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. 2020 Jul 10;18(3):1559325820936161. doi: 10.1177/1559325820936161

Table 3.

Specific Cell Surface Moieties Targeted by Nanoparticles for Use in Cancer Therapy.

Specific cell surface moieties Targeting ligands Cancer types Comments Ref
Folate receptor (FR) Folate Human squamous cell oral carcinoma (KB) In vivo, F-PEG-liposomal UA exhibited greater AUC and half-life than free UA by 6-fold and 9.8-fold, respectively. F-PEG-liposomal UA reduced tumor volume by 55% compared with the control. Animal life span was 56, 47, and 42 days for F-PEG-liposomal UA, PEG-liposomal UA, or free UA, respectively. 94
Folate receptor (FR) Folate Mouse breast cancer cell line (4T1.2) human breast cancer cell line (MCF-7) and drug-resistant cancer cell line (NCI/ADR-RES) Compared with free DOX and Doxil, FA-coupled DOX-loaded nanomicelle carriers show significantly enhanced tumor suppression with minimal toxicity. Compared with free DOX, the maximum tolerated dose is increased by about 1.5 times 95
Folate receptor (FR) Folate Mouse lymphoma expressing FR (J6456-FR) In vivo, the DOX level in J6456-FR tumors was 17-fold higher for F-liposomes compared with PEGliposomes. The DOX level was also lower in ascitic fluid (2.25-fold) and plasma fluid (14-fold) when DOX was delivered by F-liposomes compared to PEGliposomes. 96
Folate receptor (FR) Folate Human cervical cancer (HeLa); human lung cancer (A549) In vitro, FA-albumin NPs have higher cytotoxicity and cell uptake activity than free PTX and non-targeted PTX albumin NPs; in vivo, FA-albumin NPs can accumulate at the tumor site and have the most Good treatment effect. 97
Transferrin receptor (TfR) Holo-transferrin Hepatocellular carcinoma (HepG2) In vitro, compared with PEG-liposomes, free DOX, Tf-liposomes have higher cytotoxicity;
In vivo, Tf-liposomes have the best therapeutic effect. The tumor AUC after 96 hours was Tf-liposome> PEG-liposome> free DOX.
98
Transferrin receptor (TfR) Holo-transferrin Human gastric cancer (MKN45P) In vivo, the levels of cisplatin in tumor cells increased significantly when treated with Tf-PEG-liposomes compared to non-targeted liposomes, and free cisplatin. The treatment of mice bearing tumor xenografts with TfR-targeted formulation significantly prolonged the survival time of these animals compared to non-targeted liposomes, and free cisplatin. 99
CD44 receptor Hyaluronic acid (HA) Murine mammary (4T1) and human breast cancer (T47D) In vitro, HA-liposomes have higher cytotoxicity than free PTX and non-targeted PTX liposomes
In vivo, HA-liposomes can accumulate at the tumor site and have the best therapeutic effect.
100
CD44 receptor Hyaluronic acid (HA) Mouse colon carcinoma (C-26), human adenocarcinoma (PANC-1) In vivo, the order of DOX tumor accumulation was HA-liposomes > Doxil > non-targeted liposomes > free DOX. The order was reversed in tumor-free organs. A significant decrease in tumor growth and a marked increase in animal life span were observed across different tumor-types when treated with HA-liposomal DOX compared with the other 3 treatments. 101
EGFR Anti-EGFR antibody Human breast cancer (MDA-MB- 468), human glioblastoma (U87) In vivo, anti-EGFR-liposomes were internalized more efficiently than non-targeted liposomes (92 vs 5%). Anti-EGFR-liposomes were able to improve the anticancer efficacy of various drugs in mice bearing tumors compared with non-targeted liposomes and free drugs. 102
HER2 Anti-HER-2 Human breast cancer (MCF-7) In animal models, the cure rate of anti-HER2 immunoliposome-dox reached 50%, and anti-HER2 immunoliposome-dox was also superior to combinations consisting of free MAb plus free dox or free MAb plus liposomal dox. 103
HER2 Anti-HER-2 Human breast cancer (SKBR3) In vitro, the cytotoxicity of PTX/RAP to immunoliposomes increased, which may be due to increased uptake mediated by HER2 binding; immunoliposomes were better able to control tumor growth in vivo, with tumor volume averages corresponding to 25.27%, 44.38%, and 47.78% of tumor volumes of untreated control, PTX/RAP solution, and control liposomes, respectively. 104