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学科主题: 药学
题名:
Investigation of the mechanisms of improved oral bioavailability of bergenin using bergenin-phospholipid complex
作者: Guan, Shan1; Qin, Xuan1; Zhou, Zhou1; Zhang, Qiang2; Huang, Yuan1
关键词: Bergenin ; Caco-2 cell ; chitosan ; everted rat gut sac model ; phospholipid complex
刊名: DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
发表日期: 2014-02-01
DOI: 10.3109/03639045.2012.752500
卷: 40, 期:2, 页:163-171
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: IN-VIVO ; CHITOSAN ; PERMEABILITY ; DELIVERY ; CACO-2
英文摘要:

Aim: The purpose of this study was to investigate the detailed mechanisms of oral absorption enhancement of bergenin (BN) using BN-phospholipid complex (BPC). Methods: Multiple models such as ex vivo everted rat gut sac model and in vitro Caco-2 cell model were used. Meanwhile, the effect of chitosan on the enhancement of the permeability of BPC was evaluated.

Results: The limited absorption of BN was significantly improved in both ex vivo everted rat gut sac model and in vitro Caco-2 cell model when combined with phospholipid. The transport of BPC was uppermost 5.19-fold higher than that of BN. The results of ex vivo everted rat gut sac model showed that small intestine was a more suitable site for the absorption of BN and BPC than colon. Passive diffusion was the only way employed in the transport of BN, while BPC could transport across enterocytes by both passive diffusion and active transport which was found to be the clathrine-dependent receptor-mediated endocytosis. The absorption of BN was barely improved by the physical mixture of BN and phospholipid due to lack of stable intermolecular interactions. Moreover, the addition of chitosan could open the tight junctions of intestinal epithelial cells, thus significantly increasing the transport of BPC via paracellular route.

Conclusions: Totally different mechanisms, which led to the enhanced oral bioavailability, were utilized in the uptake and transport process of BPC compared with BN. These results would be of significance for the future development of oral delivery systems of BN.

语种: 英语
所属项目编号: 81173010 ; 2009CB903301
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China (973 Program)
WOS记录号: WOS:000331258400003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66306
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Sichuan Univ, West China Sch Pharm, Minist Educ, Key Lab Drug Targeting & Drug Delivery Syst, Chengdu 610041, Sichuan, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China

Recommended Citation:
Guan, Shan,Qin, Xuan,Zhou, Zhou,et al. Investigation of the mechanisms of improved oral bioavailability of bergenin using bergenin-phospholipid complex[J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,2014,40(2):163-171.
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