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

Esben Christensen, Jonas R. Henriksen, Jesper T. Jørgensen, Yasmine Amitay, Hilary Schmeeda, Alberto A. Gabizon, Andreas Kjær, Thomas Lars Andresen, Anders Elias Hansen*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

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

Keywords

  • Liposomes
  • Folate
  • Cancer
  • Imaging
  • PET
  • EPR

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