title: Small peptide-modified nanostructured lipid carriers distribution and targeting to EGFR-overexpressing tumor in vivo.
abstract: 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.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , P. R. China.
authors.forename: Cuiyan
authors.initials: C
authors.lastname: Han
authors.forename: Yao
authors.initials: Y
authors.lastname: Li
authors.forename: Mingshuang
authors.initials: M
authors.lastname: Sun
authors.forename: Chang
authors.initials: C
authors.lastname: Liu
authors.forename: Xiaoxing
authors.initials: X
authors.lastname: Ma
authors.forename: Xinggang
authors.initials: X
authors.lastname: Yang
authors.forename: Yue
authors.initials: Y
authors.lastname: Yuan
authors.forename: Weisan
authors.initials: W
authors.lastname: Pan
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002232:Carbocyanines / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics*; D065546:Drug Liberation; D066246:ErbB Receptors / Q000378:metabolism*; D005240:Feasibility Studies; D005260:Female; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D008024:Ligands; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: C574020:1,1'-dioctadecyl-3,3,3',3'-tetramethylindotricarbocyanine; D002232:Carbocyanines; D004337:Drug Carriers; D008024:Ligands; D008055:Lipids; D009842:Oligopeptides; D066246:ErbB Receptors
keywords: AEYLR peptide; Cy7; DiR; EGFR; nanostructured lipid carriers; near-infrared fluorescent imaging; tumor targeting