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Mustard-inspired delivery shuttle for enhanced blood–brain barrier penetration and effective drug delivery in glioma therapy

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Abstract

Effective penetration through the blood–brain barrier (BBB) remains a challenge for the treatment of many brain diseases. In this study, a small molecule, sinapic acid (SA), extracted from mustard, was selected as a novel bioinspired BBB-permeable ligand for efficient drug delivery in glioma treatment. SA was conjugated on the surface of zwitterionic polymer poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC)-encapsulated bovine serum albumin (BSA)-based nanoparticles, yielding nBSA-SA. The PMPC shell serves as a protective layer to prolong the in vivo blood circulation time with a better chance to cross the BBB. Furthermore, temozolomide (TMZ), which can be loaded onto the nanoparticles via electrostatic interactions with acrylic acid (AA) to generate AA-nBSA-SA-TMZ, was applied as an excellent chemotherapeutic drug for glioma therapy. The obtained nanoparticles with a distinct size show great BBB permeability. Through the mechanism study, it was found that the cell internalization of the SA-conjugated nanoparticles is an energy-dependent process with only transient disruption of the BBB. The biological evaluation results unambiguously suggest that drug-loaded nanoparticles can lead to strong apoptosis on the tumor site and increase the median survival time of glioma-bearing mice. Overall, this novel BBB-permeable ligand SA paves the way for the delivery of cargo into the brain and provides a powerful nanoplatform for glioma therapy via intravenous administration.

Graphical abstract: Mustard-inspired delivery shuttle for enhanced blood–brain barrier penetration and effective drug delivery in glioma therapy

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Publication details

The article was received on 17 Feb 2017, accepted on 19 Mar 2017 and first published on 22 Mar 2017


Article type: Paper
DOI: 10.1039/C7BM00133A
Citation: Biomater. Sci., 2017, Advance Article
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    Mustard-inspired delivery shuttle for enhanced blood–brain barrier penetration and effective drug delivery in glioma therapy

    N. Wang, P. Sun, M. Lv, G. Tong, X. Jin and X. Zhu, Biomater. Sci., 2017, Advance Article , DOI: 10.1039/C7BM00133A

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