Compared with NLCs modified by non-cleavable FA/dNP2 or a single ligand, cFA/dNP2-GA/PTX-NLC exhibited higher accumulation in breast cancer in vivo bio-distribution study, induced an enhancement of apoptosis, and achieved the maximal anticancer efficiency of GA and PTX by retaining the synergistic tumor targeting and penetration of FA and dNP2. Here, TBCA is linked to neoplasm.