摘要
目的研究鹰嘴豆芽素A(BCA)及其聚乙二醇化纳米脂质载体(PEG-BCA-NLC)的细胞吸收转运机制。方法用Caco-2细胞模型研究BCA及PEG-BCA-NLC的摄取、转运及其影响因素;用高效液相色谱法检测BCA浓度,计算其表观通透系数(Papp)。结果 Caco-2细胞对BCA及PEG-BCANLC的吸收符合被动扩散过程,但相同时间下BCA的摄取量较PEG-BCA-NLC高;加入维拉帕米可有效提高Caco-2细胞对PEG-BCA-NLC的吸收转运,Papp(肠腔侧→基底层,AP→BL)增大,而Papp(BL→AP)变小,但转运量仍较BCA溶液组低。结论 PEG-BCA-NLC在Caco-2细胞模型中的吸收转运主要是被动扩散方式,PEG-BCA-NLC不一定能显著提高药物在小肠的吸收。
Objective To investigate the absorption mechanism of Bio-chanin A （ BCA） and PEGylated BCA loaded nanostructured lipid carri-ers （ PEG -BCA -NLC ） across Caco -2 cell model.Methods Caco-2 cell monolayer model was used to explore the uptake , transport and impact factors of BCA and PEG -BCA-NLC.Drug concentration was measured by HPLC and the apparent permeability coefficients （ Papp ） were calculated.Results The main mechanism of BCA and PEG-BCA-NLC across Caco -2 monolayer model was passive diffu-sion.But under the same time , lower uptake of drug in Caco -2 cells was observed at PEG -BCA -NLC group comparing to that at BCA group.The absorption and the apparent permeability coefficient of BCA in Caco-2 cells monolayer were increased when combined with verapam-il.The Papp （AP→BL） increased and Papp （BL→PL） reduced, but the uptake content was much lower than BCA solution.Conclusion Ab-sorption process of PEG -BCA-NLC in Caco-2 cells monolayer met the characteristics of passive diffusion.However , the PEG-BCA-NLC may not significantly improve the absorption of BCA in intestinal epithelial.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2014年第8期715-718,共4页
The Chinese Journal of Clinical Pharmacology
基金
安徽中医药大学研究生科技创新基金项目(2013yb010)
