Brain cancer continues to be one of the most formidable malignancies to manage, mainly attributable to the presence of the blood-brain barrier (BBB) limiting the permeability of drugs and the diverse characteristics of brain tumors complicating treatment. The management of brain tumors has been hampered by many different factors, including the impermeability of the BBB, which restricts the delivery of chemotherapeutic agents to the tumor site, as well as intertumoral heterogeneity and the influence of brain tumor stem cells. In addition, small molecular weight drugs cannot specifically accumulate in malignant cells and have a limited circulation half-life. Nanoparticles (NPs) can be engineered to traverse the BBB and transport therapeutic medications directly into the brain, enhancing their efficacy compared with the conventional delivery of unbound drugs. Surface modifications of NPs can boost their efficiency by increasing their selectivity towards tumor receptors. This review covers treatment methods for malignant gliomas, associated risk factors, and improvements in brain drug administration, emphasizing the future potential of polymeric NPs and their mechanism for crossing the BBB. To surmount these obstacles, the newly formulated drug-delivery approach utilizing NPs, particularly those coated with cell membranes, has demonstrated potential in treating brain cancer. These NPs provide targeted tumor specificity, biocompatibility, extended circulation, enhanced BBB penetration, and immune evasion. This review focuses on coating strategies for PLGA NPs, particularly dual-targeting methods, to enhance BBB permeability and tumor-targeted delivery of drugs in brain cancer.