天山雪莲提取物固体脂质纳米粒的制备及其有效成分芦丁和绿原酸在Caco—2细胞中的摄取

摘要：目的 制备天山雪莲提取物（SIHE）的固体脂质纳米粒（SLNs），并对其形态、粒径、电位、包封率及稳定性等进行考察；考察SIHE-SLNs和SIHE中芦丁和绿原酸在Caco-2细胞中的摄取。方法 采用HPLC建立蘆丁和绿原酸的含量测定方法。采用高压匀质法制备SIHE-SLNs。采用CCK-8法测定SIHE对Caco-2细胞存活率的影响。建立Caco-2细胞模型，进行SIHE-SLNs和SIHE中有效成分芦丁和绿原酸在Caco-2细胞中的摄取。结果 制备的SIHE-SLNs具有较小的粒径和较高的包封率。SIHE浓度低于250 µg/mL对Caco-2细胞无细胞毒性。SIHE-SLNs及SIHE中芦丁和绿原酸在Caco-2细胞中的摄取量随药物浓度和药物作用时间的增加而增加，SIHE-SLNs中的摄取量高于SIHE；抑制剂维拉帕米对SIHE-SLNs和SIHE中绿原酸的作用均随浓度的增加而降低，对SIHE中两成分的降低效果更显著；底物根皮苷可以同时竞争性抑制SIHE-SLNs和SIHE中芦丁的摄取，但对绿原酸影响不大。结论 本研究制备了质量良好的SIHE-SLNs。SIHE-SLNs和SIHE中芦丁和绿原酸在Caco-2细胞中的摄取受浓度、时间和P-糖蛋白抑制剂及底物的影响。

关键词：天山雪莲提取物固体脂质纳米粒；芦丁；绿原酸；Caco-2细胞；P-糖蛋白

DOI：10.3969/j.issn.1005-5304.2018.12.019

中图分类号：R283.5；R285.5 文献标识码：A 文章编号：1005-5304（2018）12-0076-07

Abstract： Objective To prepare Saussureae Involucaratae Herba extracts （SIHE） loaded solid lipid nanoparticles （SLNs）； To inspect the shape， particle size， potential， encapsulation efficiency and stability of SIHE-SLNs； To inspect uptake of rutin and chlorogenic acid of SIHE-SLNs and SIHE in Caco-2 cells. Methods The method for determination of rutin and chlorogenic acid was established by HPLC. SIHE-SLNs were prepared by high pressure homogenization. The effects of SIHE on the survival rate of Caco-2 cells were determined by CCK-8 method. Caco-2 cell model was established， and uptake test of rutin and chlorogenic acid in Caco-2 cells was carried out. Results Prepared SIHE-SLNs had a smaller particles size and higher entrapment efficiency. SIHE had no cytotoxicity to Caco-2 cells in the dose of 250 µg/mL. The uptake of rutin and chlorogenic acid in Caco-2 cells of SIHE-SLNs and SIHE increased with increase of drug concentration and action time， while the absorption of SIHE-SLNs was higher than that of SIHE. The effects of verapamil on chlorogenic acid in SIHE-SLNs and SIHE decreased with increase of drug concentration and was more remarkable in SIHE. The substrate phloridzin could simultaneously competitively inhibit the uptake of rutin in SIHE-SLNs and SIHE， but had no effect on chlorogenic acid. Conclusion SIHE-SLNs prepared in this study have good quality. Uptake of rutin and chlorogenic acid in Caco-2 cells of SIHE-SLNs and SIHE are influenced by concentration， time， P-glycoprotein inhibitor and substrate.

Keywords： Saussureae Involucratae Herba extract loaded solid lipid nanoparticles； rutin； chlorogenic acid； Caco-2 cells； P-glycoprotein

天山雪莲为菊科植物天山雪莲Saussurea involucrata（Kar. et Kir.）Sch.-Bip.的地上部分，是维吾尔民族常用药[1-2]。天山雪莲具有散寒除湿、活血通经、抗炎镇痛、收缩子宫的功效，主要用于各种风湿性关节病、风寒湿痛、月经不调等。研究表明，天山雪莲含有黄酮类、苯丙素类、多糖、生物碱和内酯等成分，具有抗氧化、抗炎、抗疲劳和抗脑缺血/再灌注损伤等药理作用[3-5]。前期研究表明，芦丁和绿原酸是天山雪莲提取物（SIHE）的主要有效成分[6-7]，但因其溶解性较差，口服吸收效果差，生物利用度低，限制了其临床使用[8]。

推荐访问： 芦丁 天山 提取物 制备 摄取

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