期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 532, 期 2, 页码 677-685出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.03.007
关键词
Cancer imaging; Theranostic; Integrins; RGD; Nanoemulsion; NIR imaging
资金
- Ligue Nationale contre le Cancer [GB/MA/SC-12742]
- Fondation ARC pour la Recherche sur le Cancer [DOC20150602724]
- Campus France [796786A]
- French National Research Agency (ANR) as part of the Investissements d'Avenir program [ANR-10-NANO-01]
- Institut National de la Sante et de la Recherche Medicale [INSERM U1209]
- France Live Imaging program
Like several 50 nm-large nanocarriers, lipid nanoparticles (LNPs) can passively accumulate in tumors through the Enhanced Permeability and Retention (EPR) 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 alpha(v)beta(3). We demonstrate a specific targeting of the receptor with cRGD-LNPs but not with cRAD-LNP and standard LNP using HEK293(beta(3)), HEK293(beta(3))-alpha vRFP, DU145 and PC3 cell lines. We also demonstrate that cRGD-LNPs bind to alpha(v)beta 3, interfere with cell adhesion to vitronectin and co-internalize with avb3 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 EPR effect. (C) 2017 Elsevier B.V. All rights reserved.
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