Influence of borneol and muscone on geniposide transport through MDCK and MDCK-MDR1 cells as blood-brain barrier in vitro model

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• 作者：Zhen-Zhen Chen ; Yang Lu ; Shou-Ying Du ; Ke-Xin Shang ; Cheng-Bo Cai
• 关键词：Geniposide (PubChem CID ; 107848) ; Borneol (PubChem CID ; 64685) ; Muscone (PubChem CID ; 10947)
• 刊名：International Journal of Pharmaceutics
• 出版年：2013
• 出版时间：1 November, 2013
• 年：2013
• 卷：456
• 期：1
• 页码：73-79
• 全文大小：1461 K

文摘

The objective of this study was (1) to characterize geniposide transport through MDCK and MDCK-MDR1 cell lines to confirm its transport mechanism and (2) to evaluate the effect of borneol and muscone as enhancers of geniposide transport in the BBB models so as to explore the enhancement mechanism. Transport studies of geniposide were performed in both directions, from apical to basolateral and from basolateral to apical sides. Drug concentrations were analyzed by HPLC. Geniposide showed relatively poor absorption in MDCK and MDCK-MDR1 cells, apparent permeability coefficients ranging from 0.323 ¡Á 10^?6 to 0.422 ¡Á 10^?6 cm/s. The in vitro experiments showed that geniposide transport in both directions was not concentration dependent and saturable, indicating purely passive diffusion. The efflux ratio of geniposide was less than 2 in the two cell models, which suggested that geniposide was not P-gp substrates. Geniposide transport in both directions significantly increased when co-administrated with increasing concentrations of borneol and muscone. Actin staining results indicated that borneol and muscone increased geniposide transport in the BBB models may attribute to disassembly effect on tight junction integrity.