In vivo tumor targeting of ODN-PEG-folic acid/PEI polyelectrolyte complex micelles

Ji Hoon Jeong, Sun Hwa Kim, Sung Wan Kim, Tae Gwan Park

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

Abstract

A tumor-targeting antisense oligodeoxynucleotide (ODN) delivery system based on polyelectrolyte complex (PEC) micelles is demonstrated. ODN-PEG-folic acid (DN-PEG-FA) was synthesized using a heterofunctional PEG linker. The PEC micelles for the targeted ODN delivery to tumor cells were produced by ionic interactions between the ODN-PEG-FA and polyethylenimine (PEI). The in vivo targeting properties of the PEC micelles were assessed using a mouse tumor model. The size of ODN-PEG-FA/ PEI PEC micelles was 92.3 nm with a relatively narrow distribution. Cellular uptake of the ODN-PEG-FA/PEI PEC micelles by folic acid receptor over-expressing cells (KB) was greatly enhanced compared to that of ODN-PEG/PEI PEC micelles. When the ODN-PEG-FA/PEI PEC micelles were systematically administered to the mice bearing KB cell xenograft tumor, ODN was accumulated to the solid tumor in a target specific manner. This study suggests that the PEC micelles with a receptor-recognizable targeting ligand on the surface have potential for passive and active targeted delivery of ODN drugs to cancer cells.

Original languageEnglish
Pages (from-to)1409-1419
Number of pages11
JournalJournal of Biomaterials Science, Polymer Edition
Volume16
Issue number11
DOIs
StatePublished - Nov 2005
Externally publishedYes

Funding

This work was supported by the Ministry of Science and Technology, South Korea.

Keywords

  • Folic acid
  • Micelles
  • Oligodeoxynucleotide
  • Poly(ethyleneglycol)
  • Tumor targeting

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