Skip to main content
Article thumbnail
Location of Repository

FGF Receptor-Mediated Gene Delivery Using Ligands Coupled to PEI-β-CyD

By Yiping Hu, Guping Tang, Jun Liu, Wenxiang Cheng, Ye Yue, Jinchao Li and Peng Zhang


A novel vector with high gene delivery efficiency and special cell-targeting ability was developed using a good strategy that utilized low-molecular-weight polyethylenimine (PEI; molecular weight: 600 KDa [PEI600]) crosslinked to β-cyclodextrin (β-CyD) via a facile synthetic route. Fibroblast growth factor receptors (FGFRs) are highly expressed in a variety of human cancer cells and are potential targets for cancer therapy. In this paper, CY11 peptides, which have been proven to combine especially with FGFRs on cell membranes were coupled to PEI-β-CyD using N-succinimidyl-3-(2-pyridyldithio) propionate as a linker. The ratios of PEI600, β-CyD, and peptide were calculated based on proton integral values obtained from the 1H-NMR spectra of the resulting products. Electron microscope observations showed that CY11-PEI-β-CyD can efficiently condense plasmid DNA (pDNA) into nanoparticles of about 200 nm, and MTT assays suggested the decreased toxicity of the polymer. Experiments on gene delivery efficiency in vitro showed that CY11-PEI-β-CyD/pDNA polyplexes had significantly greater transgene activities than PEI-β-CyD/pDNA in the COS-7 and HepG2 cells, which positively expressed FGFR, whereas no such effect was observed in the PC-3 cells, which negatively expressed FGFR. Our current research indicated that the synthesized nonviral vector shows improved gene delivery efficiency and targeting specificity in FGFR-positive cells

Topics: Research Article
Publisher: Hindawi Publishing Corporation
OAI identifier:
Provided by: PubMed Central
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • http://www.pubmedcentral.nih.g... (external link)
  • Suggested articles


    1. (2011). A novel truncated basic fibroblast growth factor fragment-conjugated poly (ethylene glycol)-cholesterol amphiphilic polymeric drug delivery system for targeting to the FGFR-overexpressing tumor cells,”
    2. (2007). A unique and highly efficient nonviral DNA/siRNA delivery system based on PEI-bisepoxide nanoparticles,”
    3. (2008). C h u m a k o v a ,A .V .L i o p o ,V .G .A n d r e e ve ta l .
    4. (2007). FGF receptor-mediated gene delivery using ligands coupled to polyethylenimine,”
    5. (2011). G.Liu,J.Xie,F.Zhangetal.,“N-Alkyl-PEI-functionalizediron oxide nanoclusters for efficient siRNA delivery,”
    6. (2011). Gellan gum blended PEInanocompositesasgenedeliveryagents:evidencesfromin vitro and in vivo studies,”
    7. (2011). Highly effective gene transfection in vivo by alkylated polyethylenimine,”
    8. (2002). Identification of FGF receptor-binding peptides for cancer gene therapy,”
    9. (2005). Improvement of gene delivery mediated by mannosylated dendrimer/α-cyclodextrin conjugates,”
    10. (2006). Low molecular weight polyethylenimines linked by β-cyclodextrin for gene transfer into the nervous system,”
    11. (1995). O.Boussif,F.LezoualC’H,M.A.Zantaetal.,“Aversatilevector for gene and oligonucleotide transfer into cells in culture and in vivo: polyethylenimine,”
    12. (2005). P a c k ,A .S .H o ffm a n ,S .P u n ,a n dP .S .S t a y t o n ,“ D e s i g n and development of polymers for gene delivery,” Nature Reviews Drug Discovery,
    13. (2005). Polyethylene glycol-conjugated copolymers for plasmid
    14. (2010). Polyethyleneiminemodified iron oxide nanoparticles for brain tumor drug delivery using magnetic targeting and intra-carotid administration,”
    15. (2011). R .B a h a d u ra n dH .U l u d a ˇ g, “A comparative evaluation of disulfide-linked and hydrophobically-modified PEI for plasmid delivery,”
    16. (2005). Recent advances in rational gene transfer vector design based on poly(ethylene imine) and its derivatives,”
    17. (2008). Synthesis and characterization of folate-PEG-grafted-hyperbranched-PEI for tumortargeted gene delivery,”
    18. (2004). Transgenic mice overexpressing human fibroblast growth factor 23 (R176Q) delineate a putative role for parathyroid hormone in renal phosphate wasting disorders,”

    To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.