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Self-assembling supramolecular dendrimer nanosystem for PET imaging of tumors

Philippe Garrigue, Jingjie Tang, Ling Ding, Ahlem Bouhlel, Aura Tintaru, Erik Laurini, Yuanyu Huang, Zhenbin Lyu, Mengjie Zhang, Samantha Fernandez, Laure Balasse, Wenjun Lan, Eric Mas, Domenico Marson, Yuhua Weng, Xiaoxuan Liu, Suzanne Giorgio, Juan Iovanna, Sabrina Pricl, Benjamin Guillet, Ling Peng

Proc. Natl. Acad. Sci. U.S.A. 2018, doi : 10.1073/pnas.1812938115

Bioimaging plays an important role in cancer diagnosis and treatment. However, imaging sensitivity and specificity still constitute key challenges. Nanotechnology-based imaging is particularly promising for overcoming these limitations because nanosized imaging agents can specifically home in on tumors via the “Enhanced Permeation and Retention (EPR)” effect, thus resulting in enhanced imaging sensitivity and specificity. In this work, we report an original nanosystem for positron emission tomography (PET) imaging based on an amphiphilic dendrimer which bears multiple PET reporting units at the terminals. This dendrimer is able to self-assemble into small and uniform nanomicelles, which accumulate in tumors for effective PET imaging (Figure). Benefiting from the combined dendrimeric multivalence and EPR-mediated passive tumor targeting, this nanosystem demonstrates superior imaging sensitivity and specificity, with up to 14-fold increased PET signal ratios when compared to the clinical gold reference [18F]FDG (2-fluorodeoxyglucose). Most importantly, this dendrimer system can detect imaging-refractory low-glucose-uptake tumors which are otherwise undetectable using [18F]FDG. In addition, it is endowed with an excellent safety profile and favorable pharmacokinetics for PET imaging. Consequently, this dendrimer nanosystem constitutes an effective and promising approach for cancer imaging. Our study also demonstrates that nanotechnology based on self-assembling dendrimers provides a fresh perspective for bioimaging and related biomedical applications.

This is a collaborative work between Centre Interdisciplinaire de Nanoscience de Marseille (CINaM) and Centre Européen de Recherche en Imagerie Médicale (CERIMED) at Aix-Marseille University along with Centre de Recherche en Cancérologie de Marseille (CRCM), Institute de Chemie Radicale (ICR), Triest University in Italy and Beijing University of Technology in China.

Contact Dr. Ling Peng Aix-Marseille Université, CNRS, Centre Interdisciplinaire de Nanoscience de Marseille (CINaM) UMR 7325, Equipe Labellisé par La Ligue, Marseille, France
Email :

JPG - 49.9 ko

Schematic illustration of the supramolecular dendrimer nanosystem, based on a self-assembling amphiphilic dendrimer bearing radionuclide terminals, for positron emission tomography (PET) imaging of tumors

2018 PNAS Philippe - 1.4 Mo