title: In vitro and in vivo study of Baicalin-loaded mixed micelles for oral delivery.
abstract: The aim of this work was to research the potential functions and the mechanism of absorption of the baicalin (BC)-loaded micelle system that contained Pluronic P123 copolymer (P123) and sodium taurocholate (ST) as carrier materials via oral delivery. Based on the numerous advantages of oral administration, such as cost-effectiveness, flexible and accommodated dosing regimen, and improved compliance for patients, the ST-P123-MMs system would be evaluated as oral delivery vehicle of BC. In this study, X-ray powder diffractometer analysis confirmed the phase change of BC after being incorporated in mixed micelles. The release study in simulated gastric fluid/simulated intestinal fluid exhibited that BC-loaded ST-P123-MMs presented a sustained drug release behavior. Compared with coumarin-6 solution, higher cellar uptake efficiency was achieved for coumarin-6 loaded ST-P123-MMs towards Caco-2 cell lines. The in situ perfusion test in rat indicated that the absorption of BC-loaded ST-P123-MMs in intestinal tract was stronger than BC solution. After oral administration, the Cmax and AUC of BC-loaded ST-P123-MMs were 1.77 times and 1.54 times as high as those of BC suspension in rat, respectively. Promisingly, the formulated BC exhibited a prolonged circulation time with the oral bioavailability increased to 1.54-fold compared with the control group. These results all suggested that P123 and ST mixed micelles could serve as a promising approach to oral administration of BC.
authors.affiliation: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , China and.
authors.forename: Haiqun
authors.initials: H
authors.lastname: Zhang
authors.affiliation: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , China and.
authors.forename: Xiaoye
authors.initials: X
authors.lastname: Yang
authors.affiliation: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , China and.
authors.forename: Lili
authors.initials: L
authors.lastname: Zhao
authors.affiliation: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , China and.
authors.forename: Yan
authors.initials: Y
authors.lastname: Jiao
authors.affiliation: b Department of Pharmacy , Changhai Hospital, Second Military Medical University , Shanghai , China.
authors.forename: Jiyong
authors.initials: J
authors.lastname: Liu
authors.affiliation: a Department of Pharmaceutics , School of Pharmaceutical Sciences, Shandong University , Jinan , China and.
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry*; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry*; D006801:Humans; D008823:Micelles; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry; D011060:Poloxalene / Q000737:chemistry*; D051381:Rats; D013656:Taurocholic Acid / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005419:Flavonoids; D008823:Micelles; C464484:pluronic block copolymer P123; C038044:baicalin; D013656:Taurocholic Acid; D011060:Poloxalene; D017239:Paclitaxel
keywords: Baicalin; cellular uptake; mixed micelle; oral pharmacokinetics studies