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).
Type de document :
Article dans une revue
International Journal of Pharmaceutics, Elsevier, 2017, [Epub ahead of print]. 〈10.1016/j.ijpharm.2017.03.007〉
Liste complète des métadonnées

Littérature citée [14 références]  Voir  Masquer  Télécharger

http://www.hal.inserm.fr/inserm-01488572
Contributeur : Jean-Luc Coll <>
Soumis le : lundi 13 mars 2017 - 17:32:41
Dernière modification le : mercredi 14 février 2018 - 14:06:43
Document(s) archivé(s) le : mercredi 14 juin 2017 - 15:20:57

Fichier

Jungyoon Choi Int J Parm_Revis...
Fichiers produits par l'(les) auteur(s)

Identifiants

Collections

CEA | DRT | LETI

Citation

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〉

Partager

Métriques

Consultations de la notice

134

Téléchargements de fichiers

49