Targeting selenium nanoparticles combined with baicalin to treat HBV-infected liver cancer

Abstract

As a traditional Chinese medicine, baicalin exhibits high antitumor activity towards hepatitis B virus (HBV)-infected liver cancer, but low toxicity towards normal tissues. However, the properties of baicalin, including its low hydrophilicity and poor biocompatibility, have limited its clinical application. Herein, in this study, we have designed and synthesized multifunctional selenium nanoparticles (SeNPs) with baicalin (B) and folic acid (FA) surface-modifications for the targeted treatment of HBV infected liver cancer. B–SeNPs–FA showed appropriate particle size distribution, high stability, and higher cellular uptake by tumor cells than normal cells. The nanoparticles primarily targeted lysosomes in HepG2215 cells through utilization of the main pathways of caveolae-mediated endocytosis and energy-dependent endocytosis. B–SeNPs–FA induced HepG2215 cell apoptosis by down-regulating the generation of reactive oxygen species (ROS) and the expression of the HBxAg protein. In addition, B–SeNPs–FA exhibited an excellent ability to inhibit cancer cell migration and invasion. Taken together, these results suggest that baicalin-loaded selenium nanoparticles with a folic acid targeting moiety could be a promising strategy for the design and synthesis of cancer-targeted nanomaterials to treat HBV-infected liver cancer.