A method for preparing a CTX (Chlorotoxin)-targeted oxidized graphene nanometer material comprises the following steps: 1, mixing graphite and H2SO4-HClO4, stirring and mixing the mixture in an ice-bath, continuing stirring in a warm water bath , heating to 100 to 120 DEG C for deacidification, diluting to 800 to 1000 ml and then centrifuging, adding an alkali solution and then mixing and settling, stirring at 70 to 90 DEG C and filtering under the condition of being hot, washing to be approximately neutral, and freeze drying at minus 40 DEG C under the vacuum condition to obtain oxidized graphene; 2, mixing the oxidized graphene with a phosphate buffer solution, adding N-Hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride to perform an activating reaction at room temperature; adjusting the pH value of the mixture to be 7.0 to 8.0, adding CTX for reaction, centrifugating and washing the obtained product, and performing vacuum freeze drying at minus 40 DEG C to obtain the CTX-targeted oxidized graphene nanometer material. The material can be used for transporting an anticancer drug of adriamycin to a brain glioma in a targeted manner.