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Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles
Tong, Shu-Wen; Xiang, Bai; Dong, Da-Wen; Qi, Xian-Rong
关键词Docetaxel (Dtx) Micelle Antitumor Efficacy Safety Evaluation Solubilization
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2012-09-15
DOI10.1016/j.ijpharm.2012.06.014
434期:1-2页:413-419
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]TARGETED DRUG-DELIVERY ; POLYMERIC MICELLES ; COPOLYMER MICELLES ; IN-VITRO ; CANCER ; SOLUBILIZATION ; CYTOTOXICITY ; SURFACTANTS ; PACLITAXEL ; CARRIERS
英文摘要

To overcome the poor aqueous solubility of docetaxel (DTX) and the side effects of the emulsifier in the marketed formulation, we have developed a DTX-loaded micelle using a nontoxic and biodegradable amphiphilic diblock copolymer, methoxy polyethylene glycol-distearoylphosphatidylethanolamine (mPEG(2000)-DSPE). The prepared micelles exhibited a core-shell structure, and DTX was successfully encapsulated in the core with an encapsulation efficiency of 97.31 +/- 2.95% and a drug loading efficiency of 3.14 +/- 0.13%. The micelles were spherical with a hydrodynamic diameter of approximately 20 nm, which could meet the requirement for in vivo administration, and were expected to enhance the drug′s antitumor efficacy and to decrease its toxicity. To evaluate the DTX-loaded micelles, we chose a well marketed formulation, Taxotere (R), as the control. The prepared DTX micelle had a similar antiproliferative effect to Taxotere (R) in vitro but a significantly better antitumor efficacy than Taxotere (R) in vivo, which may be caused by passive targeting of the tumor by the micelles. In addition, the safety evaluation revealed that the DTX micelle was a qualified drug for use in vivo. Based on the experimental results, we propose that mPEG2000-DSPE micelle is a potent carrier for DTX. (C) 2012 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000306479400049
项目编号30970785 ; 2009CB930303 ; 20100001110056
资助机构National Natural Science Foundation of China ; National Basic Research Program of China ; Doctoral Foundation of the Ministry of Education of China
引用统计
被引频次:42[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51477
专题北京大学药学院_药剂学系
作者单位Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
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GB/T 7714
Tong, Shu-Wen,Xiang, Bai,Dong, Da-Wen,et al. Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2012,434(1-2):413-419.
APA Tong, Shu-Wen,Xiang, Bai,Dong, Da-Wen,&Qi, Xian-Rong.(2012).Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles.INTERNATIONAL JOURNAL OF PHARMACEUTICS,434(1-2),413-419.
MLA Tong, Shu-Wen,et al."Enhanced antitumor efficacy and decreased toxicity by self-associated docetaxel in phospholipid-based micelles".INTERNATIONAL JOURNAL OF PHARMACEUTICS 434.1-2(2012):413-419.
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