Advances of nanotechnology led to the development of nanoparticulate systems with many advantages due to their unique physicochemical properties. The use of iron-oxide magnetic nanoparticles (IOMNPs) in pharmaceutical areas increased in the last few decades. This article reviews the conceptual information about iron oxides, magnetic nanoparticles, methods of IOMNP synthesis, properties useful for pharmaceutical applications, advantages and disadvantages, strategies for nanoparticle assemblies, and uses in the production of drug delivery, hyperthermia, theranostics, photodynamic therapy, and as an antimicrobial. The encapsulation, coating, or dispersion of IOMNPs with biocompatible material(s) can avoid the aggregation, biodegradation, and alterations from the original state and also enable entrapping the bioactive agent on the particle via adsorption or covalent attachment. IOMNPs show great potential for target drug delivery, improving the therapy as a consequence of a higher drug effect using lower concentrations, thus reducing side effects and toxicity. Different methodologies allow IOMNP synthesis, resulting in different structures, sizes, dispersions, and surface modifications. These advantages support their utilization in pharmaceutical applications, and getting suitable drug release control on the target tissues could be beneficial in several clinical situations, such as infections, inflammations, and cancer. However, more toxicological clinical investigations about IOMNPs are necessary.