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poly-L-glutamic acid functionalized nanocomplex for improved oral drug absorption

文献类型：期刊论文

作者Zhu, Quanlei2,3; Song, Wenyi1,2; Xia, Dengning2; Fan, Weiwei2,3; Yu, Miaorong2,3; Guo, Shiyan2; Zhu, Chunliu2; Gan, Yong2
刊名JOURNAL OF MATERIALS CHEMISTRY B
出版日期2015
卷号3期号:43页码:8508-8517
ISSN号2050-750X
DOI10.1039/c5tb01425e
文献子类Article
英文摘要Poor permeability of the intestinal epithelium limits the oral absorption of many drugs. Here, a poly-L-glutamic acid (PGA)-based functional ternary nanocomplex (TC) is reported for enhancing the intestinal absorption of poorly permeable drug doxorubicin hydrochloride (Dox center dot HCl). The particle size and zeta potential of TC were 189.3 +/- 13.7 nm and -29.1 +/- 7.4 mV, respectively. The TC was shown to be more stable under simulated gastrointestinal changing pH or electrolyte content conditions than the binary nanocomplex Dox center dot HCl/PGA. Cellular uptake and the apparent permeability coefficient value (P-app) of the TC were determined to be 5.2- and 4.6-fold higher than that of Dox center dot HCl solutions, respectively. Mechanistic studies showed that active endocytosis caused by specific interactions between gamma-glutamyl terminal groups of PGA and membrane-bound gamma-glutamyl transferase contributed much to the TC-dependent Dox center dot HCl absorption. Studies on the rat model also demonstrated the highest efficiency for Dox center dot HCl absorption by the TC throughout the intestinal tract, with 2.6- and 4.2- fold higher C-max and AUC(0-24h) values compared to Dox center dot HCl solutions. In conclusion, the TC is a promising carrier for improving Dox center dot HCl intestinal absorption, and the rational design of carriers with functional polymer PGA could implement the efficient active absorption of poorly permeable drugs.
WOS关键词IN-VIVO ; CELLULAR UPTAKE ; GLUTATHIONE-CONJUGATE ; INTRACELLULAR FATE ; BARRIER FUNCTION ; DELIVERY ; NANOPARTICLES ; DOXORUBICIN ; TRANSPORT ; TRANSPEPTIDASE
资助项目National Natural Science Foundations of China[81373356] ; National Natural Science Foundations of China[81202468] ; "Science and technology innovation action plan for basic research'' of Shanghai[14JC1493200]
WOS研究方向Materials Science
语种英语
WOS记录号WOS:000364103100010
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/276697]  
专题药物制剂研究中心
通讯作者Gan, Yong
作者单位1.Nanchang Univ, Coll Med, Dept Pharm, Nanchang 330066, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China;
推荐引用方式
GB/T 7714		 Zhu, Quanlei,Song, Wenyi,Xia, Dengning,et al. poly-L-glutamic acid functionalized nanocomplex for improved oral drug absorption[J]. JOURNAL OF MATERIALS CHEMISTRY B,2015,3(43):8508-8517.
APA Zhu, Quanlei.,Song, Wenyi.,Xia, Dengning.,Fan, Weiwei.,Yu, Miaorong.,...&Gan, Yong.(2015).poly-L-glutamic acid functionalized nanocomplex for improved oral drug absorption.JOURNAL OF MATERIALS CHEMISTRY B,3(43),8508-8517.
MLA Zhu, Quanlei,et al."poly-L-glutamic acid functionalized nanocomplex for improved oral drug absorption".JOURNAL OF MATERIALS CHEMISTRY B 3.43(2015):8508-8517.

入库方式： OAI收割

来源：上海药物研究所

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