Asialoglycoprotein receptors (ASGP‐R1 and R2), which are overexpressed in hepatocellular cancer cells, are favorable candidates for HCC‐targeting drug delivery.[12, 18] Herein, galactose, a ligand for ASGPRs, was chosen to functionalize the lipopolyplexes to further enhance tumor accumulation.[19] The in vivo real‐time distribution of lipopolyplexes was tracked on HCC PDX‐bearing BALB/c mice after a single intravenous injection of DiR‐loaded SLP (SLP/DiR) or Gal‐SLP (Gal‐SLP/DiR). This evidence concerns the gene GAL and hepatocellular carcinoma.