The spacer arm length in cell-penetrating peptides influences chitosan/siRNA nanoparticle delivery for pulmonary inflammation treatment
- Authors
- Jeong, Eun Ju; Choi, Moonhwan; Lee, Jangwook; Rhim, Taiyoun; Lee, Kuen Yong
- Issue Date
- Dec-2015
- Publisher
- ROYAL SOC CHEMISTRY
- Citation
- NANOSCALE, v.7, no.47, pp.20095 - 20104
- Indexed
- SCIE
SCOPUS
- Journal Title
- NANOSCALE
- Volume
- 7
- Number
- 47
- Start Page
- 20095
- End Page
- 20104
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/155665
- DOI
- 10.1039/c5nr06903c
- ISSN
- 2040-3364
- Abstract
- Although chitosan and its derivatives have been frequently utilized as delivery vehicles for small interfering RNA (siRNA), it is challenging to improve the gene silencing efficiency of chitosan-based nanoparticles. In this study, we hypothesized that controlling the spacer arm length between a cell-penetrating peptide (CPP) and a nanoparticle could be critical to enhancing the cellular uptake as well as the gene silencing efficiency of conventional chitosan/siRNA nanoparticles. A peptide consisting of nine arginine units (R-9) was used as a CPP, and the spacer arm length was controlled by varying the number of glycine units between the peptide (R(9)G(n)) and the nanoparticle (n = 0, 4, and 10). Various physicochemical characteristics of R(9)G(n)-chitosan/siRNA nanoparticles were investigated in vitro. Increasing the spacing arm length did not significantly affect the complex formation between R(9)G(n)-chitosan and siRNA. However, R(9)G(10)-chitosan was much more effective in delivering genes both in vitro and in vivo compared with nonmodified chitosan (without the peptide) and R-9-chitosan (without the spacer arm). Chitosan derivatives modified with oligoarginine containing a spacer arm can be considered as potential delivery vehicles for various genes.
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