Aptamer functionalization of nanosystems for glioblastoma targeting through the blood-brain barrier.

  • NORLUX Neuro-Oncology Laboratory
May 25, 2017 By:
  • Monaco I
  • Camorani S
  • Colecchia D
  • Locatelli E
  • Calandro P
  • Oudin A
  • Niclou S
  • Arra C
  • Chiariello M
  • Cerchia L
  • Comes Franchini M.

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 beta 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.

2017 May. J Med Chem.60(10):4510-4516. Epub 2017 May 10.
Other information