Abstract: Malignant brain tumors seriously threaten human health.Despite the great progress in medical treatment with better clinical technology, the prognosis for most brain cancer patients still remains poor.The protective blood brain barrier (BBB) blocks the effective delivery of drugs, leading to the treatment failure of various drugs.Recent breakthroughs in nanotechnology have endowed multifunctional nanomedicines with the ability to cross the BBB, enabling accumulation of therapeutic drugs in brain tumors.This review discusses the design strategies of BBB-crossing nanomedicines and their current progress in brain tumor treatment, and summarizes the existing problems of nanomedicines for brain tumor treatment as well as the potential strategies to overcome these limitations, so as to provide reference for developing nanomedicines for brain tumor treatment.