A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas
文献类型：期刊论文
| 作者 | Li, Yan1,2; He, Hai1,2; Jia, Xinru1,2; Lu, Wan-Liang3; Lou, Jinning4; Wei, Yen5 |
| 刊名 | BIOMATERIALS
 |
| 出版日期 | 2012-05-01 |
| 卷号 | 33期号:15页码:3899-3908 |
| 关键词 | Blood-brain Barrier (Bbb) Pamam Dual-targeting Ph-sensitive Gliomas |
| ISSN号 | 0142-9612 |
| DOI | 10.1016/j.biomaterials.2012.02.004 |
| 英文摘要 | A pH-sensitive dual-targeting drug carrier (G4-DOX-PEG-Tf-TAM) was synthesized with transferrin (TO conjugated on the exterior and Tamoxifen (TAM) in the interior of the fourth generation PAMAM dendrimers for enhancing the blood-brain barrier (BBB) transportation and improving the drug accumulation in the glioma cells. It was found that, on average, 7 doxorubicine (DOX) molecules, over 30 PEG(1000) and PEG(2000) chains and one Tf group were bonded on the periphery of each G4 PAMAM dendrimer, while 29 TAM molecules were encapsulated into the interior of per dendrimer. The pH-triggered DOX release was 32% at pH 4.5 and 6% at pH 7.4, indicating a comparatively fast drug release at weak acidic condition and stable state of the carrier at physiological environment. The in vitro assay of the drug transport across the BBB model showed that G4-DOX-PEG-Tf-TAM exhibited higher BBB transportation ability with the transporting ratio of 6.06% in 3 h. The carrier was internalized into C6 glioma cells upon crossing the BBB model by the coactions of TfR-mediated endocytosis and the inhibition effect of TAM to the drug efflux transports. Moreover, it also displayed the in vitro accumulation of DOX in the avascular C6 glioma spheroids made the tumor volume effectively reduced. (C) 2012 Elsevier Ltd. All rights reserved. |
| 语种 | 英语 |
| WOS记录号 | WOS:000303273200013 |
| 出版者 | ELSEVIER SCI LTD |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/48133]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Jia, Xinru |
| 作者单位 | 1.Peking Univ, Coll Chem & Mol Engn, Minist Educ, Beijing Natl Lab Mol Sci, Beijing 100871, Peoples R China 2.Peking Univ, Coll Chem & Mol Engn, Minist Educ, Key Lab Polymer Chem & Phys, Beijing 100871, Peoples R China 3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China 4.Minist Hlth, China Japan Friendship Hosp, Inst Clin Med Sci, Beijing, Peoples R China 5.Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Yan,He, Hai,Jia, Xinru,et al. A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas[J]. BIOMATERIALS,2012,33(15):3899-3908. |
| APA | Li, Yan,He, Hai,Jia, Xinru,Lu, Wan-Liang,Lou, Jinning,&Wei, Yen.(2012).A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas.BIOMATERIALS,33(15),3899-3908. |
| MLA | Li, Yan,et al."A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas".BIOMATERIALS 33.15(2012):3899-3908. |
入库方式： OAI收割
来源：化学研究所
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