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

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.