Cancer is a global epidemic and is considered a leading cause of death. Various cancer treatments such as chemotherapy, surgery, and radiotherapy are available for the cure but those are generally associated with poor long-term survival rates. Consequently, more advanced and selective methods that have better outcomes, fewer side effects, and high efficacies are highly in demand. Among these is the use of superparamagnetic iron oxide nanoparticles (SPIONs) which act as an innovative kit for battling cancer. Low cost, magnetic properties and toxicity properties enable SPIONs to be widely utilized in biomedical applications. For example, magnetite and maghemite (Fe3O4 and γ-Fe2O3) exhibit superparamagnetic properties and are widely used in drug delivery, diagnosis, and therapy. These materials are termed SPIONs when their size is smaller than 20 nm. This review article aims to provide a brief introduction on SPIONs, focusing on their fundamental magnetism and biological applications. The quality and surface chemistry of SPIONs are crucial in biomedical applications; therefore an in-depth survey of synthetic approaches and surface modifications of SPIONs is provided along with their biological applications such as targeting, site-specific drug delivery and therapy.