Transport of Lipoamide and Lipoic Acid in Caco-2 Cell Monolayer Model
WU Xiao-fang1, CAI Jin1, WANG Jian-ta1,2, LUO Bi-lan1, HUANG Jia-yu1*, TANG Lei1,2*
1. School of Pharmacy, Guizhou Medical University, Guiyang 550025, China; 2. Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550004, China
Abstract：OBJECTIVE To study the transport of lipoamide (LAM) and lipoic acid (LA) in Caco-2 cell monolayer model in vitro. METHODS Effects of LAM and LA on the survival rate of Caco-2 cells were investigated by MTS, the bi-directional transport of lipoamide and lipoic acid from the intestinal cavity side (apical side, AP) to the basal side (basolateral side,BL) was investigated. The cumulative transport volume, apparent permeability coefficient (Papp) and transport percentage were calculated,and the relationships between transport volume and concentration and time were further studied. RESULTS The transport amounts of LAM and LA were increased in time-and concentration-dependent manners, the Papps of LAM and LA (AP→BL) were 2.443 44×10-5-2.392 91×10-5 and 8.179 78×10-6-7.897 25×10-6 cm·s-1, and the Papps(BL→AP) were 2.258 13×10-5-2.214 3×10-5 and 8.267 98×10-6-7.926 73×10-6 cm·s-1, respectively. CONCLUSION In the transport test of Caco-2 cells, LAM is superior to LA, suggesting that it is well absorbed orally and has high bioavailability. But it is still necessary to verify the pharmacokinetic data in vivo.
吴晓芳, 蔡进, 王建塔, 罗碧兰, 黄家宇, 汤磊. 硫辛酰胺与硫辛酸在Caco-2细胞单层模型中的转运研究[J]. 中国药学杂志, 2020, 55(7): 542-548.
WU Xiao-fang, CAI Jin, WANG Jian-ta, LUO Bi-lan, HUANG Jia-yu, TANG Lei. Transport of Lipoamide and Lipoic Acid in Caco-2 Cell Monolayer Model. Chinese Pharmaceutical Journal, 2020, 55(7): 542-548.
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2020, Vol. 55 
