Given the limited sensitivity of screening methods and the lack of effective therapeutic interventions for malignant brain tumors such as glioblastoma multiforme (also known as GBM), diagnostic and therapeutic procedures for these tumors are rarely performed on a routine basis. Nanostructures with great selectivity, including silica-based nanovehicles, metallic nanostructures, lipid nanoparticles, quantum dots, and polymeric nanoparticles, have been demonstrated to have excellent potential for passing the BBB efficiently. Based on tumor-derived cells, surface modification, encapsulation of contrast agent, bio composition, and functionalities by appropriate coating materials can all be used to take advantage of the photodynamic, magnetic, and optical capabilities of nanostructures. As a result, nanotechnology has revolutionized the detection, screening, as well as treatment of malignancies and brain tumors. In recent years, nanostructures with biomimetic activities have been designed for uptake by tumors in deep cancer regions, with the goal of monitoring and treating the disease. Also, nanostructures are exceptional nano-vehicles for delivering therapeutic agents to their targeted areas due to their special physicochemical properties, which include nanosized dimensions, larger surface area, specific geometrical characteristics, and the capabilities to encompass various substances within their inner parts or on their exterior surface. This paper describes the current developments of several nanostructures such as dendrimers, liposomes, carbon dots, carbon nanotubes, micelles, and metallic nanoparticles for efficient detection of GBM as well as drug delivery in GBM treatment. The importance of metallic nanoparticle-based radiosensitization, as well as immunotherapy, as good ways to fight metastasis and GBM growth, will also be discussed.