复方一枝蒿复合磷脂脂质体的制备及其在Caco-2细胞模型中的吸收特性研究  

Preparation of Co.YiZhiHao composite phospholipid liposomes and investigation of its intestinal transportation on Caco-2 cell monolayer model

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作  者:陈蕾 姜雯[2] 曾诚 潘晓梅[2] 邢建国 

机构地区:[1]新疆维吾尔自治区卫生与计划生育委员会药品采购中心,乌鲁木齐830000 [2]新疆医科大学第六附属医院药剂科,乌鲁木齐830002 [3]新疆维吾尔自治区药物研究所,乌鲁木齐830004

出  处:《新疆医科大学学报》2016年第3期320-323,326,共5页Journal of Xinjiang Medical University

基  金:新疆维吾尔自治区自然科学基金(2014211C136)

摘  要:目的通过建立体外Caco-2细胞模型,考察复方一枝蒿提取物和复方一枝蒿复合磷脂脂质体的转运机制。方法采用硫酸铵梯度法制备复方一枝蒿复合磷脂脂质体,考察其理化性质,并利用Caco-2细胞模型,研究和评估复方一枝蒿提取物和复方一枝蒿复合磷脂脂质体的肠吸收和转运特征。结果在Caco-2细胞单层模型中,复方一枝蒿复合磷脂脂质体的渗透系数(Papp)与复方一枝蒿提取物对比增加了6倍,复方一枝蒿提取物从apical(A,肠腔面)到basolateral(B,基底面)的(Papp)等于B到A,转运符合被动扩散,通过复合磷脂脂质体包裹后,提高复方一枝蒿提取物透射率(A到B的(Papp)>B到A的(Papp))具有一定的主动转运效果。结论通过复合磷脂脂质体包裹复方一枝蒿提取物促进了其跨膜转运,并进一步提高了复方一枝蒿提取物的转运能力。Objective To investigate the mechanisms of action of transportation of compound YIZHIHAO extract(CYE)and compound YiZhiHao(CY)composite phospholipid liposomes(CPL)across Caco-2cell monolayer model.Methods The method of ammonium sulfate transmembrane gradients was adopted to prepare compound YiZhiHao composite phospholipid liposomes(CYCPL),and Caco-2cell was applied to evaluate the transport properties of CYE and CYCPL.The concentration of CYE in Caco-2cell experiment was determined by HPLC.Results In Caco-2cell uptake,a 6-fold increase on CYE permeability was obtained for CPL when compared with CYE alone,and Pappof Apical to Basolateral was equal to that of Basolateral to Apical,which indicated that the transport of CYE was passive diffusion.Due to CPL,the permeating amount of CYE was enhanced.Conclusion CPL could enhance transport of CYE and the permeating enhancement was obviously improved on Caco-2cell monolayer model.

关 键 词:复方一枝蒿提取物 复合磷脂脂质体 包封率 CACO-2细胞模型 

分 类 号:R914[医药卫生—药物化学]

 

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