Review
Copyright ©The Author(s) 2024.
World J Hepatol. Feb 27, 2024; 16(2): 164-176
Published online Feb 27, 2024. doi: 10.4254/wjh.v16.i2.164
Table 1 Summary of nanoformulations utilizing Glypican-3 as a targeting receptor in hepatocellular carcinoma treatment
Targeting ligand
Particle size
Nanocarrier
Payload
In vitro or/and in vivo results
GC33[54]100-150 nmPEG PLGASorafenibGC33 modified nanoparticles in vitro: Specifically target GPC3-positive HepG2 cells, resulting in cell cycle arrest at G0/1 phase; in vivo: Inhibit the growth of liver cancer and improve the survival rate of tumor-bearing mice
YP7[55]N/AAlbuminPaclitaxelYP-7 bounded-nanoparticles induce rapid target-specific necrotic cell death and increase the concentration of paclitaxel within HCC tumors
Clone 9C2[56]85-99 nmTPGS PCLSorafenib9C2 antibody conjugated nanoparticles in vitro: Have a higher cellular uptake and a 7.5-fold increase in IC50 value compared to free sorafenib; in vivo: Can greatly inhibit tumor growth with no significant side effects
Peptide G12[57]Approximately 100 nmLiposomeSorafenibG12-modified liposomes in vitro: Have enhanced specific-targeting and internalization into GPC3-positive cancer cells; in vivo: Show a superior precise antitumor effect with marked tumor suppression
Peptide[58]105-117 nmPEG PLGASorafenibPeptide-labeled nanoparticles in vitro: Significantly increase cytotoxicity against Hep3B cells; in vivo: Show good uptake and inhibited tumor growth
Table 2 List of different nanoformulations for Asialoglycoprotein Receptor targeted therapy in hepatocellular carcinoma
Targeting ligand
Particle size
Nanocarrier
Payload
In vitro or/and in vivo results
Lactose[64]Approximately 115 nmPCL-PEG-CHOSorafenib
Curcumin
Lactose modified nanoparticles in vitro: Improve the efficiency of loaded drugs and exhibit better cytotoxicity; in vivo: The inhibition rate is 77.4%
Galactose[65]92-136 nmPEG PCL; MicellesPaclitaxelIC50 values of Gal decorated nanoparticles decreased from 11.7 to 1.1 μg/mL with increasing Gal concentration from 10% to 30%, supporting receptor-mediated endocytosis mechanism
ASP[66]Approximately 228 nmDeoxycholic acidDoxorubicinASP modified nanoformulations in vitro: Internalize into HepG2 cells via ASGPR-mediated recognition and inhibit cell proliferation; in vivo: Suppress the tumor growth and reduce the side effects of free DOX
CS[62]Approximately 80 nmChitosanSimvastatinCS decorated nanoparticles enhance the cytotoxicity of the loading drug against HepG2 cells owing to its enhanced cellular uptake
LA[67]Approximately 310 nmCholesterol LiposomeOxaliplatinLA presents as a promising ligand for targeted drug delivery in the treatment of BEL7402 cancer cells
Pullulan[68]140-170 nmPLGA; PBAEPaclitaxel; Combretastatin A4Pullulan labeled nanoparticles enhance targeting capability and efficacy in HCC treatment both in vivo and in vitro
Pectin[69]Approximately 300 nmCa(OH)2; NaHCO35-FuPectin-based nanoparticles reduced the IC50 value to 0.17 mol/L in HepG2 cells, a significant decrease compared to the 0.45 mol/L IC50 value for free 5-Fu
Table 3 Summary of dual-targeted nanoformulations in hepatocellular carcinoma therapy
Ligand 1
Ligand 2
Nanocarrier
Payload
Particle size
Folic acid[100]Lactobionic acidChitosan5-Fu163 ± 10 nm
Folic acid[101]Lactobionic acidBerberine; DiosminCasein micellesApproximately 200 nm
Glycyrrhetinic acid[102]Hyaluronic acidCarbodiimide
Paclitaxe200-320 nm
Lactobionic acid[103]Glycyrrhetinic acidChitosan; Acrylic acidDOXApproximately 274 nm
Lactoferrin[104]Lactobionic acid/Glycyrrhetinic acidPhospholipid complexSorafenib; quercetin169 ± 1.5; 230 ± 1.7
Biotin[105]Lactobionic acidPEG; PLGACurcumin 5-Fu110-187 nm