Drug delivery and distribution in the central nervous system (CNS) and the inner ear represent a challenge for the medical and scientific world, especially because of the blood-brain and the blood-perilymph barriers. Solutions are being studied to circumvent or to facilitate drug diffusion across these structures. Using superparamagnetic iron oxide nanoparticles (SPIONs), which can be coated to change their properties and ensure biocompatibility, represents a promising tool as a drug carrier. They can act as nanocarriers and can be driven with precision by magnetic forces. The aim of this study was to systematically review the use of SPIONs in the CNS and the inner ear. A systematic PubMed search between 1999 and 2019 yielded 97 studies. In this review, we describe the applications of the SPIONS, their design, their administration, their pharmacokinetic, their toxicity and the methods used for targeted delivery of drugs into the ear and the CNS.