Liver cancer is one of the most common human malignancies worldwide. Currently, chemotherapy remains the cornerstone for liver cancer treatment. However, chemotherapy often causes many side effects, such as leukopenia, digestive reaction, hepatic and renal dysfunction and hair loss. Recently, great advances in nanoparticles-based liver-targeting drug delivery systems have been developed to overcome these problems. Glycyrrhetinic acid (GA), a pentacyclic triterpenoid extracted from the root of licorice, and has been widely used in liver cancer therapy. GA is capable of binding to hepatocytes via the specific site of GA-R on the surface of hepatic parenchymatous cells. From this prospective, this review highlights GA-mediated nanoparticles liver-targeting drug delivery systems from different polymer materials.