Abstract: The blood-brain barrier (BBB) restricts the entry of most drugs into the brain, making it a major therapeutic obstacle to the central nervous system diseases. The brain-targeting biomimetic drug delivery strategies have recently been extensively investigated due to its promising prospects. In the brain tumor microenvironments, some specific nutrient transporters and signal receptors are overexpressed in the blood epithelium or tumor cells to support the rapid growth of tumor. This article reviewed the research progress of brain-targeting biomimetic delivery strategies mediated by nutrient transports and signal receptors related pathways in recent years and their applications in brain cancer therapy.