title: Effects of β-cyclodextrin on the intestinal absorption of berberine hydrochloride, a P-glycoprotein substrate.
abstract: The major objective of this work is to investigate the enhancing effect of β-cyclodextrin on the intestinal absorption of berberine hydrochloride, a P-glycoprotein (Pgp) substrate. The inclusion complexation behavior of BBH with β-CD was investigated by phase-solubility diagram, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry, NMR spectroscopy, and molecular modeling studies. Results indicated that the 1,3-benzodioxole of BBH was included into the cavity of β-CD to form an inclusion complex which exhibited higher dissolution rate than BBH in vitro. The intestinal absorption of the inclusion complex in rats was significantly higher than the free drug due to its solubilizing effect and Pgp modulatory activity. The mechanisms of β-CD on Pgp modulation were demonstrated by modifying the Pgp ATPase activity, the Pgp mRNA level and the Pgp expression.
authors.affiliation: Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, PR China.
authors.forename: Ye
authors.initials: Y
authors.lastname: Zhang
authors.forename: Yuan-Lu
authors.initials: YL
authors.lastname: Cui
authors.forename: Li-Na
authors.initials: LN
authors.lastname: Gao
authors.forename: Heng-Li
authors.initials: HL
authors.lastname: Jiang
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics* / Q000378:metabolism; D000818:Animals; D001599:Berberine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000378:metabolism* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D004149:Dioxoles / Q000737:chemistry; D015870:Gene Expression / Q000187:drug effects; D007408:Intestinal Absorption / Q000502:physiology*; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008958:Models, Molecular; D012333:RNA, Messenger / Q000235:genetics* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004149:Dioxoles; D012333:RNA, Messenger; D047392:beta-Cyclodextrins; D001599:Berberine; C040539:1,3-benzodioxole