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

Ilaria Monaco, Simona Camorani, David Colecchia, Erica Locatelli, Pierpaolo Calandro, Anais Oudin, Simone P. Niclou, Claudio Arra, Mario Chiariello, Laura Cerchia, Mauro Comes Franchini

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)4510-4516
Number of pages7
JournalJournal of Medicinal Chemistry
Volume60
Issue number10
DOIs
Publication statusPublished - May 25 2017

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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