Transepithelial transport of rosuvastatin and effect of ursolic acid on its transport in Caco-2 monolayers.

The aim of this study was to determine transepithelial transport characteristics of rosuvastatin and effect of ursolic acid (P-gp potential inhibitor) and ko143 (ABC transporters selective inhibitor) on its transport in Caco-2 monolayers. A reliable Caco-2 cell monolayers model was established. The TEER value was used to inspect integrity of cell model. Apparent permeability coefficients (Papp(BL-AP) and Papp(AP-BL)) were used to analyze transepithelial transport of rosuvastatin. Uptake of rosuvastatin was time- and concentration-dependent in Caco-2 cell. The ko143 but not ursolic acid had effect on the uptake of rosuvastatin in Caco-2 cell monolayer model and affected apparent permeability coefficient and apparent permeability of rosuvastatin. Active transport and passive diffusion absorption existed in transepithelial transport of rosuvastatin in Caco-2 cell model. Ursolic acid had no effect on transport of rosuvastatin in Caco-2 cell monolayer. The result indicated that ursolic acid may not cause effect on intestinal absorption of rosuvastatin.

Citation

Wen Jin Hua, Hu Jin Fang, Wei Xiao Hua. Transepithelial transport of rosuvastatin and effect of ursolic acid on its transport in Caco-2 monolayers. European journal of drug metabolism and pharmacokinetics. 2012 Sep;37(3):225-31

Mesh Tags

Substances

PMID: 22562361

search → result