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Self-Assembled Core-Shell-Type Lipid-Polymer Hybrid Nanoparticles: Intracellular Trafficking and Relevance for Oral Absorption

文献类型：期刊论文

作者Li, Qiuxia2,3; Xia, Dengning3; Tao, Jinsong3,4; Shen, Aijun1,3; He, Yuan2,3; Gan, Yong3; Wang, Chi2
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
出版日期2017-10
卷号106期号:10页码:3120-3130
ISSN号0022-3549
关键词endocytosis drug transport oral absorption poly(lactic-co-glycolic acid) nanoparticles saquinavir
DOI10.1016/j.xphs.2017.05.029
文献子类Article
英文摘要Lipid-polymer hybrid nanoparticles (NPs) are advantageous for drug delivery. However, their intracellular trafficking mechanism and relevance for oral drug absorption are poorly understood. In this study, self-assembled core-shell lipid-polymer hybrid NPs made of poly(lactic-co-glycolic acid) (PLGA) and various lipids were developed to study their differing intracellular trafficking in intestinal epithelial cells and their relevance for oral absorption of a model drug saquinavir (SQV). Our results demonstrated that the endocytosis and exocytosis of hybrid NPs could be changed by varying the kind of lipid. A glyceride mixture (hybrid NPs-1) decreased endocytosis but increased exocytosis in Caco-2 cells, whereas the phospholipid (E200) (hybrid NPs-2) decreased endocytosis but exocytosis was unaffected as compared with PLGA nanoparticles. The transport of hybrid NPs-1 in cells involved various pathways, including caveolae/lipid raft-dependent endocytosis, and clathrin-mediated endocytosis and macropinocytosis, which was different from the other groups of NPs that involved only caveolae/lipid raft-dependent endocytosis. Compared with that of the reference formulation (nanoemulsion), the oral absorption of SQV-loaded hybrid NPs in rats was poor, probably due to the limited drug release and transcytosis of NPs across the intestinal epithelium. In conclusion, the intracellular processing of hybrid NPs in intestinal epithelia can be altered by adding lipids to the NP. However, it appears unfavorable to use PLGA-based NPs to improve oral absorption of SQV compared with nanoemulsion. Our findings will be essential in the development of polymer-based NPs for the oral delivery of drugs with the purpose of improving their oral absorption. (C) 2017 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
WOS关键词DRUG-DELIVERY PLATFORM ; PLGA NANOPARTICLES ; EPITHELIAL-CELLS ; BIODEGRADABLE MICROPARTICLES ; TRANSPORT PATHWAYS ; CELLULAR UPTAKE ; SAQUINAVIR ; ENDOCYTOSIS ; MECHANISMS ; RAFTS
资助项目National Natural Science Foundations of China[81673379] ; National Natural Science Foundations of China[81373356] ; Youth Innovation Promotion Association CAS[2017336] ; Pharmaceutical Innovation Project of Chinese Academy of Sciences[CASIMM0120163016] ; Shanghai Science and Technology Innovation Action Plan for Basic Research[14JC1493200]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
出版者WILEY
WOS记录号WOS:000417340200022
源URL[http://119.78.100.183/handle/2S10ELR8/272459]  
专题药物制剂研究中心
通讯作者Xia, Dengning; Gan, Yong; Wang, Chi
作者单位1.China Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Nanjing 210009, Jiangsu, Peoples R China
2.Chongqing Med Univ, Sch Pharm, Dept Pharmaceut, Chongqing 400016, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
4.Nanchang Univ, Dept Pharm, Coll Clin Med, Nanchang 330047, Jiangxi, Peoples R China;
推荐引用方式
GB/T 7714		 Li, Qiuxia,Xia, Dengning,Tao, Jinsong,et al. Self-Assembled Core-Shell-Type Lipid-Polymer Hybrid Nanoparticles: Intracellular Trafficking and Relevance for Oral Absorption[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2017,106(10):3120-3130.
APA Li, Qiuxia.,Xia, Dengning.,Tao, Jinsong.,Shen, Aijun.,He, Yuan.,...&Wang, Chi.(2017).Self-Assembled Core-Shell-Type Lipid-Polymer Hybrid Nanoparticles: Intracellular Trafficking and Relevance for Oral Absorption.JOURNAL OF PHARMACEUTICAL SCIENCES,106(10),3120-3130.
MLA Li, Qiuxia,et al."Self-Assembled Core-Shell-Type Lipid-Polymer Hybrid Nanoparticles: Intracellular Trafficking and Relevance for Oral Absorption".JOURNAL OF PHARMACEUTICAL SCIENCES 106.10(2017):3120-3130.

入库方式： OAI收割

来源：上海药物研究所

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