Liver-targeting doxorubicin-conjugated polymeric prodrug with pH-triggered drug release profile
文献类型：期刊论文
| 作者 | Huang, Jin2,3; Gao, Feng2; Tang, Xiaoxin2; Yu, Jiahui2; Wang, Daxin4; Liu, Shiyuan5; Li, Yaping1
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| 刊名 | POLYMER INTERNATIONAL
 |
| 出版日期 | 2010-10 |
| 卷号 | 59期号:10页码:1390-1396 |
| 关键词 | Gal-PEG-b-PAMAM-Dox(n) polymeric prodrug pH-triggered drug release doxorubicin liver-targeting |
| ISSN号 | 0959-8103 |
| DOI | 10.1002/pi.2880 |
| 文献子类 | Article |
| 英文摘要 | The aim of the research presented was to develop a potential liver-targeting prolonged-circulation polymeric prodrug of doxorubicin (Dox) with a pH-triggered drug release profile. In particular, linear dendritic block copolymers composed of polyamidoamine dendrimer (PAMAM) and poly(ethylene glycol) (PEG; number-average molecular weight of 2000 g mol(-1)) with or without galactose (Gal) were synthesized. Dox was coupled to the copolymers via an acid-labile hydrazone linker. These prodrugs, designated Gal-PEG-b-PAMAM-Dox(n) and mPEG-b-PAMAM-Dox(m), showed accelerated Dox release as the pH decreased from 8.0 to 5.6. Cytotoxicity of the prodrugs was lower than that of free Dox due to the gradual drug release nature. Compared to mPEG-b-PAMAM-Dox(m), Gal-PEG-b-PAMAM-Dox(n) showed rather high cytotoxicity against Bel-7402, suggestive of its galactose receptor-mediated enhanced tumor uptake. This galactose receptor-mediated liver-targeted profile was further confirmed by the prolonged retention time in hepatoma tissue monitored using magnetic resonance imaging. Gal-PEG-b-PAMAM-Dox(n) showed better in vivo antitumor efficacy than free Dox, suggesting its great potential as a polymeric antitumor prodrug. (C) 2010 Society of Chemical Industry |
| WOS关键词 | DELIVERY ; DENDRIMERS ; CYTOTOXICITY ; COPOLYMER ; MECHANISM ; PAMAM ; MICE |
| 资助项目 | Shanghai Municipality Commission[0852nm03700] ; Shanghai Municipality Commission[0952nm05300] ; Shanghai Municipality Commission[09540709000] ; Shanghai Municipality Commission[10410710000] ; Chinese Ministry of Science and Technology[2007CB936104] ; Chinese Ministry of Science and Technology[2009CB930300] ; WUT[00000000] |
| WOS研究方向 | Polymer Science |
| 语种 | 英语 |
| WOS记录号 | WOS:000283103300011 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278769]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Yu, Jiahui |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China 2.E China Normal Univ, Inst Adv Interdisciplinary Res, Shanghai 200062, Peoples R China; 3.Wuhan Univ Technol, Coll Chem Engn, Wuhan 430070, Peoples R China; 4.Yangzhou Univ, Subei Hosp Jiangsu Prov, Yangzhou 225001, Peoples R China; 5.Changzheng Hosp, Dept Diagnost Imaging, Shanghai 200003, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Huang, Jin,Gao, Feng,Tang, Xiaoxin,et al. Liver-targeting doxorubicin-conjugated polymeric prodrug with pH-triggered drug release profile[J]. POLYMER INTERNATIONAL,2010,59(10):1390-1396. |
| APA | Huang, Jin.,Gao, Feng.,Tang, Xiaoxin.,Yu, Jiahui.,Wang, Daxin.,...&Li, Yaping.(2010).Liver-targeting doxorubicin-conjugated polymeric prodrug with pH-triggered drug release profile.POLYMER INTERNATIONAL,59(10),1390-1396. |
| MLA | Huang, Jin,et al."Liver-targeting doxorubicin-conjugated polymeric prodrug with pH-triggered drug release profile".POLYMER INTERNATIONAL 59.10(2010):1390-1396. |
入库方式： OAI收割
来源：上海药物研究所
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