Table 3.
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 |