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. 2017 May 25;60(10):4510-4516.
doi: 10.1021/acs.jmedchem.7b00527. Epub 2017 May 10.

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

Ilaria Monaco  1 , Simona Camorani  2 , David Colecchia  3 , Erica Locatelli  1 , Pierpaolo Calandro  3 , Anais Oudin  4 , Simone Niclou  4 , Claudio Arra  5 , Mario Chiariello  3 , Laura Cerchia  2 , Mauro Comes Franchini  1
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Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier

Ilaria Monaco et al. J Med Chem. .

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 β 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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