The blood-brain barrier (BBB) is one of the most essential protection mechanisms in the central nervous system (CNS). It selectively allows individual molecules such as small lipid-soluble molecules to pass through the capillary endothelial membrane while limiting the passage of pathogens or toxins. However, this protection mechanism is also a major obstacle during disease state since it dramatically hinders the drug delivery. In recent years, various tactics have been applied to assist drugs to cross the BBB including osmotic disruption of the BBB and chemical modification of prodrugs. Additionally, nanoparticles (NPs)-mediated drug delivery is emerging as an effective and non-invasive system to treat cerebral diseases. In this review, we will summarize and analyze the advances in the drug delivery across the BBB using various NPs in the last decade. The NPs will cover both traditional and novel nanocarriers. The traditional nanocarriers consist of poly(butylcyanoacrylate), poly(lactic-co-glycolic acid), poly(lactic acid) NPs, liposomes and inorganic systems. In the meanwhile, novel nanocarriers such as carbon quantum dots with their recent applications in drug delivery will also be introduced. In terms of significance, this review clearly depicts the BBB structure and comprehensively describes various NPs-mediated drug delivery systems according to different NPs species. Also, the BBB penetration mechanisms are concluded in general, emphasized and investigated in each drug delivery system.