The invention relates to an active targeting brain-tumor-resisting drug and a preparation method thereof and specifically discloses a compound. The compound comprises a nano-carrier with the particle size less than 200nm and a target molecule, and the target molecule is coupled to the surface of the nano-carrier and has high affinity on a neuropeptide receptor Y1 on a blood brain barrier and a neuropeptide receptor Y2 on brain tumor cells. The invention further discloses a composition comprising the compound and a preparation method and application of the composition. The compound or the composition can effectively cross the blood brain barrier to get into the brain and can be combined with the brain tumor cells in a high specificity manner so as to deliver the antitumor drug into the tumor cells, drug concentration in the cells is heightened effectively, and the brain tumor cells are killed powerfully.