Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier.
Ilaria MonacoSimona CamoraniDavid ColecchiaErica LocatelliPierpaolo CalandroAnais OudinSimone NiclouClaudio ArraMario ChiarielloLaura CerchiaMauro Comes FranchiniPublished in: Journal of medicinal chemistry (2017)
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.
Keyphrases
- growth factor
- cancer therapy
- drug delivery
- blood brain barrier
- gold nanoparticles
- induced apoptosis
- photodynamic therapy
- sensitive detection
- cell cycle arrest
- air pollution
- particulate matter
- cell proliferation
- magnetic nanoparticles
- small molecule
- label free
- endoplasmic reticulum stress
- heavy metals
- oxidative stress