Journal article
Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
Department of Micro- and Nanotechnology, Technical University of Denmark1
Colloids and Biological Interfaces, Department of Micro- and Nanotechnology, Technical University of Denmark2
Department of Chemistry, Technical University of Denmark3
University of Copenhagen4
Hebrew University of Jerusalem5
Department of Electrical Engineering, Technical University of Denmark6
Background: Active, ligand-mediated, targeting of functionalized liposomes to folate receptors (FRs) overexpressed on cancer cells could potentially improve drug delivery and specificity. Studies on folate-targeting liposomes (FTLs) have, however, yielded varying results and generally fail to display a clear benefit of FR targeting.
Method: Tumor accumulating potential of FTLs and NTLs were investigated in a FR overexpressing xenograft model by positron emission tomography/computed tomography imaging. Results: Tumors displayed significantly lower activity of FTLs than NTLs. Furthermore, FTLs displayed worse circulating properties and increased liver-accumulation than NTLs. Conclusion: This study underlines that long-circulating properties of liposomes must be achieved to take advantage of EPR-dependent tumor accumulation which may be lost by functionalization.
FR-functionalization negatively affected both tumor accumulation and circulation properties.
| Language: | English |
|---|---|
| Publisher: | Dove Medical Press |
| Year: | 2018 |
| Pages: | 7647-7656 |
| ISSN: | 11782013 and 11769114 |
| Types: | Journal article |
| DOI: | 10.2147/IJN.S182579 |
| ORCIDs: | Christensen, Esben , Henriksen, Jonas R. , Andresen, Thomas Lars , Hansen, Anders Elias and 0000-0002-2706-5547 |
