RGDS covalently surfaced nanodiamond as a tumor targeting carrier of VEGF-siRNA: synthesis, characterization and bioassay

Chunying Cui; Yaonan Wang; Wen Zhao; Kaikai Yang; Xueyun Jiang; Shan Li; Ming Zhao; Yuanbo Song; Shiqi Peng

doi:10.1039/c5tb01602a

RGDS covalently surfaced nanodiamond as a tumor targeting carrier of VEGF-siRNA: synthesis, characterization and bioassay

J Mater Chem B. 2015 Dec 28;3(48):9260-9268. doi: 10.1039/c5tb01602a. Epub 2015 Nov 13.

Authors

Chunying Cui¹, Yaonan Wang, Wen Zhao, Kaikai Yang, Xueyun Jiang, Shan Li, Ming Zhao, Yuanbo Song, Shiqi Peng

Affiliation

¹ School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, Beijing 100069, China. sqpeng@bjmu.edu.cn mingzhao@bjmu.edu.cn.

PMID: 32262925
DOI: 10.1039/c5tb01602a

Abstract

A nonviral tumor targeting vector for siRNA transfer is of importance. Here, a novel delivery system consisting of a covalent conjugate of NDCO-RGDS and VEGF-siRNA, NDCO-RGDS/VEGF-siRNA, was presented. In vitro, NDCO-RGDS/VEGF-siRNA released and transferred VEGF-siRNA in a long-acting manner. Compared to the control, NDCO-RGDS/VEGF-siRNA decreased the expression of VEGF mRNA and protein in HeLa cells by 88.41 ± 3.49% and 83.94 ± 2.00%, respectively. In vivo, NDCO-RGDS/VEGF-siRNA exhibited gene silencing and slowed tumor growth. FT-MS spectrum analysis revealed that NDCO-RGDS/VEGF-siRNA mainly distributed in tumor tissue of the treated S180 mice. Therefore NDCO-RGDS could be considered a promising nonviral tumor-targeting vector for siRNA transfer in tumor therapy.