title: Enhancing effects of chitosan and chitosan hydrochloride on intestinal absorption of berberine in rats.
abstract: Berberine chloride (BBR) is a plant alkaloid that has been used for centuries for treatment of inflammation, dysentery, and liver diseases. It is poorly absorbed from the gastrointestinal (GI) tract and its various clinical uses are limited because of its poor bioavailability. The object of the present study was to investigate the absorption enhancing effect of chitosan on BBR. Mixtures of BBR and chitosan were prepared and the absorption enhancement was investigated in rats. The results showed a dose-dependent absorption enhancement produced by chitosan. Formulations containing 0.5%, 1.5%, and 3.0% chitosan resulted in improvement of AUC(0-36 h) values by 1.9, 2.2, 2.5 times. The absorption enhancing ability of chitosan may be due to its ability to improve the BBR paracellular pathway in the intestinal tract. Chitosan hydrochloride, a salt of chitosan, was also investigated in this study. However, the addition of 2.0% and 3.3% chitosan hydrochloride to BBR solution did not produce any increase in either C(max) or AUC(0-36 h) of BBR. Subsequent solubility studies suggested that the reduced berberine chloride solubility in chitosan hydrochloride may limit the enhancement ability. This study showed that the optimum formulation producing the highest BBR absorption is the BBR solution containing 3.0% chitosan.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Wenhua 103, Liaoning, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Chen
authors.forename: Dongjiao
authors.initials: D
authors.lastname: Fan
authors.forename: Lingkuo
authors.initials: L
authors.lastname: Meng
authors.forename: Yuqiang
authors.initials: Y
authors.lastname: Miao
authors.forename: Shenshen
authors.initials: S
authors.lastname: Yang
authors.forename: Yan
authors.initials: Y
authors.lastname: Weng
authors.forename: Haibing
authors.initials: H
authors.lastname: He
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001599:Berberine / Q000737:chemistry* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry*; D041981:Gastrointestinal Tract / Q000378:metabolism; D007408:Intestinal Absorption; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D012996:Solutions / Q000737:chemistry
chemical_list: D012996:Solutions; D001599:Berberine; D048271:Chitosan