학술논문

Aptamer Functionalization of Nanosystems for Glioblastoma Targeting through the Blood-Brain Barrier.
Document Type
Article
Source
Journal of Medicinal Chemistry. 5/25/2017, Vol. 60 Issue 10, p4510-4516. 7p.
Subject
*POLYMERS
*NANOPARTICLES
*TUMOR treatment
*TARGETED drug delivery
*GROWTH factors
*BLOOD-brain barrier
Language
ISSN
0022-2623
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. [ABSTRACT FROM AUTHOR]