posted on 2019-11-01, 18:40authored byQiang Zhang, Dan Xu, Qiuyan Guo, Wenjun Shan, Jun Yang, Tongtong Lin, Shefang Ye, Xi Zhou, Yunlong Ge, Shengli Bi, Lei Ren
The progression of
hepatic fibrosis can lead to cirrhosis and hepatic
failure, but the development of antifibrotic drugs have faced the
challenges of poor effectiveness and targeted specificity. Herein,
a theranostic strategy was carried to encapsulate a natural medicine
(Quercetin, QR) into hepatitis B core (HBc) protein nanocages (NCs)
for imaging and targeted treatment of hepatic fibrosis. It was noted
that nanoparticles (RGD-HBc/QR) with surface-displayed RGD targeting
ligand exhibit a rather high selectivity toward activated HSCs via
the binding affinity with integrin αvβ3, and an efficient inhibition of proliferation and activation
of hepatic stellate cells (HSCs) in vitro and in vivo. Once encapsulated
in quercetin–gadolinium complex and/or labeled with the NIR
fluorescent probes (Cy5.5), the resulting nanoparticles (RGD-HBc/QGd)
show great potential as NIR fluorescent and magnetic resonance imaging
contrast agents for hepatic fibrosis in vivo. Therefore, the multifunctional
integrin-targeted nanoparticles could selectively deliver QR to the
activated HSCs, and may provide an effective antifibrotic theranostic
strategy.