Glioblastoma multiforme is the most malignant and invasive brain tumor, characterized by a heterogeneous histological nature. This primary tumor is considered a grade IV neoplasm with astrocytic differentiation; the average incidence rate is 3.2 cases per 100.000 people and the median age of diagnosis is 64 years with typically mean survival rates after diagnosis less than two years. Currently, standard therapies generally include surgical resection, combined with radiotherapy, chemotherapy, but these approaches minimally extend the average patient survival. In the last decades, biomedical research and, in particular, nanomedicine have developed several strategies in order to enhance conventional anticancer therapies. Nanocarriers represent an innovative and versatile solution, as they can be used both for imaging and therapeutic purposes.