目的制备由^(D)A7R肽修饰的红细胞膜包裹的PLGA纳米粒,并进行体外评价。方法合成DSPE-PEG 2000-^(D)A7R,制备PLGA纳米粒,制备由^(D)A7R肽修饰的红细胞膜包裹纳米粒(^(D)A7R-NP),用透射电子显微镜(transmission electron microscope,TEM...目的制备由^(D)A7R肽修饰的红细胞膜包裹的PLGA纳米粒,并进行体外评价。方法合成DSPE-PEG 2000-^(D)A7R,制备PLGA纳米粒,制备由^(D)A7R肽修饰的红细胞膜包裹纳米粒(^(D)A7R-NP),用透射电子显微镜(transmission electron microscope,TEM)、粒径分析仪等进行表征。结果制备的^(D)A7R-NP平均粒径为(102.8±11.7)nm,包封率为79.14%±2.57%,体外4~8℃可稳定保存30 d,模拟血浆中48 h稳定。细胞实验表明^(D)A7R-NP跨越血脑屏障(blood-brain barrier,BBB)的能力显著提高。结论制备的由^(D)A7R肽修饰的红细胞膜包裹的PLGA纳米粒理化特性良好,且具有良好的脑靶向潜力。展开更多
Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VE...Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VEGFR-2 and NRP-1 may be a potential antiangiogenic and antitumor strategy.A7R,a peptide with sequence of Ala-Thr-Trp-Leu-Pro-Pro-Arg that was found by phage display of peptide libraries,can preferentially target VEGFR-2 and NRP-1 and destroy the binding between vascular endothelial growth factor 165(VEGF165)and VEGFR-2 or NRP-1.This peptide is a new potent inhibitor of tumor angiogenesis and a targeting ligand for cancer therapy.This review describes the discovery,function and mechanism of the action of A7R,and further introduces the applications of A7R in antitumor angiogenic treatments,tumor angiogenesis imaging and targeted drug delivery systems.In this review,strategies to deliver different drugs by A7R-modified liposomes and nanoparticles are highlighted.A7R,a new dual targeting ligand of VEGFR-2 and NRP-1,is expected to have efficient therapeutic or targeting roles in tumor drug delivery.展开更多
基金funded by National Natural Science Foundation of China(No.81302686)Primary Research&Developement Plan of Shandong Province(No.2016GSF201083)
文摘Vascular endothelial growth factor receptor 2(VEGFR-2)and neuropilin-1(NRP-1)are two prominent antiangiogenic targets.They are highly expressed on vascular endothelial cells and some tumor cells.Therefore,targeting VEGFR-2 and NRP-1 may be a potential antiangiogenic and antitumor strategy.A7R,a peptide with sequence of Ala-Thr-Trp-Leu-Pro-Pro-Arg that was found by phage display of peptide libraries,can preferentially target VEGFR-2 and NRP-1 and destroy the binding between vascular endothelial growth factor 165(VEGF165)and VEGFR-2 or NRP-1.This peptide is a new potent inhibitor of tumor angiogenesis and a targeting ligand for cancer therapy.This review describes the discovery,function and mechanism of the action of A7R,and further introduces the applications of A7R in antitumor angiogenic treatments,tumor angiogenesis imaging and targeted drug delivery systems.In this review,strategies to deliver different drugs by A7R-modified liposomes and nanoparticles are highlighted.A7R,a new dual targeting ligand of VEGFR-2 and NRP-1,is expected to have efficient therapeutic or targeting roles in tumor drug delivery.
