Effect of the stability and deformability of self-assembled glycol chitosan nanoparticles on tumor-targeting efficiency

Jin Hee Na, Seung Young Lee, Sangmin Lee, Heebeom Koo, Kyung Hyun Min, Seo Young Jeong, Soon Hong Yuk, Kwangmeyung Kim, Ick Chan Kwon

Research output: Contribution to journalArticlepeer-review

88 Citations (Scopus)


To evaluate the tumor targeting efficiency of self-assembled polymeric nanoparticles, four glycol chitosan nanoparticles (CNPs) with different degrees of hydrophobic substitution were prepared by coupling 7.5, 12, 23, and 35 wt.% of 5β-cholanic acid to hydrophilic glycol chitosan polymer (GC). The sizes and zeta-potentials of different CNPs in aqueous condition were not significantly different, but their stability and deformability were greatly dependent upon the degree of substitution (DS) of 5β-cholanic acid. With an increase in hydrophobicity, CNPs became more stable and rigid, as characterized by SDS-PAGE and filtration tests. To compare with CNPs, linear GC and polystyrene nanoparticles (PSNPs) were employed as controls. In vivo tumor accumulation of Cy5.5-labeled linear GC, polystyrene nanoparticles (PSNPs) and CNPs were monitored in flank tumors and liver tumor-bearing mice models using near-infrared fluorescence (NIRF) imaging systems. CNPs displayed higher tumor accumulation than GC and PSNPs via the enhanced permeability and retention (EPR) effect. Interestingly, CNPs containing 23 wt.% of 5β-cholanic acid (CNP-23%) showed the highest tumor-targeting efficiency compared to other CNPs. As exemplified in this study, the stability of CNP-23% is better than CNP-7.5% and CNP-12% containing 7.5 wt.% and 12 wt.% of 5β-cholanic acid, respectively, and the deformability of CNP-23% is better than that of CNP-35% containing 35 wt.% of 5β-cholanic acid. We proposed that the superior tumor-targeting efficiency of CNP-23% is mainly due to their balanced stability and deformability in vivo. This study demonstrates that the degree of hydrophobic substitution of self-assembled nanoparticles could determine their stability and deformability. Importantly, they were founded to be the key factors which affect their tumor-targeting efficiency in vivo, and so that these factors should be highly considered during developing nanoparticles for tumor-targeted imaging or drug delivery.

Original languageEnglish
Pages (from-to)2-9
Number of pages8
JournalJournal of Controlled Release
Issue number1
Publication statusPublished - 2012 Oct 10

Bibliographical note

Funding Information:
This study was funded by the GRL Program, M.D.-Ph.D. Program ( 2010–0019863 , 2010–0019864 ), the Fusion Technology Project ( 2009–0081876 ) of MEST and the Intramural Research Program (Theragnosis) of KIST.

Copyright 2013 Elsevier B.V., All rights reserved.


  • Deformability
  • Degree of substitution
  • Glycol chitosan nanoparticles
  • In vivo imaging
  • Stability
  • Tumor targeting

ASJC Scopus subject areas

  • Pharmaceutical Science


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