title: Effects of borneol on the intestinal transport and absorption of two P-glycoprotein substrates in rats.
abstract: 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 C(max) and AUC(0→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.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, Dongchuan Road 800, Shanghai 200240, China.
authors.forename: Huijuan
authors.initials: H
authors.lastname: He
authors.forename: Qi
authors.initials: Q
authors.lastname: Shen
authors.forename: Jian
authors.initials: J
authors.lastname: Li
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000042:Absorption / Q000187:drug effects; D000284:Administration, Oral; D000818:Animals; D001692:Biological Transport; D001892:Camphanes / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D003078:Colchicine / Q000032:analysis / Q000378:metabolism* / Q000493:pharmacokinetics; D004058:Diffusion / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005456:Fluorescent Dyes / Q000032:analysis / Q000378:metabolism; D006074:Gout Suppressants / Q000032:analysis / Q000378:metabolism / Q000494:pharmacology*; D007408:Intestinal Absorption / Q000187:drug effects; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D020112:Rhodamine 123 / Q000032:analysis / Q000378:metabolism*
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D001892:Camphanes; D005456:Fluorescent Dyes; D006074:Gout Suppressants; D020112:Rhodamine 123; C022871:isoborneol; D003078:Colchicine