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

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

Journal of medicinal chemistry (2017-05-05)
Ilaria Monaco, Simona Camorani, David Colecchia, Erica Locatelli, Pierpaolo Calandro, Anais Oudin, Simone Niclou, Claudio Arra, Mario Chiariello, Laura Cerchia, Mauro Comes Franchini
摘要

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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Sigma-Aldrich
Thiol poly(ethylene glycol)-block-poly(lactide-co-glycolide), PEG average Mn 5,000, PLGA average Mn 15,000, lactide:glycolide 50:50
Sigma-Aldrich
Maleimide poly(ethylene glycol)-block-poly(lactide-co-glycolide), PEG average Mn 5,000, PLGA average Mn 15,000, lactide:glycolide 50:50
Sigma-Aldrich
N-Hydroxysuccinimide poly(ethylene glycol)-block-poly(lactide-co-glycolide), PEG average Mn 5000, PLGA average Mn 15000, lactide:glycolide 50:50