Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
Int J Nanomedicine. 2011;6:3151-62. doi: 10.2147/IJN.S25741. Epub 2011 Dec 2.
The aim of this study was to investigate the intestinal mucus-penetrating properties and intestinal cellular uptake of two types of liposomes modified by Pluronic F127 (PF127).
The two types of liposomes, ie, PF127-inlaid liposomes and PF127-adsorbed liposomes, were prepared by a thin-film hydration method followed by extrusion, in which coumarin 6 was loaded as a fluorescence marker. A modified Franz diffusion cell mounted with the intestinal mucus of rats was used to study the diffusion characteristics of the two types of PF127 liposomes. Cell uptake studies were conducted in Caco-2 cells and analyzed using confocal laser scanning microcopy as well as flow cytometry.
The diffusion efficiency of the two types of PF127-modified liposomes through intestinal rat mucus was 5-7-fold higher than that of unmodified liposomes. Compared with unmodified liposomes, PF127-inlaid liposomes showed significantly higher cellular uptake of courmarin 6. PF127-adsorbed liposomes showed a lower cellular uptake. Moreover, and interestingly, the two types of PF127-modified liposomes showed different cellular uptake mechanisms in Caco-2 cells.
PF127-inlaid liposomes with improved intestinal mucus-penetrating ability and enhanced cellular uptake might be a potential carrier candidate for oral drug delivery.
本研究旨在研究两种经 Pluronic F127（PF127）修饰的脂质体的肠道黏液穿透特性和肠道细胞摄取特性。
采用薄膜水化法制备 PF127 镶嵌脂质体和 PF127 吸附脂质体，其中香豆素 6 作为荧光标记物。使用改良的 Franz 扩散池，该扩散池带有大鼠肠黏液，研究两种类型的 PF127 脂质体的扩散特性。在 Caco-2 细胞中进行细胞摄取研究，并使用共聚焦激光扫描显微镜和流式细胞术进行分析。
两种类型的 PF127 修饰的脂质体通过大鼠肠道黏液的扩散效率比未修饰的脂质体高 5-7 倍。与未修饰的脂质体相比，PF127 镶嵌脂质体对香豆素 6 的细胞摄取明显更高。PF127 吸附脂质体的细胞摄取较低。此外，有趣的是，两种类型的 PF127 修饰的脂质体在 Caco-2 细胞中表现出不同的细胞摄取机制。
具有改善的肠道黏液穿透能力和增强的细胞摄取能力的 PF127 镶嵌脂质体可能是口服药物递送的潜在载体候选物。
