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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Monaco I,Camorani S,Colecchia D,Locatelli E,Calandro P,Oudin A,Niclou S,Arra C,Chiariello M,Cerchia L,Comes Franchini M

doi

10.1021/acs.jmedchem.7b00527

subject

Has Abstract

pub_date

2017-05-25 00:00:00

pages

4510-4516

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

60

pub_type

杂志文章

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