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However, it is inefficient in inhibiting tumor metastasis. MicroRNA\u201010b is uninvolved in regulating the growth of primary tumors; however, it could induce early tumor metastases and is a key regulator of chemotherapeutic resistance to 5\u2010FU. A multifunctional nanovehicle that can carry small molecule drugs not only through the hydrophobic pockets of conjugated <jats:italic>\u03b2<\/jats:italic>\u2010cyclodextrin but also through electrostatic interaction between the conjugated peptides and siRNA to target functional genes is previously developed. In this study, a nanovehicle, named GCD, with epithelium growth factor receptor (EGFR)\u2010targeted characteristics to simultaneously deliver chemotherapeutic and nucleotide drugs to distinct targets in CRC, is employed. These data show that co\u2010delivery of 5\u2010FU and anti\u2010miR\u201010b can be effectively applied to targeted therapy of EGFR\u2010overexpressed CRC, particularly inhibiting the metastasis of CRC. 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