The site-directed conjugation to monovalent CTX-Fab’ fragments rendered liposomes with enhanced tumor accumulation (2916.0 ± 507.84 ng/g) compared to CTX (1546.02 ± 362.41 ng/g) or in the absence of targeting ligands (891.06 ± 155.1 ng/g), which also improved efficacy in mice inoculated with EGFR-positive colorectal cancer cells and treated with three i.v. 2.5 mg/kg doses at days 12, 15, and 18 post-cancer-cell implantation. Here, EGFR is linked to cancer.