Brain cancer has become an emerging medical disorder that poses a threat to human life due to the uncontrolled growth of cancer cells and their gradual spread to other organs. The most aggressive and life-threatening of the several types of Brain cancer is GBM. Treating GBM is difficult considering drugs are not exposed at the brain's site of action because of BBTB and BBB. Only a few cytotoxic drugs are presently used to treat GBM, including temozolomide, paclitaxel, and doxorubicin, and only temozolomide has enough BBB penetration. In this context, engineered nanoparticles are used to transport chemotherapeutic medications and reduce notable peripheral toxicity on normal cells; for necessary drug dosages. They are investigated as drug carriers to address the problem of drug resistance linked to traditional chemotherapy treatments. Many nanostructures, such as polymeric, lipid-based, and inorganic nanoparticles, have been developed as drug-delivery methods in recent decades. To be therapeutically successful as a GBM therapy, ENP formulations must diffuse through the BBB and efficiently deliver the drugs to the target cells. Various coatings and surface modifications of nanostructures can be tailored with different targeting moieties to facilitate the uptake of drug carriers by malignant cells while safeguarding healthy tissues from damage.