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Targeting tumors with cyclic RGD-conjugated lipid nanoparticles loaded with an IR780 NIR

Abstract : Like several 50 nm-large nanocarriers, lipid nanoparticles (LNPs) can passively accumulate in tumors through the Enhanced Permeability and Retention effect. In this study, we developed PEGylated LNPs loaded with IR780 iodide as a contrast agent for NIR fluorescence imaging and modified them with cyclic RGD peptides in order to target integrin αvβ3. We demonstrate a specific targeting of the receptor with cRGD-LNPs but not with cRAD-LNP and standard LNP using HEK293(β3), HEK293(β3)-αvRFP, DU145 and PC3 cell lines. We also demonstrate that cRGD-LNPs bind to αvβ3, interfere with cell adhesion to vitronectin and co-internalize with αvβ3 within one hour. We then investigated their biodistribution and tumor targeting in mice bearing DU145 or M21 tumors. We observed no significant differences between cRGD-LNP and the non-targeted ones regarding their biodistribution and accumulation/retention in tumors. This suggested that despite an efficient formulation of the cRGD-LNPs, the cRGD-mediated targeting was not increasing the total amount of LNP that can already accumulate passively in the subcutaneous tumors via the Enhanced Permeability and Retention effect (EPR).
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Submitted on : Monday, March 13, 2017 - 5:32:41 PM
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Jungyoon Choi, Emilie Rustique, Maxime Henry, Mélanie Guidetti, Véronique Josserand, et al.. Targeting tumors with cyclic RGD-conjugated lipid nanoparticles loaded with an IR780 NIR. International Journal of Pharmaceutics, Elsevier, 2017, [Epub ahead of print]. ⟨10.1016/j.ijpharm.2017.03.007⟩. ⟨inserm-01488572⟩



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