title: New tumor-targeted nanosized delivery carrier for oligonucleotides: characteristics in vitro and in vivo.
abstract: BACKGROUND
  The purpose of this study was to investigate the in vitro and in vivo characteristics of a new tumor-targeted nanosized delivery carrier for antisense oligonucleotide (ASON).
  
  
  METHODS
  Polyethylenimine (PEI) was used to condense ASON to form nanosized complexes (PEI/ASON), which were then modified using asparagine-glycine-arginine (NGR) peptide to obtain a tumor-targeted nanosized delivery carrier (NGR/PEI/ASON). The conditions required to form PEI/ASON were investigated.
  
  
  RESULTS
  A linear correlation between the natural logarithm of the N/P ratio (PEI to ASON) and the zeta potential of the PEI/ASON complexes was found, ranging from 1.5 to 5.0. The pH of the solution strongly influenced the zeta potential of the PEI/ASON complexes. PEI/ASON and NGR/PEI/ASON were stable in RPMI-1640 culture medium in the presence of Dextran 70. Incorporation of ASON into PEI/ASON and NGR/PEI/ASON complexes prevented degradation of ASON by DNase I.
  
  
  CONCLUSIONS
  Both ASON/PEI and NGR/PEI/ASON complexes enhanced the uptake of ASON by EC9706 cells in vitro. In vivo, NGR/PEI/ASON complexes had the ability to target tumor tissues effectively.
authors.affiliation: School of Pharmaceutical Sciences, Medical School of Zhengzhou University, Zhengzhou, People's Republic of China.
authors.forename: Tianyang
authors.initials: T
authors.lastname: Zhou
authors.forename: Xin
authors.initials: X
authors.lastname: Jia
authors.forename: Huixiang
authors.initials: H
authors.lastname: Li
authors.forename: Jin
authors.initials: J
authors.lastname: Wang
authors.forename: Hongling
authors.initials: H
authors.lastname: Zhang
authors.forename: Youmei
authors.initials: Y
authors.lastname: A
authors.forename: Zhenzhong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D003850:Deoxyribonuclease I / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D018613:Microscopy, Confocal; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D009374:Neoplasms, Experimental; D016376:Oligonucleotides, Antisense / Q000008:administration & dosage / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry; D011094:Polyethyleneimine / Q000737:chemistry; D055672:Static Electricity; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; C526428:NGR peptide; D016376:Oligonucleotides, Antisense; D009842:Oligopeptides; D011094:Polyethyleneimine; D003850:Deoxyribonuclease I