Abstract
Macromolecular nanoparticles can extravasate and accumulate within tumor tissues via the passive targeting system, reflecting enhanced permeability and the retention effect. However, the unsatisfactory tumor therapeutic efficacy of the passive-targeting system, attributable to the retention of extravasated nanoparticles in the vicinity of tumor vessels, argues that a new system that facilitates intracellular delivery of nanoparticles within tumors is needed. Here, we developed hydrophobically modified glycol chitosan (HGC) nanoparticles conjugated with interleukin-4 receptor (IL-4R) binding peptides, termed I4R, and tested them in mice bearing IL-4R-positive tumors. These HGC-I4R nanoparticles exhibited enhanced IL-4R-dependent cellular uptake in tumors compared to nonconjugated nanoparticles, leading to better therapeutic and imaging efficacy. We conclude that I4R facilitates and enhances cellular uptake of nanoparticles in tumor tissues. This study suggests that the intracelluar uptake of nanoparticles in tumors is an essential factor to consider in designing nanoparticles for tumor-targeted drug delivery and imaging.
Original language | English |
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Pages (from-to) | 493-499 |
Number of pages | 7 |
Journal | Journal of Controlled Release |
Volume | 157 |
Issue number | 3 |
DOIs | |
State | Published - 10 Feb 2012 |
Bibliographical note
Funding Information:This research was supported by the WCU (World Class University) program through the Korea Science and Engineering Foundation ( R33-2008-000-10054-0 ), the National Research foundation of Korea (NRF) grant funded by the Korea government (MEST) ( 2010-0029206 , 2011-001043 0), and the Converging Research Center Program through the Ministry of Education, Science and Technology ( 2010K001054 ).
Keywords
- Cancer imaging
- Cancer therapy
- Homing peptide
- Nanoparticles
- Tumor targeting