Enhanced Anti-Glioma Efficacy by Borneol Combined With CGKRK-Modified Paclitaxel Self-Assembled Redox-Sensitive Nanoparticles

The serious therapeutic obstacles to glioma treatment include poor penetration across the blood-brain barrier (BBB) and low accumulation of therapeutic drugs at tumor sites. In this study, borneol combined with CGKRK peptide (a ligand of the heparan sulfate which overexpress on the glioma cells) mod...

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Main Authors: Lingyan Lv (Author), Xinrui Li (Author), Wei Qian (Author), Shennan Li (Author), Yan Jiang (Author), Yaokun Xiong (Author), Jianpei Xu (Author), Wei Lv (Author), Xiaoyan Liu (Author), Yun Chen (Author), Yulin Tang (Author), Hongliang Xin (Author)
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Published: Frontiers Media S.A., 2020-04-01T00:00:00Z.
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042 |a dc 
100 1 0 |a Lingyan Lv  |e author 
700 1 0 |a Lingyan Lv  |e author 
700 1 0 |a Xinrui Li  |e author 
700 1 0 |a Xinrui Li  |e author 
700 1 0 |a Wei Qian  |e author 
700 1 0 |a Shennan Li  |e author 
700 1 0 |a Yan Jiang  |e author 
700 1 0 |a Yaokun Xiong  |e author 
700 1 0 |a Jianpei Xu  |e author 
700 1 0 |a Wei Lv  |e author 
700 1 0 |a Xiaoyan Liu  |e author 
700 1 0 |a Yun Chen  |e author 
700 1 0 |a Yulin Tang  |e author 
700 1 0 |a Hongliang Xin  |e author 
245 0 0 |a Enhanced Anti-Glioma Efficacy by Borneol Combined With CGKRK-Modified Paclitaxel Self-Assembled Redox-Sensitive Nanoparticles 
260 |b Frontiers Media S.A.,   |c 2020-04-01T00:00:00Z. 
500 |a 1663-9812 
500 |a 10.3389/fphar.2020.00558 
520 |a The serious therapeutic obstacles to glioma treatment include poor penetration across the blood-brain barrier (BBB) and low accumulation of therapeutic drugs at tumor sites. In this study, borneol combined with CGKRK peptide (a ligand of the heparan sulfate which overexpress on the glioma cells) modified paclitaxel prodrug self-assembled redox-responsive nanoparticles (CGKRK-PSNPs) were hypothesized to enhance the BBB penetration ability and active tumor targeting efficiency, respectively. The resulting CGKRK-PSNPs possessed a spherical shape with a small particle size (105.61 ± 1.53 nm) and high drug loading for PTX (54.18 ± 1.13%). The drug release behavior proved that CGKRK-PSNPs were highly sensitive to glutathione (GSH) redox environment. The in vitro cell experiments suggested that CGKRK-PSNPs significantly increased the cellular uptake and cytotoxicity of U87MG cells, meanwhile CGKRK-PSNPs showed the low cytotoxicity against BCEC cells. Combined with borneol, CGKRK-PSNPs exhibited enhanced transportation across in vitro BBB model. In intracranial U87MG glioma-bearing nude mice, the higher accumulation of CGKRK-PSNPs combined with borneol was observed through real-time fluorescence image. Moreover, the in vivo anti-glioma results confirmed that CGKRK-PSNPs combined with borneol could improve the anti-glioma efficacy with the prolonged medium survival time (39 days). In conclusion, the collaborative strategy of CGKRK-PSNPs combined with borneol provided a promising drug delivery routine for glioblastoma therapy. 
546 |a EN 
690 |a borneol 
690 |a blood-brain barrier penetration 
690 |a paclitaxel 
690 |a redox-responsive nanoparticles 
690 |a CGKRK peptide 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Frontiers in Pharmacology, Vol 11 (2020) 
787 0 |n https://www.frontiersin.org/article/10.3389/fphar.2020.00558/full 
787 0 |n https://doaj.org/toc/1663-9812 
856 4 1 |u https://doaj.org/article/7fa9ad9d0ac34d2fb2cb3c67d902f343  |z Connect to this object online.