The preparation and the cell uptake of polymer vesicles modified with dual ligands
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摘要: 目的 构建一种主动靶向的新型纳米药物载体——聚合物泡囊(polymer vesicles,PVs),并考察其细胞摄取。 方法 以马来酰亚胺-聚乙二醇-聚乳酸-羟基乙酸共聚物(MAL-PEG-PLGA)为载体材料,通过自组装制备PVs,用转铁蛋白(Tf)与Tet-1对PVs进行修饰,构建纳米药物载体(Tf/Tet-1-PVs)。以香豆素-6作为荧光探针包载于药物载体,考察脑微血管内皮细胞(BCEC)及神经细胞(Neuro-2a)对载体系统的摄取。 结果 PVs粒径约80 nm,形态圆整,电镜观察具有明显膜层结构。BCEC细胞和Neuro-2a细胞对Tf/Tet-1-PVs的摄取均显著优于空白对照组和单配体修饰对照组。 结论 PVs经双配体Tf及Tet-1修饰后可促进脑微血管内皮细胞和神经细胞的摄取。Abstract: Objective To construct an active targeting drug delivery system- polymer vesicles(PVs),and examined the cellular uptake. Methods Maleimide-polyethylene glycol-poly(lactic-co-glycolic acid)(MAL-PEG-PLGA)was used as carrier materials to prepare PVs by self-assembling.And then PVs was modified by Tf and Tet-1(Tf/Tet-1-PVs).To evaluate its active targeting,coumarin-6 was used as a fluorescent probe to analyze cellular uptake of PVs for both BCEC and Neuro-2a cells. Results PVs was about 80 nm with rounded shape and had obvious film structure.Tf/Tet-1-PVs exhibited a significant role in promoting cellular uptake for both BCEC and Neuro-2a cells compared with control and single ligand-modified group. Conclusion PVs modified with dual ligands could promote the cell uptake for both brain capillary cells and nerve cells.
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Key words:
- brain targeting /
- polymer vesicles /
- blood-brain barrier(BBB)
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[1] 吴 珍,杜士明,董永成.纳米粒作为脑靶向给药系统的研究进展[J].中国药房,2007,18(13):1029-1031. [2] Pardridge WM.Blood-brain barrier drug targeting:the future of brain drug development[J].Mol Interv,2003,3(2):90-105. [3] Overmoyer B,Silverman P,Holder LW,et al.Pegylated liposomal doxorubicin and cyclophosphamide as first-line therapy for patients with metastatic or recurrent breast cancer[J].Clin Breast Cancer,2005,6(2):150-157. [4] Vorobiof DA, Rapoport BL,Chasen MR,et al.First line therapy with paclitaxel (Taxol) and pegylated liposomal doxorubicin (Caelyx) in patients with metastatic breast cancer:a multicentre phase II study[J].Breast,2004,13(3):219-226. [5] Boulikas T.Clinical overview on lipoplatin:a successful liposomal formulation of cisplatin[J].Expert Opin Investig Drugs,2009,18(8):1197-1218. [6] Gentile E,Cilurzo F,Marzio LD,et al.Liposomal chemotherapeutics[J].Future Oncol,2013,9(12):1849-1859. [7] 陆 彬. 新型给药系统聚合物泡囊及其研究进展(上)[J].中国药师,2009,12(4):439-442,446. [8] Cheng JJ,Teply BA,Sherifi I,et al.Formulation of functionalized PLGA-PEG nanoparticles for in vivo targeted drug delivery[J].Biomaterials,2007,28(5):869-876. [9] Zhang PC,Hu LJ,Yin Q,et al.Transferrin-modified c[RGDfK]-paclitaxel loaded hybrid micelle for sequential blood-brain barrier penetration and glioma targeting therapy[J].Mol Pharm,2012,9(6):1590-1598. [10] Kwon EJ,Lasiene J,Jacobson BE,et al.Targeted nonviral delivery vehicles to neural progenitor cells in the mouse subventricularzone[J].Biomaterials,2010,31(8):2417-2424. -
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