Abstract: As a structural barrier between the brain and the systemic circulation, the blood-brain barrier prevents macromolecules and most small-molecule drugs from entering the brain, which make it difficuct to treat central diseases.Various solute carriers such as glucose transporters and amino acid transporters which can transport various nutrients into the brain, are highly expressed on the blood-brain barrier.The ligand corresponding to the transporter is modified on the nano-drug carrier, and the drug is carried across the blood-brain barrier through transporter-mediated transport, which can achieve high-efficiency delivery of drugs to the brain and improve the diagnostic sensitivity and therapeutic effect of central diseases.In this paper, we review different types of solute carriers to mediate nanoformulations such as liposomes, metal nanoparticles, polymer micelles and dendrimers across the blood-brain barrier for the treatment of brain diseases and discuss the opportunities and challenges of this strategy in future applications.