Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood–Brain Barrier

Authors :: Mauro Comes Franchini
Simona Camorani
Mario Chiariello
David Colecchia
Anais Oudin
Ilaria Monaco
Pierpaolo Calandro
Laura Cerchia
Simone P. Niclou
Erica Locatelli
Claudio Arra
Monaco, Ilaria
Camorani, Simona
Colecchia, David
Locatelli, Erica
Calandro, Pierpaolo
Oudin, Anai
Niclou, Simone
Arra, Claudio
Chiariello, Mario
Cerchia, Laura
Comes Franchini, Mauro
Source :: Journal of medicinal chemistry (2017). doi:10.1021/acs.jmedchem.7b00527, info:cnr-pdr/source/autori:Monaco I1, Camorani S2, Colecchia D3, Locatelli E1, Calandro P3, Oudin A4, Niclou S4, Arra C5, Chiariello M3, Cerchia L2, Comes Franchini M1./titolo:Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier./doi:10.1021%2Facs.jmedchem.7b00527/rivista:Journal of medicinal chemistry/anno:2017/pagina_da:/pagina_a:/intervallo_pagine:/volume
Publication Year :: 2017
Publisher :: American Chemical Society (ACS), 2017.
Abstract: Polymeric nanoparticles (PNPs) may efficiently deliver in vivo therapeutics to tumors when conjugated to specific targeting agents. Gint4.T aptamer specifically recognizes platelet-derived growth factor receptor Î² and can cross the blood-brain barrier (BBB). We synthesized Gint4.T-conjugated PNPs able of high uptake into U87MG glioblastoma (GBM) cells and with astonishing EC50 value (38 pM) when loaded with a PI3K-mTOR inhibitor. We also demonstrated in vivo BBB passage and tumor accumulation in a GBM orthotopic model.

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