What is it about?
This review summarizes recent progress in biomaterials functionalized with glycyrrhetinic acid (GA) for targeted liver cancer therapy. GA, a triterpenoid from licorice roots, binds specific receptors on hepatocyte membranes, making it a promising ligand to improve the selectivity of drug delivery systems (DDSs). The article highlights GA‑modified nanoparticles, hybrid compounds, and multifunctional carriers designed to enhance drug uptake into liver cancer cells, reduce systemic toxicity, and increase therapeutic efficacy. It also covers emerging GA‑based systems capable of delivering multiple agents, nucleic acids (siRNA/pDNA), or photodynamic therapy (PDT) photosensitizers.
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Why is it important?
Conventional chemotherapy for liver tumors suffers from limited selectivity, high toxicity, and resistance mechanisms. Targeted DDSs decorated with GA offer a strategy to increase drug accumulation in hepatocytes while minimizing exposure to healthy tissues. The review outlines how GA‑functionalized materials may improve bioavailability, intracellular delivery, and endosomal escape, and how the intrinsic biological activity of GA could provide additional therapeutic contributions. These characteristics make GA‑based platforms relevant tools for improving the management of hepatocellular carcinoma.
Perspectives
Although promising, most GA‑functionalized systems have only been tested in vitro or in limited in vivo models. Their translation faces challenges including incomplete knowledge of hepatic GA receptors, variability in receptor expression, and uncertainties about their physiological roles. Additional concerns involve drug–GA interactions with metabolic enzymes (CYP450, UGTs), potential modulation of P‑glycoprotein, and licorice‑related adverse effects such as pseudohyperaldosteronism. Furthermore, the complexity of producing advanced GA‑based DDSs raises issues of reproducibility, scale‑up, quality control, and cost. Future studies must better characterize receptor biology, safety, and pharmacokinetics, and evaluate GA‑functionalized biomaterials in clinically relevant models before considering therapeutic applications.
Prof. Antonio Speciale
University of Messina
Read the Original
This page is a summary of: Recent Advances in Glycyrrhetinic Acid-Functionalized Biomaterials for Liver Cancer-Targeting Therapy, Molecules, March 2022, MDPI AG,
DOI: 10.3390/molecules27061775.
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