Masuda Y, Yoshikawa H, Takada K, Muranishi S
J Pharmacobiodyn. 1986 Oct;9(10):793-8. doi: 10.1248/bpb1978.9.793.
The enhancement of absorption of water soluble macromolecules by lipid-surfactant mixed micelles (MM) was performed in two in vitro experimental systems using rat large intestine, which were isolated epithelial cells containing transcellular route alone and everted sac involving trans- and paracellular routes. Four kinds of fluorescein isothiocyanate-labelled dextrans (FDs) having different average molecular weights (9K-70K) were used as models of water soluble macromolecules. In the absence of MM, very poor transport of FDs was observed in both isolated epithelial cells and everted sac experiments. Linoleic acid-polyoxyethylated (60 mol) hydrogenated castor oil (HCO60) MM enhanced the transport of FDs in both systems, especially for smaller size FDs. This promotive effect by MM decreased with an increase in molecular weight of FDs in both systems. Although enhanced transport of the largest FD (molecular weight, 70K) by MM was clearly demonstrated in the everted sac, the enhanced transport of the same FD in the isolated cells was negligible. These results suggest the possibility of participation of paracellular route as well as transcellular route in the enhancing effect of MM on the large intestinal absorption of water soluble macromolecules.
利用大鼠大肠，在两个体外实验系统中研究了脂质 - 表面活性剂混合胶束（MM）对水溶性大分子吸收的增强作用。这两个系统分别是仅含跨细胞途径的分离上皮细胞和涉及跨细胞与细胞旁途径的外翻肠囊。使用四种具有不同平均分子量（9K - 70K）的异硫氰酸荧光素标记葡聚糖（FDs）作为水溶性大分子的模型。在不存在MM的情况下，在分离上皮细胞和外翻肠囊实验中均观察到FDs的转运非常差。亚油酸聚氧乙烯化（60摩尔）氢化蓖麻油（HCO60）混合胶束在两个系统中均增强了FDs的转运，尤其是对于较小尺寸的FDs。在两个系统中，MM的这种促进作用均随着FDs分子量的增加而降低。尽管在外翻肠囊中清楚地证明了MM对最大的FD（分子量70K）的转运增强作用，但在分离细胞中相同FD的转运增强可忽略不计。这些结果表明，细胞旁途径以及跨细胞途径可能参与了MM对水溶性大分子大肠吸收的增强作用。
