Transport features and structural optimization of solid lipid nanoparticles crossing the intestinal epithelium
文献类型：期刊论文
| 作者 | Chai, Guihong1,3; Meng, Yufang2; Chen, Shaoqing3; Hu, Fuqiang3; Gan, Yong1 ; Yuan, Hong3
|
| 刊名 | RSC ADVANCES
 |
| 出版日期 | 2016 |
| 卷号 | 6期号:74页码:70433-70445 |
| ISSN号 | 2046-2069 |
| DOI | 10.1039/c6ra12978a |
| 文献子类 | Article |
| 英文摘要 | Solid lipid nanoparticles (SLNs) have been used to encapsulate drugs with poor solubility and membrane permeability to improve oral bioavailability. In vitro experiments that determine the SLNs fabrication parameters necessary to achieve satisfactory absorption is important to avoid costly and timeconsuming animal experiments. In this study, the Madin-Darby canine kidney (MDCK) cell line was employed to construct a simulated epithelial cell monolayer, and the transport features of SLNs were investigated. Subsequently, SLNs prepared with solid lipid materials with different carbon chain lengths or modified with different amounts of polyethylene glycol monostearate (SA-PEG2000) were used to investigate the relationship between nanoparticle structures and transcytosis efficiency, and the related mechanisms were revealed. Moreover, rats were employed to compare the in vitro and in situ intestinal absorption of these various SLNs. The results demonstrated that the endocytosis and endocellular delivery of SLNs crossing the MDCK cell monolayer were vesicle-mediated processes. Studies of the transport capacity of various SLNs across the cell monolayer showed that the transcytosis of SLNs decreased with increasing carbon chain length, and improved with a certain amount of hydrophilic modification (SA-PEG2000, 20%, w/w). The analysis of molecular mechanisms demonstrated that SLNs prepared by solid lipid materials with a short carbon chain were inclined to be transcytosed via endoplasmic reticulum (ER)-and Golgi complex-mediated pathways; further, SLNs containing an increasingly long carbon chain showed proportionally lower transcytosis by these two organelles. Furthermore, a certain amount of hydrophilic modification can evade transcytosis via the ER-and Golgi complex-mediated pathways for more effective transcytosis. Moreover, the intestinal absorption results were consistent with that found in the simulated epithelial cell monolayer. In conclusion, SLNs prepared with solid lipid materials with a medium-length carbon chain and surface-modified with a certain amount of hydrophilic modification can transcytosis effectively. |
| WOS关键词 | ORAL-DRUG DELIVERY ; IN-VITRO ; POLYMER NANOPARTICLES ; CELL MONOLAYER ; GENE DELIVERY ; MUCUS ; ABSORPTION ; MECHANISMS ; PEPTIDES ; PATHWAYS |
| 资助项目 | National Nature Science Foundation of China[81573366] ; National Nature Science Foundation of China[81473144] ; National Nature Science Foundation of China[8127342] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000381512800091 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276206]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Gan, Yong; Yuan, Hong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Zhejiang Med Co Ltd, Xinchang Pharmaceut Factory, Xinchang 312500, Peoples R China 3.Zhejiang Univ, Coll Pharmaceut Sci, 866 Yuhangtang Rd, Hangzhou 310058, Zhejiang, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Chai, Guihong,Meng, Yufang,Chen, Shaoqing,et al. Transport features and structural optimization of solid lipid nanoparticles crossing the intestinal epithelium[J]. RSC ADVANCES,2016,6(74):70433-70445. |
| APA | Chai, Guihong,Meng, Yufang,Chen, Shaoqing,Hu, Fuqiang,Gan, Yong,&Yuan, Hong.(2016).Transport features and structural optimization of solid lipid nanoparticles crossing the intestinal epithelium.RSC ADVANCES,6(74),70433-70445. |
| MLA | Chai, Guihong,et al."Transport features and structural optimization of solid lipid nanoparticles crossing the intestinal epithelium".RSC ADVANCES 6.74(2016):70433-70445. |
入库方式： OAI收割
来源：上海药物研究所
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