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双配体修饰聚合物泡囊的制备及细胞摄取
引用本文:解方园,俞媛,耿雯倩,钟延强. 双配体修饰聚合物泡囊的制备及细胞摄取[J]. 药学实践杂志, 2015, 33(1): 44-48
作者姓名:解方园  俞媛  耿雯倩  钟延强
作者单位:第二军医大学药学院药剂学教研室, 上海 200433,第二军医大学药学院药剂学教研室, 上海 200433,第二军医大学药学院药剂学教研室, 上海 200433,第二军医大学药学院药剂学教研室, 上海 200433
基金项目:国家自然科学基金(81302714);上海市科委纳米专项(11nm0504400)
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80nm,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。

关 键 词:脑靶向  聚合物泡囊  血脑屏障
收稿时间:2014-10-11
修稿时间:2014-11-25

The preparation and the cell uptake of polymer vesicles modified with dual ligands
XIE Fangyuan,YU Yuan,GENG Wenqian and ZHONG Yanqiang. The preparation and the cell uptake of polymer vesicles modified with dual ligands[J]. The Journal of Pharmaceutical Practice, 2015, 33(1): 44-48
Authors:XIE Fangyuan  YU Yuan  GENG Wenqian  ZHONG Yanqiang
Affiliation:Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China and Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
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.
Keywords:brain targeting  polymer vesicles  blood-brain barrier(BBB)
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