Nowadays, a malignant brain tumor is one of the most life-threatening diseases with poor prognosis, high risk of recurrence, and low survival rate for patients because of the existence of the blood-brain barrier (BBB) and the lack of efficient diagnostic and therapeutic paradigms. So far, many researchers have devoted their efforts to innovating advanced drugs to efficiently cross the BBB and selectively target brain tumors for optimal imaging and therapy outcomes. Herein, we update the most recent developments in nanomedicines for the diagnosis and treatment of brain tumors in preclinical mouse models. The special focus is on burgeoning drug delivery carriers to improve the specificity of visualization and to enhance the efficacy of brain tumor treatment. Also, we highlight the challenges and perspectives for the future development of brain tumor theranostics. This review is expected to receive wide attention from researchers, professors, and students in various fields to participate in future advancements in preclinical research and clinical translation of brain tumor nanomedicines.