Since the in vitro antitumor activity of PF403 is about 1000 times greater than that the pro-drug CAT3 and PF403 can penetrate the blood-brain barrier and incur an anti-glioma effects [12], the increased bioavailability and Cmax of PF403, that were obtained through the oral administration OA-CAT3-SLN, would significantly contribute in exerting a better anti-glioma effect. Here, SLC7A3 is linked to glioma.