modification, magnetic nanomaterials have good biocompatibility, high drug loading capacity, and targeted aggregation under the effect of an external magnetic field, which have attracted the attention of researchers. Compared with traditional drugs, the magnetic nanoparticle-based drug delivery system has the features of specific targeting, slow-releasing, and high bioavailability. This article reviews the research progresses of magnetic nanomaterials in targeted delivery for chemotherapy.