Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation
文献类型:期刊论文
作者 | Zhang, Pengcheng1![]() ![]() ![]() ![]() ![]() |
刊名 | JOURNAL OF CONTROLLED RELEASE
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出版日期 | 2012-05-10 |
卷号 | 159期号:3页码:429-434 |
关键词 | Blood-brain barrier (BBB) Transferrin Polyphosphoester Micelle Glioma |
ISSN号 | 0168-3659 |
DOI | 10.1016/j.jconrel.2012.01.031 |
文献子类 | Article |
英文摘要 | The successful treatment of central nervous system (CNS) disorders is hampered by inefficient drug delivery across the blood-brain barrier (BBB). Transferrin (Tf) could facilitate the transcytosis of coupled nanocarriers through Tf receptor (TfR) mediated pathway. In this study, Tf-modified paclitaxel-loaded polyphosphoester hybrid micells (TPM) was prepared and evaluated for its in vitro and in vivo brain-targeting efficiency. The polyphosphoester hybrid micelle formed a core-shell structure in aqueous solution, and demonstrated high drug entrapping efficiency (89.9 +/- 3.4%). In addition, the micelle showed negligible hemolysis even at 2.0 mg/mL. The TPM was 87.85 +/- 2.32 nm with zeta potentials -12.33 +/- 1.46 mV, and PTX showed sustained release from TPM. TPM demonstrated enhanced cellular uptake and brain accumulation, which were 2 and 1.8-fold of PM, respectively. TPM exhibited strongest anti-glioma activity, and the mean survival time of mice bearing intracranial U-87 MG glioma treated with TPM (39.5 days) was significantly longer than those treated with Taxol (R) (33.6 days). These results indicated that Tf conjugated micelle could be a promising carrier for brain-targeting drug delivery. (C) 2012 Elsevier B.V. All rights reserved. |
WOS关键词 | DRUG-DELIVERY ; POLYMERIC MICELLES ; BARRIER BBB ; NANOPARTICLES ; PHARMACOKINETICS ; TRANSPORT ; VITRO ; RATS |
资助项目 | National Basic Research Program of China[2010CB934000] ; National Basic Research Program of China[2009CB930304] ; National Basic Research Program of China[2007CB935804] ; National Natural Science Foundation of China[30925041] ; National Natural Science Foundation of China[30901866] ; Shanghai Elitist Program[11XD1406200] |
WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
语种 | 英语 |
WOS记录号 | WOS:000305001600016 |
出版者 | ELSEVIER SCIENCE BV |
源URL | [http://119.78.100.183/handle/2S10ELR8/278078] ![]() |
专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物制剂研究中心 |
通讯作者 | Feng, Linyin |
作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Zhang, Pengcheng,Hu, Luojuan,Yin, Qi,et al. Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation[J]. JOURNAL OF CONTROLLED RELEASE,2012,159(3):429-434. |
APA | Zhang, Pengcheng,Hu, Luojuan,Yin, Qi,Zhang, Zhiwen,Feng, Linyin,&Li, Yaping.(2012).Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation.JOURNAL OF CONTROLLED RELEASE,159(3),429-434. |
MLA | Zhang, Pengcheng,et al."Transferrin-conjugated polyphosphoester hybrid micelle loading paclitaxel for brain-targeting delivery: Synthesis, preparation and in vivo evaluation".JOURNAL OF CONTROLLED RELEASE 159.3(2012):429-434. |
入库方式: OAI收割
来源:上海药物研究所
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