Targeting of stabilized plasmid lipid particles to hepatocytes in vivo by means of coupled lactoferrin

Weeke-Klimp, A. H., Bartsch, M., Morselt, H. W. M., Van Veen-Hof, I., Meijer, D. K. F., Scherphof, G. L. & Kamps, J. A. A. M., 2007, In : Journal of Drug Targeting. 15, 9, p. 585-594 10 p.

Research output: Contribution to journalArticleAcademicpeer-review

  • Alida H. Weeke-Klimp
  • Martin Bartsch
  • Henrieette W. M. Morselt
  • Ingrid Van Veen-Hof
  • Dirk K. F. Meijer
  • Gerrit L. Scherphof
  • Jan A. A. M. Kamps

For non-viral gene delivery we prepared stabilized plasmid lipid particles (SPLPs), to which lactoferrin (LF) was coupled as a hepatocyte specific targeting ligand. LF-SPLPs and untargeted SPLPs labeled with [H-3]cholesteryloleyl-ether were injected into rats. About 87% of the LF-SPLPs were eliminated from the blood within 5 min, while 80% of untargeted SPLPs were still circulating after 2 h. Fifty-two percent of the LF-SPLPs were taken up by hepatocytes, while non-parenchymal liver cells accounted for 16% of the uptake. Despite the efficient targeting of LF-SPLPs to hepatocytes and their capacity to transfect HepG2 and COS-7 cells in vitro, expression of a reporter gene was not detected in vivo. Overall, covalent coupling of LF to SPLPs leads to massive delivery in hepatocytes after systemic administration. However, these LF-SPLPs are not able to transfect these cells in vivo.

Original languageEnglish
Pages (from-to)585-594
Number of pages10
JournalJournal of Drug Targeting
Issue number9
Publication statusPublished - 2007


  • stabilized plasmid lipid particles, lactoferrin, gene targeting, hepatocytes, non-parenchymal liver cells, GENE-TRANSFER, RAT-LIVER, ENDOTHELIAL-CELLS, KUPFFER CELLS, BINDING, DNA, ACTIVATION, LIPOSOMES, DELIVERY, PROTEIN

ID: 4649694