Controlled Chemical Derivatisation of Carbon Nanotubes with Imaging, Targeting, and Therapeutic Capabilities.
In drug delivery, carbon nanotubes (CNTs) hold a great potential as carriers because of their ability to easily cross biological barriers and be internalised into cells. Their high aspect ratio allows multi-functionalisation and their development as a multimodal platform for targeted therapy. In this article, we report the controlled covalent derivatisation of triple-functionalised CNTs with the anticancer drug gemcitabine, folic acid as a targeting ligand and fluorescein as a probe. The anticancer activity of gemcitabine was maintained after covalent grafting onto the CNTs. The functionalised nanotubes were internalised into both folate-positive and negative cells, suggesting the passive diffusion of CNTs. Overall, our approach is versatile and offers a precise chemical control of the sidewall functionalisation of CNTs and the possibility to manoeuvre the types of functionalities required on the nanotubes for a multimodal therapeutic strategy.
CNRS, Institut de Biologie Moléculaire et Cellulaire, Laboratoire d'Immunopathologie et Chimie Thérapeutique, UPR 3572, 67000 Strasbourg (France). c.menard@ibmc-cnrs.unistra.fr.
Cécilia
C
Ménard-Moyon
Pharmacy and Therapeutics, School of Clinical and Experimental Medicine, Medical School, University of Birmingham, Birmingham, B15 2TT (UK).
Hanene
H
Ali-Boucetta
Dipartimento di Scienze Molecolari e Nanosistemi, Università Ca' Foscari di Venezia, Venezia, 30123 (Italy).
Chiara
C
Fabbro
CNRS, Institut de Biologie Moléculaire et Cellulaire, Laboratoire d'Immunopathologie et Chimie Thérapeutique, UPR 3572, 67000 Strasbourg (France).
Olivier
O
Chaloin
Nanomedicine Laboratory, Institute of Inflammation and Repair, Faculty of Medical and Human Sciences, AV Hill Building, The University of Manchester, Manchester, M13 9PT (UK).
Kostas
K
Kostarelos
CNRS, Institut de Biologie Moléculaire et Cellulaire, Laboratoire d'Immunopathologie et Chimie Thérapeutique, UPR 3572, 67000 Strasbourg (France). a.bianco@ibmc-cnrs.unistra.fr.
Alberto
A
Bianco
cancer; carbon nanotubes; drug delivery; fluorescent probes; functionalization