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.
Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier / Monaco, Ilaria; Camorani, Simona; Colecchia, David; Locatelli, Erica; Calandro, Pierpaolo; Oudin, Anais; Niclou, Simone; Arra, Claudio; Chiariello, Mario; Cerchia, Laura; Comes Franchini, Mauro. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 60:10(2017), pp. 4510-4516. [10.1021/acs.jmedchem.7b00527]
Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier
MONACO, ILARIA;LOCATELLI, ERICA;COMES FRANCHINI, MAURO
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 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
