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Peptides have recently emerged as a promising class of targeting ligands for specific drug delivery in cancer treatment, which avoid undesirable side effects of the systemic administration of chemotherapeutics. Their conjugation with nanoparticles has been demonstrated to improve the functionality of peptides resulting in a versatile platform for biomedical applications. In this work, the development of carboxymethylchitosan/poly(amidoamine) (CMCht/PAMAM) dendrimer nanoparticles functionalized with YIGSR laminin receptor binding peptide for the active targeting and specific delivery of therapeutic agents into colorectal cancer cells is described. The successful functionalization is confirmed by several physico‐chemical characterization techniques. The selectivity of the YIGSR‐CMCht/PAMAM dendrimer nanoparticles is first validated in vitro using a micropatterned array of 67 kDa laminin receptor. Next, the …