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.

Monaco, I., Camorani, S., Colecchia, D., Locatelli, E., Calandro, P., Oudin, A., et al. (2017). Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier. JOURNAL OF MEDICINAL CHEMISTRY, 60(10), 4510-4516 [10.1021/acs.jmedchem.7b00527].

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

MONACO, ILARIA;LOCATELLI, ERICA;COMES FRANCHINI, MAURO
2017

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.
2017
Monaco, I., Camorani, S., Colecchia, D., Locatelli, E., Calandro, P., Oudin, A., et al. (2017). Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier. JOURNAL OF MEDICINAL CHEMISTRY, 60(10), 4510-4516 [10.1021/acs.jmedchem.7b00527].
Monaco, Ilaria; Camorani, Simona; Colecchia, David; Locatelli, Erica; Calandro, Pierpaolo; Oudin, Anais; Niclou, Simone; Arra, Claudio; Chiariello, Ma...espandi
File in questo prodotto:
Eventuali allegati, non sono esposti

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/607218
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? 45
  • Scopus 107
  • ???jsp.display-item.citation.isi??? 100
social impact