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

Esben Christensen,1–3 Jonas R Henriksen,2,4 Jesper T Jørgensen,3 Yasmine Amitay,5 Hilary Shmeeda,5 Alberto A Gabizon,5 Andreas Kjær,3 Thomas L Andresen,1,2 Anders E Hansen1–3 1Department of Micro- and Nanotechnology, DTU Nanotech, Technical University of Den...

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Autores principales:	Christensen E, Henriksen JR, Jørgensen JT, Amitay Y, Shmeeda H, Gabizon A, Kjær A, Andresen TL, Hansen AE
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	Liposomes Folate Cancer Imaging PET Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/2816f66ef9fe428ea118584e0c7bde5f
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spelling	oai:doaj.org-article:2816f66ef9fe428ea118584e0c7bde5f2021-12-02T05:07:38ZFolate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts1178-2013https://doaj.org/article/2816f66ef9fe428ea118584e0c7bde5f2018-11-01T00:00:00Zhttps://www.dovepress.com/folate-receptor-targeting-of-radiolabeled-liposomes-reduces-intratumor-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Esben Christensen,1–3 Jonas R Henriksen,2,4 Jesper T Jørgensen,3 Yasmine Amitay,5 Hilary Shmeeda,5 Alberto A Gabizon,5 Andreas Kjær,3 Thomas L Andresen,1,2 Anders E Hansen1–3 1Department of Micro- and Nanotechnology, DTU Nanotech, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 2Center for Nanomedicine and Theranostics, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 3Cluster for Molecular Imaging, Department of Biomedical Sciences and Department of Clinical Physiology, Nuclear Medicine & PET, University of Copenhagen and Rigshospitalet, DK-2200 & DK-2100, Copenhagen, Denmark; 4Department of Chemistry, DTU Chemistry, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 5Shaare Zedek Medical Center and Hebrew University – School of Medicine, Jerusalem, Israel 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. Keywords: liposomes, folate, cancer, imaging, PET, EPRChristensen EHenriksen JRJørgensen JTAmitay YShmeeda HGabizon AKjær AAndresen TLHansen AEDove Medical PressarticleLiposomesFolateCancerImagingPETMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 7647-7656 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Liposomes Folate Cancer Imaging PET Medicine (General) R5-920
spellingShingle	Liposomes Folate Cancer Imaging PET Medicine (General) R5-920 Christensen E Henriksen JR Jørgensen JT Amitay Y Shmeeda H Gabizon A Kjær A Andresen TL Hansen AE Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
description	Esben Christensen,1–3 Jonas R Henriksen,2,4 Jesper T Jørgensen,3 Yasmine Amitay,5 Hilary Shmeeda,5 Alberto A Gabizon,5 Andreas Kjær,3 Thomas L Andresen,1,2 Anders E Hansen1–3 1Department of Micro- and Nanotechnology, DTU Nanotech, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 2Center for Nanomedicine and Theranostics, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 3Cluster for Molecular Imaging, Department of Biomedical Sciences and Department of Clinical Physiology, Nuclear Medicine & PET, University of Copenhagen and Rigshospitalet, DK-2200 & DK-2100, Copenhagen, Denmark; 4Department of Chemistry, DTU Chemistry, Technical University of Denmark, DK-2800 Kongens Lyngby, Denmark; 5Shaare Zedek Medical Center and Hebrew University – School of Medicine, Jerusalem, Israel 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. Keywords: liposomes, folate, cancer, imaging, PET, EPR
format	article
author	Christensen E Henriksen JR Jørgensen JT Amitay Y Shmeeda H Gabizon A Kjær A Andresen TL Hansen AE
author_facet	Christensen E Henriksen JR Jørgensen JT Amitay Y Shmeeda H Gabizon A Kjær A Andresen TL Hansen AE
author_sort	Christensen E
title	Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
title_short	Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
title_full	Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
title_fullStr	Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
title_full_unstemmed	Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts
title_sort	folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human kb carcinoma xenografts
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/2816f66ef9fe428ea118584e0c7bde5f
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Folate receptor targeting of radiolabeled liposomes reduces intratumoral liposome accumulation in human KB carcinoma xenografts

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