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INTRODUCTION Glioblastoma multiforme is the most common and the most aggressive primary brain tumor, with a median survival of 14 months. This dismal prognostic has turned research towards nanomedicine as a new therapeutic approach that can deliver therapeutic compounds to GBM. AREAS COVERED The review covers recent advances in targeted delivery of therapeutic compounds to glioblastoma tumors. To reach the tumors, nanocarriers and their cargo should cross the Blood-Brain Barrier (BBB) standing between the blood stream and the tumor. For that purpose, different peptides to facilitate BBB crossing have been added to the nanoparticles. As result, an increase in BBB crossing was observed. Other significant effort has been devoted to selectively target direct the nanocarrier and its cargo to GBM tumors. Once again, targeting peptides have been used. EXPERT OPINION Besides significant advances, a more successful design of nanocarriers for efficient BBB crossing and delivery of diagnostic and/or therapeutic molecules to CNS will be needed to achieve efficient nanomedicine-based therapeutics for glioblastoma. This will require a significant effort improving chemical architecture of nanocarriers, identifying the critical design parameters that might play a key role facilitating both BBB crossing and GBM selective targeting.