5A2-SC8 TFA is an ionizable amino lipid used in lipid nanoparticles (LNPs), offering high delivery potential and low in vivo toxicity. It effectively delivers small RNAs, such as siRNA and miRNA, to tumor cells. Moreover, 5A2-SC8 TFA LNPs provide unique delivery paths for RNA within the liver, enhancing therapeutic outcomes in cancer models.

5A2-SC8 LNPs have ApoE protein coronas on their surfaces, which bind to LDL-R on hepatocyte surfaces and are taken up by these cells through receptor-mediated endocytosis.

Administered intravenously, 5A2-SC8 (75 mg/kg;I.V.; single dose) is well-tolerated by mice with chronic aggressive liver cancer, showing no impact on survival. Additionally, 5A2-SC8 (0.5 mg/kg; i.v.; 6 h) facilitates the passage of Cy5.5 dye-labeled siFVII through the Kupffer cells in the liver, leading to its internalization into hepatocytes.