Chol-CTPP, a ligand with a dual targeting effect on the blood-brain barrier (BBB) and glioma cells, serves as the precursor to Lip-CTPP when combined with another mitochondria-targeting ligand (Chol-TPP). Lip-CTPP emerges as a potential carrier facilitating the collaborative anti-glioma efficacy of doxorubicin (DOX) and lonidamine (LND). It significantly enhances the inhibition of tumor cell proliferation, migration, and invasion, promotes apoptosis and necrosis, and disrupts mitochondrial function [1].