Small peptide-modified nanostructured lipid carriers distribution and targeting to EGFR-overexpressing tumor in vivo.

Ala-Glu-Tyr-Leu-Arg (AEYLR) was identified as a small peptide ligand targeting epidermal growth factor receptors (EGFR) in vitro in our previous study. The in vivo targeting ability of AEYLR and AEYLR-conjugated nanostructured lipid carriers (NLC) was studied in this paper. Near-infrared fluorescent (NIFR) dye 1,1'-dioctadecyltetramethyl indotricarbocyanine iodide (DiR)-loaded and AEYLR-modified NLC (A-D-NLC) were prepared. The average diameter, zeta potential, coupling efficiency between AEYLR and NLC and the amount of DiR released from A-D-NLC were used to evaluate their in vivo characteristics. AEYLR was labeled by Cy7 and A549 xenograft tumor-bearing mice model were establish. The in vivo distribution in tumor-bearing mice of A-D-NLC and Cy7-AEYLR was examined using NIRF imaging experiments at different times post-injection. AEYLR and AEYLR-conjugated NLC showed obvious targeting to A549 xenograft tumor compared with the control group. These results suggested that AEYLR-modified NLC could be considered as a promising targeted delivery system for combination cancer chemotherapy to improve therapeutic efficacy and to minimize adverse effects.