Theranostic Quercetin Nanoparticle for Treatment of Hepatic Fibrosis.
Qiang ZhangDan XuQiuyan GuoWenjun ShanJun YangTongtong LinShefang YeXi ZhouYunlong GeShengli BiLei RenPublished in: Bioconjugate chemistry (2019)
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.
Keyphrases
- fluorescence imaging
- photodynamic therapy
- cancer therapy
- magnetic resonance imaging
- living cells
- systematic review
- randomized controlled trial
- quantum dots
- fluorescent probe
- high resolution
- drug delivery
- magnetic resonance
- contrast enhanced
- computed tomography
- iron oxide
- climate change
- oxidative stress
- small molecule
- combination therapy
- walled carbon nanotubes
- cell cycle arrest
- label free
- pulmonary fibrosis
- smoking cessation
- cell adhesion
- pi k akt
- dna binding