Iron oxide nanoparticles are the most popular magnetic nanoparticles used in biomedical applications due to their low cost, low toxicity, and unique magnetic property. Magnetic iron oxide nanoparticles, including magnetite (Fe 3 O 4 ) and maghemite (γ-Fe 2 O 3 ), usually exhibit a superparamagnetic property as their size goes smaller than 20 nm, which are often denoted as superparamagnetic iron oxide nanoparticles (SPIONs) and utilized for drug delivery, diagnosis, therapy, and etc. This review article gives a brief introduction on magnetic iron oxide nanoparticles in terms of their fundamentals of magnetism, magnetic resonance imaging (MRI), and drug delivery, as well as the synthesis approaches, surface coating, and application examples from recent key literatures. Because the quality and surface chemistry play important roles in biomedical applications, our review focuses on the synthesis approaches and surface modifications of iron oxide nanoparticles. We aim to provide a detailed introduction to readers who are new to this field, helping them to choose suitable synthesis methods and to optimize the surface chemistry of iron oxide nanoparticles for their interests.