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 P. Niclou, Claudio Arra, Mario Chiariello, Laura Cerchia, Mauro Comes Franchini

Research output: Contribution to journalArticle

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 - May 25 2017

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Glioblastoma
Blood-Brain Barrier
Nanoparticles
Platelet-Derived Growth Factor Receptors
Phosphatidylinositol 3-Kinases
Neoplasms
Therapeutics

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Monaco, I., Camorani, S., Colecchia, D., Locatelli, E., Calandro, P., Oudin, A., ... Comes Franchini, M. (2017). Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier. Journal of Medicinal Chemistry, 60(10), 4510-4516. https://doi.org/10.1021/acs.jmedchem.7b00527

Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier. / Monaco, Ilaria; Camorani, Simona; Colecchia, David; Locatelli, Erica; Calandro, Pierpaolo; Oudin, Anais; Niclou, Simone P.; Arra, Claudio; Chiariello, Mario; Cerchia, Laura; Comes Franchini, Mauro.

In: Journal of Medicinal Chemistry, Vol. 60, No. 10, 25.05.2017, p. 4510-4516.

Research output: Contribution to journalArticle

Monaco, I, Camorani, S, Colecchia, D, Locatelli, E, Calandro, P, Oudin, A, Niclou, SP, Arra, C, Chiariello, M, Cerchia, L & Comes Franchini, M 2017, 'Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier', Journal of Medicinal Chemistry, vol. 60, no. 10, pp. 4510-4516. https://doi.org/10.1021/acs.jmedchem.7b00527
Monaco, Ilaria ; Camorani, Simona ; Colecchia, David ; Locatelli, Erica ; Calandro, Pierpaolo ; Oudin, Anais ; Niclou, Simone P. ; Arra, Claudio ; Chiariello, Mario ; Cerchia, Laura ; Comes Franchini, Mauro. / Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier. In: Journal of Medicinal Chemistry. 2017 ; Vol. 60, No. 10. pp. 4510-4516.
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