Tumor-homing glycol chitosan/polyethylenimine nanoparticles for the systemic delivery of siRNA in tumor-bearing mice

Myung Sook Huh, Seung Young Lee, Sangjin Park, Seulki Lee, Hyunjin Chung, Sojin Lee, Yongseok Choi, Yu Kyoung Oh, Jae Hyung Park, Seo Young Jeong, Kuiwon Choi, Kwangmeyung Kim, Ick Chan Kwon

Research output: Contribution to journalArticlepeer-review

145 Scopus citations


Here, we designed a new nano-sized siRNA carrier system composed of biocompatible/biodegradable glycol chitosan polymer (GC) and strongly positively charged polyethylenimine (PEI) polymers. In order to make a stable and tumor-homing nano-sized carrier, each polymer was modified with hydrophobic 5β-cholanic acid, and they were simply mixed to form self-assembled GC-PEI nanoparticles (GC-PEI NPs), due to the strong hydrophobic interactions of 5β-cholanic acids in the polymers. The freshly prepared GC-PEI NPs showed a stable nanoparticle structure (350. nm) and they presented a strongly positive-charged surface (ζ potential = 23.8) that is enough to complex tightly with negatively charged RFP-siRNAs, designed for inhibiting red fluorescent protein (RFP) expression. The siRNA encapsulated nanoparticles (siRNA-GC-PEI NPs) formed more compact and stable nanoparticle structures (250. nm) at 1: 5 weight ratio of siRNA to GC-PEI nanoparticles. In vitro RFP expressing B16F10 tumor cell (RFP/B16F10) culture system, the siRNA-GC-PEI NPs presented a rapid time-dependent cellular uptake profile within 1. h. Moreover, the internalized siRNA-GC-PEI NPs lead to specific mRNA breaks down. Furthermore, our new formulation of siRNA-GC-PEI NPs presented a significant inhibition of RFP gene expression of RFP/B16F10-bearing mice, due to their higher tumor-targeting ability. These results revealed the promising potential of GC-PEI NPs as a stable and effective nano-sized siRNA delivery system for cancer treatment.

Original languageEnglish
Pages (from-to)134-143
Number of pages10
JournalJournal of Controlled Release
Issue number2
StatePublished - Jun 2010

Bibliographical note

Funding Information:
This work was financially supported by the Real-Time Molecular Imaging Project , Global Research Laboratory , and by the National Research Foundation (Pioneer Research Center; 2009-0081523, Fusion Technology Project; 2009-0081876, and 2009k001595) of Korea funded by MEST, and by the grant to the Intramural Research Program of the KIST (Theragnosis).


  • Cancer treatment
  • Glycol chitosan
  • Nanoparticle delivery system
  • Polyethylenimine
  • SiRNA
  • Tumor-targeting delivery


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