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The Pharmaceutical Society of Korea (대한약학회)
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Evaluation of Transferrin-Polyethylenimine Conjugate for Targeted Gene Delivery

  • Lee Kyung Man (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Kim In Sook (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Lee Yong Bok (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Shin Sang Chul (College of Pharmacy and Research Institute of Drug Development, Chonnam National University) ;
  • Lee Kang Choon (College of Pharmacy, SungKyunKwan University) ;
  • Oh In Joon (College of Pharmacy and Research Institute of Drug Development, Chonnam National University)
  • Published : 2005.06.01
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Abstract

With the aim to improve the specificity and to reduce the cytotoxicity of polyethylenimine (PEI), we have synthesized the conjugates of the branched PEI (25 kDa) with transferrin. The trans-ferrin-PEI (TP) conjugates with five compositions were synthesized using periodate oxidation method and confirmed by FT-IR spectroscopy and gel permeation chromatography. The free amine contents of TP conjugates, which were able to condense and deliver DNA, increased as the amount of PEI increased. TP/DNA polyplexes were characterized by measuring gel elec-trophoresis, ethidium bromide fluorescence quenching, particle size and zeta potential of complexes. Complete complexation of the polyplexes was observed above the N/P ratio of 5 in TP/DNA, and above 3 in PEI/DNA, respectively. The zeta potential of the complexes decreased as the amount of transferrin in TP conjugates increased. Transfection efficiency of TP conjugates was evaluated in HeLa cell and Jurkat cell systems. Among the five compositions of TP conjugates, TP-2 system mediated a higher $\beta$-galactosidase gene expression than PEI system in Jurkat cell which was known to express elevated numbers of transferrin receptors. From the results of the cell viability based on MTT assay, TP conjugates showed lower cytotoxicity com-pared with the PEI system. We expect that the TP conjugate can be used efficiently as a non-viral gene delivery vector.

Keywords

References

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