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 Shmeeda, Alberto A Gabizon, Andreas Kjær, Thomas L Andresen, Anders E Hansen

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 overex-pressing 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.

OriginalsprogEngelsk
TidsskriftInternational Journal of Nanomedicine
Vol/bind13
Sider (fra-til)7647-7656
Antal sider10
ISSN1176-9114
DOI
StatusUdgivet - 2018

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