中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2014年
8期
715-718
,共4页
罗晴%王雷%林彤远%朱婷婷%陈卫东
囉晴%王雷%林彤遠%硃婷婷%陳衛東
라청%왕뢰%림동원%주정정%진위동
鹰嘴豆芽素A%Caco-2细胞%摄取%转运
鷹嘴豆芽素A%Caco-2細胞%攝取%轉運
응취두아소A%Caco-2세포%섭취%전운
biochanin A%Caco-2 cell%uptake%transport
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-BCA-NLC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。
目的:研究鷹嘴豆芽素 A ( BCA )及其聚乙二醇化納米脂質載體( PEG-BCA-NLC)的細胞吸收轉運機製。方法用Caco-2細胞模型研究BCA及PEG-BCA-NLC的攝取、轉運及其影響因素;用高效液相色譜法檢測BCA濃度,計算其錶觀通透繫數( Papp )。結果 Caco-2細胞對BCA及PEG-BCA-NLC的吸收符閤被動擴散過程,但相同時間下BCA的攝取量較PEG-BCA-NLC高;加入維拉帕米可有效提高Caco-2細胞對PEG-BCA-NLC的吸收轉運,Papp (腸腔側→基底層,AP→BL)增大,而Papp( BL→AP)變小,但轉運量仍較BCA溶液組低。結論 PEG-BCA-NLC在Caco-2細胞模型中的吸收轉運主要是被動擴散方式,PEG-BCA-NLC不一定能顯著提高藥物在小腸的吸收。
목적:연구응취두아소 A ( BCA )급기취을이순화납미지질재체( PEG-BCA-NLC)적세포흡수전운궤제。방법용Caco-2세포모형연구BCA급PEG-BCA-NLC적섭취、전운급기영향인소;용고효액상색보법검측BCA농도,계산기표관통투계수( Papp )。결과 Caco-2세포대BCA급PEG-BCA-NLC적흡수부합피동확산과정,단상동시간하BCA적섭취량교PEG-BCA-NLC고;가입유랍파미가유효제고Caco-2세포대PEG-BCA-NLC적흡수전운,Papp (장강측→기저층,AP→BL)증대,이Papp( BL→AP)변소,단전운량잉교BCA용액조저。결론 PEG-BCA-NLC재Caco-2세포모형중적흡수전운주요시피동확산방식,PEG-BCA-NLC불일정능현저제고약물재소장적흡수。
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.