Through the use of OA-CAT3-SLN, the in vitro cellular uptake and transepithelial transport were increased significantly, promoting more CAT3 conversion into PF403 in plasma, and higher bioavailability and Cmax of PF403, which allowed a higher drug concentration to accumulate in the brain tissue to demonstrate enhanced anti-glioma effect. This evidence concerns the gene SLC7A3 and central nervous system cancer.