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Riboflavin-Targeted Drug Delivery

Institute for Experimental Molecular Imaging, University Hospital Aachen, Forckenbeckstrasse 55, 52074 Aachen, Germany
Fraunhofer MEVIS, Institute for Medical Image Computing, Forckenbeckstrasse 55, 52074 Aachen, Germany
Author to whom correspondence should be addressed.
Cancers 2020, 12(2), 295;
Received: 13 November 2019 / Revised: 14 January 2020 / Accepted: 25 January 2020 / Published: 27 January 2020
(This article belongs to the Special Issue Cancer Nanomedicine)
Active targeting can improve the retention of drugs and drug delivery systems in tumors, thereby enhancing their therapeutic efficacy. In this context, vitamin receptors that are overexpressed in many cancers are promising targets. In the last decade, attention and research were mainly centered on vitamin B9 (folate) targeting; however, the focus is slowly shifting towards vitamin B2 (riboflavin). Interestingly, while the riboflavin carrier protein was discovered in the 1960s, the three riboflavin transporters (RFVT 1-3) were only identified recently. It has been shown that riboflavin transporters and the riboflavin carrier protein are overexpressed in many tumor types, tumor stem cells, and the tumor neovasculature. Furthermore, a clinical study has demonstrated that tumor cells exhibit increased riboflavin metabolism as compared to normal cells. Moreover, riboflavin and its derivatives have been conjugated to ultrasmall iron oxide nanoparticles, polyethylene glycol polymers, dendrimers, and liposomes. These conjugates have shown a high affinity towards tumors in preclinical studies. This review article summarizes knowledge on RFVT expression in healthy and pathological tissues, discusses riboflavin internalization pathways, and provides an overview of RF-targeted diagnostics and therapeutics. View Full-Text
Keywords: riboflavin; vitamin B2; targeted drug delivery; active targeting; theranostics; nanomedicines; molecular imaging; nanoparticle riboflavin; vitamin B2; targeted drug delivery; active targeting; theranostics; nanomedicines; molecular imaging; nanoparticle
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MDPI and ACS Style

Darguzyte, M.; Drude, N.; Lammers, T.; Kiessling, F. Riboflavin-Targeted Drug Delivery. Cancers 2020, 12, 295.

AMA Style

Darguzyte M, Drude N, Lammers T, Kiessling F. Riboflavin-Targeted Drug Delivery. Cancers. 2020; 12(2):295.

Chicago/Turabian Style

Darguzyte, Milita; Drude, Natascha; Lammers, Twan; Kiessling, Fabian. 2020. "Riboflavin-Targeted Drug Delivery" Cancers 12, no. 2: 295.

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