Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment

Zhu, Hongyan; Liu, Wanwan; Cheng, Ziting; Yao, Ke; Yang, Yu; Xu, Bohui; Su, Gaoxing

doi:10.3390/ijms18102029

Open AccessArticle

Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment

by

Hongyan Zhu

^*,

Wanwan Liu

,

Ziting Cheng

,

Ke Yao

,

Yu Yang

,

Bohui Xu

and

Gaoxing Su

^*

School of Pharmacy, Nantong University, Nantong 226001, China

^*

Authors to whom correspondence should be addressed.

Int. J. Mol. Sci. 2017, 18(10), 2029; https://doi.org/10.3390/ijms18102029

Submission received: 7 September 2017 / Revised: 18 September 2017 / Accepted: 18 September 2017 / Published: 22 September 2017

(This article belongs to the Special Issue Bioactive Nanoparticles)

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Abstract

In this work, we report the engineering of gold nanostars (GNS) to deliver small interfering RNA (siRNA) into HepG2 cells. The ligand DG-PEG-Lipoic acid (LA)-Lys-9R (hydrazone) was designed to functionalize GNS, and create the nanoparticles named as 9R/DG-GNS (hydrazone). In the ligand, 2-deoxyglucose (DG) is the targeting molecule, polyethylene glycol (PEG) helps to improve the dispersity and biocompatibility, 9-poly-d-arginine (9R) is employed to provide a positive surface charge and adsorb negative siRNA, and hydrazone bonds are pH-responsive and can avoid receptor-mediated endosomal recycling. Compared to GNS alone, 9R/DG-GNS (hydrazone) showed superior transfection efficiency. The expressions of cyclooxygenase-2 (COX-2) in HepG2 and SGC7901 cells were significantly suppressed by siRNA/9R/DG-GNS (hydrazone) complex. Notably, 9R/DG-GNS (hydrazone) possessed low cytotoxicity even at high concentrations in both normal cells and tumor cells. The combination treatment of siRNA/9R/DG-GNS (hydrazone) complex inhibited the cell growth rate by more than 75%. These results verified that the pH-responsive GNS complex is a promising siRNA delivery system for cancer therapy, and it is anticipated that near-infrared absorbing GNS with good photothermal conversion efficiency can be potentially used for photothermal therapy of tumors.

Keywords: gold nanostars; targeted delivery; siRNA; cancer treatment; cyclooxygenase-2; gene silence

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MDPI and ACS Style

Zhu, H.; Liu, W.; Cheng, Z.; Yao, K.; Yang, Y.; Xu, B.; Su, G. Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment. Int. J. Mol. Sci. 2017, 18, 2029. https://doi.org/10.3390/ijms18102029

AMA Style

Zhu H, Liu W, Cheng Z, Yao K, Yang Y, Xu B, Su G. Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment. International Journal of Molecular Sciences. 2017; 18(10):2029. https://doi.org/10.3390/ijms18102029

Chicago/Turabian Style

Zhu, Hongyan, Wanwan Liu, Ziting Cheng, Ke Yao, Yu Yang, Bohui Xu, and Gaoxing Su. 2017. "Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment" International Journal of Molecular Sciences 18, no. 10: 2029. https://doi.org/10.3390/ijms18102029

APA Style

Zhu, H., Liu, W., Cheng, Z., Yao, K., Yang, Y., Xu, B., & Su, G. (2017). Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment. International Journal of Molecular Sciences, 18(10), 2029. https://doi.org/10.3390/ijms18102029

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Targeted Delivery of siRNA with pH-Responsive Hybrid Gold Nanostars for Cancer Treatment

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