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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、60 μg/mL)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 (Kapp) 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 (Papp) of those drugs containing low-concentration, medium-concentration and high-concentration (20, 40, 60 μg/mL) of silymarin in Caco-2 cell model were also investigated. RESULTS: Compared with Silymarin suspension, Ka and Kapp of 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 Papp of 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.
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
SilymarinEnteric coated-PLGA nanoparticlein situ intestine perfusion modelColonic adenoma Caco-2 cellAbsorption
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