Crossing the blood–brain barrier with graphene nanostructures

Abstract: Therapeutic approaches for the delivery of drugs to the central nervous system are hampered by the presence of the blood–brain barrier (BBB); overcoming this barrier is the clinical goal for the treatment of neurological disorders, including Alzheimer’s disease and Parkinson’s disease. The BBB is a cellular barrier of a highly impermeable nature that is predominantly formed by a tightly bound continuous layer of endothelial cells; it acts as a gatekeeper to restrict the free diffusion of bloodborne pathogens into the central nervous system. Targeted drug delivery systems have been explored over the past decade for crossing the BBB. Very recently, graphene nanostructures have shown great potential for crossing the BBB due to their exceptional features such as high electron mobility, ease of synthesis and functionalization, as well as control over size, shape, and the drug release profile. Graphene is evolving as a system not only to detect diseased lesions but also, in parallel, to treat neurological disorders while demonstrating minimal side effects. Given the rapid developments of innovative graphene-based delivery platforms, the present review sheds light on the status and prospects of graphene for crossing the BBB by improving, preserving, or rescuing brain energetics, with a specific focus on how graphene alters neuronal cell function.