双配体修饰聚合物泡囊的制备及细胞摄取

The preparation and the cell uptake of polymer vesicles modified with dual ligands

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。

Objective To construct an active targeting drug delivery systempolymer vesicles（PVs）, and examined the cellular uptake. Methods Maleimide polyethylene glycolpoly（lacticcoglycolic acid）（MALPEGPLGA）was used as carrier materials to prepare PVs by selfassembling. And then PVs was modified by Tf and Tet1（Tf/Tet1PVs）. To evaluate its active targeting, coumarin6 was used as a fluorescent probe to analyze cellular uptake of PVs for both BCEC and Neuro2a cells. Results PVs was about 80 nm with rounded shape and had obvious film structure. Tf/Tet1PVs exhibited a significant role in promoting cellular uptake for both BCEC and Neuro2a cells compared with control and single ligandmodified group. Conclusion PVs modified with dual ligands could promote the cell uptake for both brain capillary cells and nerve cells.