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Enhanced Systemic Anti-Angiogenic siVEGF Delivery Using PEGylated Oligo-D-arginine

Title
Enhanced Systemic Anti-Angiogenic siVEGF Delivery Using PEGylated Oligo-D-arginine
Author
김용희
Keywords
angiogenesis; enhanced permeability and enhanced effect; siVEGF delivery; PEGylation; antitumor therapy
Issue Date
2017-07
Publisher
AMER CHEMICAL SOC
Citation
MOLECULAR PHARMACEUTICS, v. 14, no. 9, page. 3059-3068
Abstract
Angiogenesis mainly mediated by upregulation of vascular endothelial growth factor (VEGF) provides a hallmark of rapidly proliferating tumor cells and an essential component of the tumor growth and microenvironment, making it a targetable process for antitumor therapy. RNA interference (RNAi) provides a very effective tool for developing antitumor therapies; however, its application to date has been hampered due to the lack of efficient small interfering RNA (siRNA) delivery systems in vivo. Here, we report a polymeric gene carrier system based on PEGylation of a cationic cysteine-ended 9-mer arginine oligopeptide (CR9C), which provides effective siRNA systemic delivery and specifically suppresses VEGF (siVEGF). The PEG500-CR9C/siVEGF oligopeptoplex provided improved blood circulation, enhanced protection from serum proteases, reduced uptake in the liver and kidneys, enhanced tumor targeting, and down-regulated intratumoral VEGF level, which comprehensively resulted in improved antitumor efficacy without significant toxicity in vivo. PEG500-CR9C has a great potential for safe and efficient siRNA delivery with diverse applications.
URI
https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.7b00282https://repository.hanyang.ac.kr/handle/20.500.11754/114858
ISSN
1543-8384
DOI
10.1021/acs.molpharmaceut.7b00282
Appears in Collections:
COLLEGE OF ENGINEERING[S](공과대학) > BIOENGINEERING(생명공학과) > Articles
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