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首页> 外文期刊>Vascular pharmacology >Binding and uptake of transferrin-bound liposomes targeted to transferrin receptors of endothelial cells.
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Binding and uptake of transferrin-bound liposomes targeted to transferrin receptors of endothelial cells.

机译：靶向内皮细胞转铁蛋白受体的与转铁蛋白结合的脂质体的结合和摄取。

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摘要

The use of liposomes as carriers for site-specific delivery is an attractive strategy, especially for the vascular endothelium that by position is an accessible target for drug and gene delivery via the blood circulation. The aim of this study was to detect whether liposomes coupled to transferrin (Tf)-bound and are taken up by aortic endothelial cells (EC) following the pathway of Tf interaction with transferrin receptors, reportedly expressed on their cell membrane. To this purpose, small unilamellar liposomes of different compositions, either classical (C) or sterically stabilized (SS), have been prepared, characterized and coupled with transferrin (Tf-liposomes). To assess the binding and uptake, cultured EC were incubated with fluorescently labelled Tf-liposomes for various times intervals (from 5 min to 24 h) at 4 and 37 degrees C, and further investigated by flow cytometry, fluorimetry and fluorescence microscopy. The results showed that: (i) binding of Tf-liposomes to EC was specific; (ii) the EC binding of SS-Tf-liposomes was lower than that of C-Tf-liposomes; and (iii) after 30 min of incubation, both C- and SS-Tf-liposomes appeared localized in the acidic compartments of the cells. Together, the data indicate that transferrin-bound liposomes are specifically taken up by EC by a receptor-mediated mechanism employing the pathway of surface-exposed Tf receptors.
机译：使用脂质体作为用于位点特异性递送的载体是一种有吸引力的策略，特别是对于血管内皮，该血管内皮通过位置是通过血液循环进行药物和基因递送的可及目标。这项研究的目的是检测脂质体是否与转铁蛋白（Tf）结合并且是否通过Tf与转铁蛋白受体相互作用的途径被主动脉内皮细胞（EC）吸收，据报道它们在细胞膜上表达。为了这个目的，已经制备了不同组成的小的单层脂质体，经典的（C）或空间稳定的（SS），特征化并与转铁蛋白（Tf-脂质体）偶联。为了评估结合和摄取，将培养的EC与荧光标记的Tf-脂质体在4和37℃下不同时间间隔（5分钟至24小时）温育，并进一步通过流式细胞术，荧光法和荧光显微镜检查。结果表明：（i）Tf-脂质体与EC的结合是特异性的; （ii）SS-Tf-脂质体的EC结合低于C-Tf-脂质体的EC结合; （iii）孵育30分钟后，C-Tf-脂质体和SS-Tf-脂质体均位于细胞的酸性区室中。总之，数据表明运铁蛋白结合的脂质体是由EC通过采用表面暴露的Tf受体途径的受体介导的机制特异性吸收的。

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