SODIUM CAPRATE ELICITS DILATATIONS IN HUMAN INTESTINAL TIGHT JUNCTIONS AND ENHANCES DRUG ABSORPTION BY THE PARACELLULAR ROUTE

被引:215
作者
ANDERBERG, EK [1 ]
LINDMARK, T [1 ]
ARTURSSON, P [1 ]
机构
[1] UNIV UPPSALA,CTR BIOMED,DEPT PHARMACEUT,BOX 580,S-75123 UPPSALA,SWEDEN
关键词
ABSORPTION ENHANCER; TIGHT JUNCTION; DRUG ABSORPTION; INTESTINAL EPITHELIUM; CACO-2; FATTY ACID; SODIUM CAPRATE;
D O I
10.1023/A:1018909210879
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The effects of the absorption enhancer sodium caprate on human intestinal epithelial cells were investigated using Caco-2 cell monolayers. The effects on epithelial integrity and drug transport are dependent on time and concentration and are decreased by Ca2+, most likely through the formation of Ca2+ soaps. Morphological data indicate that exposure to sodium caprate results in cytoskeletal changes and in structural alterations of the tight junctions in the form of dilatations, while the effects on the apical cell membranes are limited. We conclude that sodium caprate increases the absorption of drugs mainly by the paracellular route.
引用
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页码:857 / 864
页数:8
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