Influence of Physicochemical Properties and PEG Modification of Magnetic Liposomes on Their Interaction with Intestinal Epithelial Caco-2 Cells
Influence of Physicochemical Properties and PEG Modification of Magnetic Liposomes on Their Interaction with Intestinal Epithelial Caco-2 Cells
复制标题
DOI：
10.1248/bpb.b17-00563
复制
发表时间：
2017-12-01
影响因子：
2
通讯作者：
Fujita, Takuya
中科院分区：
文献类型：
--
作者：
Kono, Yusuke;Jinzai, Hitomi;Fujita, Takuya
本研究旨在研究磁性脂质体的粒径(100、500 nm)、表面电荷(阳离子、中性和阴离子)以及聚乙二醇(PEG)修饰对其与人小肠上皮细胞株Caco-2相互作用的影响。在磁场作用下，所有磁性脂质体的细胞结合量均显著增加。磁性阳离子脂质体对Caco-2细胞的结合和内化作用最强。此外，与大磁性脂质体相比，小磁性脂质体更有效地结合和吸收到细胞中。相反，聚乙二醇化修饰显著减弱了磁场对磁性脂质体细胞结合的增强作用。我们还发现磁性阳离子脂质体对Caco-2细胞具有最高的滞留性能。此外，大磁性脂质体对细胞的滞留时间远长于小磁性脂质体。此外，磁性阳离子和中性脂质体在Caco-2细胞中具有较高的稳定性，而磁性阴离子脂质体在Caco-2细胞中降解迅速。这些结果表明，磁性脂质体的物理化学性质和聚乙二醇化修饰对其肠道上皮转运有很大影响。
The present study aimed to investigate the effect of particle size (100, 500 nm), surface charge (cationic, neutral and anionic) and polyethylene glycol (PEG) modification of magnetic liposomes on their interaction with the human intestinal epithelial cell line, Caco-2. The cellular associated amount of all the magnetic liposomes was significantly increased by the presence of a magnetic field. The highest association and internalization into Caco-2 cells was observed with magnetic cationic liposomes. Moreover, small magnetic liposomes were more efficiently associated and taken up into the cells, than large ones. In contrast, PEG modification significantly attenuated the enhancing effect of the magnetic field on the cellular association of magnetic liposomes. We also found that magnetic cationic liposomes had the highest retention properties to Caco-2 cells. Moreover, the retention of large magnetic liposomes to the cells was much longer than that of small ones. In addition, magnetic cationic and neutral liposomes had relatively high stability in Caco-2 cells, whereas magnetic anionic liposomes rapidly degraded. These results indicate that the physicochemical properties and PEG modification of magnetic liposomes greatly influences their intestinal epithelial transport.