Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts

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Esben Christensen, Jonas R. Henriksen, Jesper T. Jorgensen, Yasmine Amitay, Hilary Shmeeda, Alberto A. Gabizon, Andreas Kjaer, Thomas L. Andresen, Anders E. Hansen

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.
Original languageEnglish
JournalInternational Journal of Nanomedicine
Volume13
Pages (from-to)7647-7656
ISSN1176-9114
DOIs
Publication statusPublished - 2018

    Research areas

  • liposomes, folate, cancer, imaging, PET, EPR

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