Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
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Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts. / Christensen, Esben; Henriksen, Jonas R.; Jorgensen, Jesper T.; Amitay, Yasmine; Shmeeda, Hilary; Gabizon, Alberto A.; Kjaer, Andreas; Andresen, Thomas L.; Hansen, Anders E.
I: International Journal of Nanomedicine, Bind 13, 2018, s. 7647-7656.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › fagfællebedømt
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TY - JOUR
T1 - Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
AU - Christensen, Esben
AU - Henriksen, Jonas R.
AU - Jorgensen, Jesper T.
AU - Amitay, Yasmine
AU - Shmeeda, Hilary
AU - Gabizon, Alberto A.
AU - Kjaer, Andreas
AU - Andresen, Thomas L.
AU - Hansen, Anders E.
PY - 2018
Y1 - 2018
N2 - 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.
AB - 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.
KW - liposomes
KW - folate
KW - cancer
KW - imaging
KW - PET
KW - EPR
U2 - 10.2147/IJN.S182579
DO - 10.2147/IJN.S182579
M3 - Journal article
C2 - 30538449
VL - 13
SP - 7647
EP - 7656
JO - International Journal of Nanomedicine
JF - International Journal of Nanomedicine
SN - 1176-9114
ER -
ID: 209682245