In multifunctional vinblastine liposomes, the newly synthesized TfR-T12-PEG2000-DSPE acts as a BBB-targeting molecule that specifically binds to transferrin receptors, facilitates the ferrying of the liposomes across the BBB by RMT, and allows the liposomes to penetrate brain glioma cells and glioma stem cells via RME. Here, TFRC is linked to central nervous system cancer.