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. 2021 Dec 25;14(1):41. doi: 10.3390/pharmaceutics14010041

Table 1.

Different nanoformulations showing ASGPR targeting in HCC.

Targeting Moiety Nanocarrier Cargo Carried by Nanocarrier In Vitro and/or In Vivo Studies and Results
Pullulan (Pul), Arabinogalactan (AGn), and Pul-AGn [45] Polyethylene sebacate (PES) nanoparticles Doxorubicin ASGPR-mediated uptake in HepG2 cells, biodistribution and hepatic disposition in vivo and antitumor activity and toxicity testing in vivo showed that Pul and Pul-AGn labeling increased liver uptake with hepatocyte: nonparenchymal cell ratio of 85:15
Lactose [211] Shell cross-linking nanoparticles Doxorubicin In vitro cytotoxicity and cellular uptake in HepG2 cells showed that lactose conjugated NPs were internalized through a lactose-mediated mechanism
Galactose [212] Cyclodextrins Not applicable In vitro and in vivo adherence of hepatocytes to formulation proved that the enzymatically synthesized NPs were specific to hepatocytes
Galactose [213] Cross-linked pH-sensitive micelles Paclitaxel In vitro hepatoma targeting in HepG2 cells and in vivo biodistribution and antitumor studies showed that galactose conjugated NPs underwent receptor-mediated endocytosis mechanism in vitro with enhanced drug accumulation at the tumor sites in vivo
Galactosamine [214] Albumin nanoparticles Doxorubicin In vitro cytotoxicity and cellular uptake in HepG2 concluded that the NPs were selectively taken up by HepG2 cells due to the surface ASGPR as opposed to ASGPR-negative cells
Lactoferrin [215] PEGylated liposomes Not applicable In vitro cellular uptake in HepG2 lines and in vivo imaging for targeting in HepG2 bearing mice showed that cell uptake was efficiently associated with ASGPR-positive HepG2 cells compared to negative control along with increased drug accumulation in tumors treated with conjugated NPs