The lactoferrin-conjugated biodegradable polymersome holding doxorubicin and tetrandrine (Lf-PO-Dox/Tet) antitumor agents loaded into a drug delivery system demonstrated the strongest cytotoxicity against C6 glioma cells and had a greater uptake index with C6 cells than PO-DOX, PO-Dox/Tet, or Lf-PO-Dox by integrating both BBB and glioma-targeting moieties and an MDR inhibitor [93]. Here, LTF is linked to central nervous system cancer.