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KMID : 0043320110340071161
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Archives of Pharmacal Research
2011 Volume.34 No. 7 p.1161 ~ p.1170
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Effects of borneol on the intestinal transport and absorption of two P-glycoprotein substrates in rats
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He Huijuan
Shen Qi
Li Jian
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Abstract
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As the most prevalent route of delivery, oral administration has the challenge of potentially low bioavailability in part because P-glycoprotein (P-gp) in the intestinal tract affects absorption. Therefore, absorption enhancers or P-gp inhibitors are strategies to solve this problem. The aim of the present study was to investigate the effects of borneol on transportation of colchicine and rhodamine123, two P-gp substrates, in rats. In vitro transportation was assessed with a diffusion chamber system with isolated rat intestines. Different concentrations of borneol (10, 40 and 80 μg/mL) were prepared in solutions with two P-gp substrates compared with blank solutions. The in vivo effects on colchicine were assessed by a pharmacokinetic study. Borneol enhanced the absorptive transport of two P-gp substrates, which was relevant to the concentration. A pharmacokinetic study showed that in the presence of borneol, a significant increase in Cmax and AUC0→8 of colchicine occurred when compared to colchicine alone. The study showed that borneol affected two P-gp substrates in the intestine, possibly by inhibiting the effects of P-gp and enhancing intestinal absorption of drugs. Therefore, borneol could be developed as a P-gp inhibitor and absorptive enhancer.
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KEYWORD
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P-glycoprotein, Colchicine, Rhodamine123, Borneol, Intestinal absorption, Bioavailability
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