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 Niclou
  • , Claudio Arra
  • , Mario Chiariello*
  • , Laura Cerchia
  • , Mauro Comes Franchini
  • *Corresponding author for this work

Research output: Contribution to journalArticleResearchpeer-review

126 Citations (Scopus)

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 - 25 May 2017

Fingerprint

Dive into the research topics of 'Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier'. Together they form a unique fingerprint.

Cite this