Self-assembly nanoparticles based on c(RGDfk) peptide for the delivery of siRNA targeting VEGFR2 gene for tumor therapy
The clinical application of small interference RNA (siRNA) has been restricted by poor intracellular uptake, low serum stability, non-targeting property et al.During last decades, a lot of effort has been devoted to explore materials for siRNA delivery.In this study, a biodegradable, tumor-targeted, peptide self-assembled nanoparticles (NPs) (c(RGDfk)-PEG-MAL hereinafter referred to as RPM) was found to be an effective siRNA carrier both in vitro and in vivo.The characterizations of the NPs were well studied by transmission electron microscopy (TEM), circular dichroism (CD) spectrum and dynamic light scattering (DLS).Studies in vitro demonstrated that RPM/VEGFR2-siRNA NPs are negligible cytotoxicity and can lead to gene silencing in HUVECs effectively.The study on zebra-fish showed it”s inhibition of neovascularization.And studies on animal model of tumor bearing nude mice indicated that it can significantly inhibit the tumor growth, remarkably reduce the vessels in tumor tissue, and down VEGFR2 (mRNA and protein) expression obviously.Furthermore, no immunogenicity was found by ELISA assay suggested RPM is negligible biological toxicity in vivo.In conclusion, RPM may provide a safe and effective delivery vector for the clinical application of siRNA in the near future.
siRNA delivery self-assembly nanoparticles tumor-targeting gene silencing
Li Liu Xiaoxia Liu Qian Xu Ping Wu Xialin Zuo Jingjing Zhang Houliang Deng Zhuomin Wu Aimin Ji
Department of Pharmacy,Zhujiang hospital,Southern Medical University,Guangzhou,Guangdong 510282,PR China.Zhujiang Hospital,Southern Medical University 253 Industry Avenue Guangzhou 510282 P.R.China
国内会议
广州
英文
61-76
2014-01-11（万方平台首次上网日期，不代表论文的发表时间）