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In vitro Cytotoxicity Assays Tumor angiogenesis promotes HCC development and metastasis. To investigate the in vitro cytotoxicity of different drug formulations, both MTT and Live/Dead assay were carried out on two-level cell culture systems (Figure 4C, Supporting Figure 1): BEL7402 cells alone or BEL7402/HUVEC co-cultured cells. As shown in Figure 4Dand E, all drug treatment groups showed concentration-dependent cytotoxicity against BEL7402 cells and co-cultured system. Meanwhile, the CUCA/GA&Gal-Lip exhibited higher toxicity than CUCA/Lip and CUCA/Gal-Lip. It might be attributed to the stronger liver-targeting capability of dual-ligand-modified Lip, which was shown in the cellular uptake analysis (Figure 3). Interestingly, the IC

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