水飞蓟素肠溶聚乳酸-羟基乙酸共聚物纳米粒在大鼠在体肠灌流模型及Caco-2细胞模型中的吸收研究  

Study on the Absorption of Silymarin Enteric Coated- PLGA Nanoparticles in Rat in situ Intestine Perfusion Model and Caco-2 Cell Model

作　　者：何静[1] 邱妍川[2] 杨延音[2] 林凤云[2] 刘松青[3] 江尚飞[2] 朱照静[2] 

机构地区：[1]重庆医药高等专科学校继续教育学院,重庆401331 [2]重庆医药高等专科学校药学院,重庆401331 [3]第三军医大学第一附属医院药剂科,重庆400038

出　　处：《中国药房》2017年第1期46-49,共4页China Pharmacy

基　　金：重庆市科技攻关计划项目(No.cstc2012ggyyjs10008);重庆市医学科研计划项目(No.2012-2-256)

摘　　要：目的:研究水飞蓟素肠溶聚乳酸-羟基乙酸共聚物(PLGA)纳米粒在大鼠在体肠灌流模型及结肠腺癌Caco-2细胞模型中的吸收特性。方法:采用高效液相色谱法测定水飞蓟素含量,考察水飞蓟素混悬液、水飞蓟素PLGA纳米粒和水飞蓟素肠溶PLGA纳米粒在大鼠在体肠灌流模型十二指肠、空肠、回肠和结肠的吸收速率常数(Ka)和表观吸收系数(Kapp)及其含低、中、高质量浓度(20、40、60μg/m L)水飞蓟素时在Caco-2细胞模型中的表观渗透系数(Papp)。结果:与水飞蓟素混悬液比较,水飞蓟素PLGA纳米粒和水飞蓟素肠溶PLGA纳米粒在十二指肠、空肠、回肠和结肠的Ka、Kapp均增加(P<0.05);与对应浓度水飞蓟素混悬液比较,含低、中、高质量浓度水飞蓟素的肠溶PLGA纳米粒和PLGA纳米粒在Caco-2细胞模型中的双向Papp均增加(P<0.05),其中水飞蓟素的肠溶PLGA纳米粒与PLGA纳米粒间差异无统计学意义(P>0.05)。结论:水飞蓟素肠溶PLGA纳米粒可有效增加水飞蓟素肠内吸收及Caco-2细胞摄取和跨膜转运速率。OBJECTIVE：To study the absorption features of Silymarin enteric coated- polyllactic- co- glycolic acid（PLGA）nanoparticles in rat in situ intestine perfusion model and colonic adenoma Caco-2 cell model. METHODS：HPLC method was used to determine the content of silymarin. The absorption rate constant（Ka）and apparent absorption coefficient（K（app））of Silymarin suspension,Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were investigated in duodenum,jejunum,ileum and colon of rat in situ intestine perfusion model;the apparent permeability coefficient（P（app））of those drugs containing lowconcentration,medium-concentration and high-concentration（20,40,60 μg/m L）of silymarin in Caco-2 cell model were also investigated. RESULTS：Compared with Silymarin suspension,Kaand Kappof Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were all increased in duodenum,jejunum,ileum and colon（P〈0.05）;compared with the corresponding concentration Silymarin suspension,two-way Pappof Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles containing low- concentration,medium- concentration and high- concentration of silymarin were all increased in Caco- 2 cell model（P〈0.05）;there was no statistical significance between Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles（P〉0.05）. CONCLUSIONS：Silymarin enteric coated-PLGA nanoparticles can effectively increase the intestinal absorption,cellular uptake and transmembrane transport rate of silymarin.

关 键 词：水飞蓟素 肠溶聚乳酸-羟基乙酸共聚物纳米粒 在体肠灌流模型 结肠腺癌Caco-2细胞 吸收 

分 类 号：R965[医药卫生—药理学]