文獻名：Protein corona precoating on redox-responsive chitosan-based nano-carriers for improving the therapeutic effect of nucleic acid drugs

作者： Han Yang^a，Tingting Liu^a，Yan Xu^a，Gaoxing Su^a，Tianqing Liu^b，Yanyan Yu^a，Bohui Xu^a

^a School of Pharmacy, Nantong University, No. 19 Qixiu Road, Nantong, 226001, China

^b NICM Health Research Institute, Western Sydney University, Westmead, Australia

摘要：Spontaneous formation of protein corona on chitosan-based nano-carriers is inevitable once they enter the blood, which is considered to be an important factor that weakens the delivery efficiency and therapeutic effect of nucleic acid drugs. For this, cyclic RGDyK peptide (cRGD) modified bovine serum albumin (BSA) was designed as a corona to precoat on redox-responsive chitosan-based nano-carriers (TsR NPs) before administration. The effects of the precoating corona on the pharmaceutical properties and delivery efficiency of the nano-carriers and the therapeutic effect of model siRNA (siVEGF) were investigated. The results showed that BSA-cRGD formed steady corona around TsR NPs, which enhanced targeting ability to cancer cells and reduced serum proteins adsorption. The Bc corona improved the stability and biocompatibility of TsR NPs, increased the intracellular uptake, facilitated the lysosomal escape and maintained their redox-sensitive responsiveness, resulting in enhanced gene silencing efficiency and anti-tumor proliferation effects both in vitro and in vivo.

關鍵詞：Protein corona，Precoating，Chitosan，BSA-cRGD，Redox-responsive，siRNA