Stapled RGD Peptide Enables Glioma-Targeted Drug Delivery by Overcoming Multiple Barriers

ACS Applied Materials & Interfaces
Huitong RuanWeiyue Lu

Abstract

Malignant glioma, the most frequent and aggressive central nervous system (CNS) tumor, severely threatens human health. One reason for its poor prognosis and short survival is the presence of the blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB), which restrict the penetration of therapeutics into the brain at different stages of glioma. Herein, inspired by the peptide stapling technique, we designed a cyclic RGD ligand via an all-hydrocarbon staple (stapled RGD, sRGD) to facilitate BBB penetration while retaining the capacity of BBTB penetration and targeting ability to glioma cells. As expected, sRGD-modified micelles were able to penetrate the in vitro BBB model while retaining the glioma targeted capability. The results of the in vivo imaging studies further revealed that this nanocarrier could not only efficiently transverse the intact BBB of normal mice, but also could specifically target glioma cells of intracranial glioma-bearing nude mice. Furthermore, Paclitaxel-loaded sRGD-modified micelles exhibited improved antiglioma efficacy in vitro and significantly prolonged survival time of glioma-bearing nude mice. Overall, this sRGD peptide showed potency for glioma-targeted drug delivery by overcoming multiple...Continue Reading

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Citations

Jul 8, 2017·ACS Applied Materials & Interfaces·Jiani MaoWeiyue Lu
Jan 19, 2019·Biomaterials Science·Zhuxuan JiangChangyou Zhan
May 10, 2019·Artificial Cells, Nanomedicine, and Biotechnology·Guangping YuShengsong Tang
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Feb 23, 2021·Asian Journal of Pharmaceutical Sciences·Huan WangChangyou Zhan
Apr 30, 2021·International Journal of Pharmaceutics·Solmaz Mojarad-JabaliHadi Valizadeh
Jun 8, 2021·RSC Medicinal Chemistry·Ruchika GoyalVibin Ramakrishnan
Sep 20, 2017·ACS Applied Materials & Interfaces·Tao SunChen Jiang
May 24, 2018·ACS Applied Materials & Interfaces·Man YingWeiyue Lu
Aug 17, 2019·ACS Chemical Neuroscience·Kowthavarapu Venkata KrishnaSunil Kumar Dubey

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