In this study, we propose a type of functionalized lipid vesicles, named as multifunctional vinblastine liposomes, which potentially transfer vinblastine across the BBB and subsequently eliminate brain glioma cells and glioma stem cells when equipped with the transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8. This evidence concerns the gene TFRC and brain glioma.