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Amphiphilic Phospholipid-Based Riboflavin Derivatives for Tumor Targeting Nanomedicines

dc.contributor.authorBEZTSINNA, Nataliia
dc.contributor.authorTSVETKOVA, Yoanna
dc.contributor.authorBARTNECK, Matthias
dc.contributor.authorLAMMERS, Twan
dc.contributor.authorKIESSLING, Fabian
dc.contributor.authorBERQUE BESTEL, Isabelle
dc.date.accessioned2020-09-03T07:56:29Z
dc.date.available2020-09-03T07:56:29Z
dc.date.issued2016
dc.identifier.issn1043-1802
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/10908
dc.description.abstractEnRiboflavin (RF) is an essential vitamin for cellular metabolism. Recent studies have shown that RF is internalized through RF transporters, which are highly overexpressed by prostate and breast cancer cells, as well as by angiogenic endothelium. Here, we present an optimized synthesis protocol for preparing tailor-made amphiphilic phospholipid-based RF derivatives using phosphoramidite chemistry. The prepared RF amphiphile-RfdiC14-can be inserted into liposome formulations for targeted drug delivery. The obtained liposomes had a hydrodynamic size of 115 +/- 5 rim with narrow size distribution (PDI 0.06) and a zeta potential of -52 +/- 3 mV. In vitro uptake studies showed that RfdiC14-containing liposomes were strongly internalized in HUVEC, PC3, and A431 cells, in a specific and transporter-mediated manner. To assess the RF targeting potential in vivo, an amphiphile containing PEG spacer between RF and a lipid was prepared DSPE-PEG-RF. The latter was successfully incorporated into long-circulating near-infrared-labeled liposomes (141 +/- 1 nm in diameter, PDI 0.07, zeta potential of -33 +/- 1 mV). The longitudinal mu CT/FMT biodistribution studies in PC3 xenograft bearing mice demonstrated similar pharmacokinetics profile of DSPE-PEG-RF-functionalized liposomes compared to control. The subsequent histological evaluation of resected tumors revealed higher degree of tumor retention as well as colocalization of targeted liposomes with endothelial cells emphasizing the targeting potential of RF amphiphiles and their utility for the lipid-containing drug delivery systems.
dc.language.isoen
dc.title.enAmphiphilic Phospholipid-Based Riboflavin Derivatives for Tumor Targeting Nanomedicines
dc.typeArticle de revue
dc.identifier.doi10.1021/acs.bioconjchem.6b00317
dc.subject.halChimie/Matériaux
bordeaux.journalBioconjugate Chemistry
bordeaux.page2048-2061
bordeaux.volume27
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248*
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN, UMR 5248)
bordeaux.issue9
bordeaux.institutionUniversité de Bordeaux
bordeaux.institutionBordeaux INP
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioconjugate%20Chemistry&rft.date=2016&rft.volume=27&rft.issue=9&rft.spage=2048-2061&rft.epage=2048-2061&rft.eissn=1043-1802&rft.issn=1043-1802&rft.au=BEZTSINNA,%20Nataliia&TSVETKOVA,%20Yoanna&BARTNECK,%20Matthias&LAMMERS,%20Twan&KIESSLING,%20Fabian&rft.genre=article


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