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Investigation of the mechanisms of improved oral bioavailability of bergenin using bergenin-phospholipid complex
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
2014-02-01
DOI10.3109/03639045.2012.752500
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
WOS记录号WOS:000331258400003
引用统计
被引频次:6[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/66306
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Guan, Shan,Qin, Xuan,Zhou, Zhou,Zhang, Qiang,&Huang, Yuan.(2014).Investigation of the mechanisms of improved oral bioavailability of bergenin using bergenin-phospholipid complex.DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,40(2),163-171.
MLA Guan, Shan,et al."Investigation of the mechanisms of improved oral bioavailability of bergenin using bergenin-phospholipid complex".DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 40.2(2014):163-171.
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