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学科主题: 药学
题名:
A folate modified pH sensitive targeted polymeric micelle alleviated systemic toxicity of doxorubicin (DOX) in multi-drug resistant tumor bearing mice
作者: Li, Xinru1; Yang, Xiucong1; Lin, Zhiqiang1; Wang, Dan1; Mei, Dong1; He, Bing1; Wang, Xiaoyou1; Wang, Xueqing1; Zhang, Qiang1; Gao, Wei1,2
关键词: PH sensitive micelle ; Systemic toxicity ; Folate ; Multi-drug resistant ; Doxorubicin
刊名: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
发表日期: 2015-08-30
DOI: 10.1016/j.ejps.2015.04.018
卷: 76, 页:95-101
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]: DELIVERY-SYSTEMS ; DRUG-RESISTANCE ; CANCER ; CARDIOTOXICITY ; RECEPTOR ; REVERSAL ; THERAPY
英文摘要:

Purpose: The purpose of this work was to demonstrate the advantages of a folate modified pH sensitive micelle system (HPPF) on reducing the systemic toxicity of antitumor drug doxorubicin (DOX) as well as increasing the antitumor efficacy on multi-drug resistant tumor.

Methods: The micelle HPPF was fabricated by PHIS PEG and Fol-PEG-PLA using dialysis method. Multi-drug resistant human breast-cancer cell (MCF-7Adr) was used to test the therapeutic effect of DOX loaded HPPF micelles (HPPF/DOX). Nude mice bearing MCF-7Adr tumor was used to evaluate the systemic toxicity of HPPF/DOX.

Results: The micelle HPPF was successfully prepared with good size uniformity and pH sensitivity. The in vitro experiments showed that HPPF significantly increased the intracellular level and cytotoxicity of DOX. The in vivo experiments demonstrated that HPPF had largely reduced the mortality and body weight loss, improved the animal status and decreased damages on heart and lung tissues comparing to free DOX.

Conclusions: The HPPF/DOX could significantly increase the antitumor efficacy of DOX and largely alleviate the systemic side effects induced by high dose DOX in the treatment of multi-drug resistant tumor. (C) 2015 Elsevier B.V. All rights reserved.

语种: 英语
所属项目编号: 81402857
项目资助者: National Science Foundation of China
WOS记录号: WOS:000356980300011
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/63116
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Tianjin Med Univ, Sch Pharm, Tianjin Key Lab Technol Enabling Dev Clin Therape, Tianjin 300070, Peoples R China

Recommended Citation:
Li, Xinru,Yang, Xiucong,Lin, Zhiqiang,et al. A folate modified pH sensitive targeted polymeric micelle alleviated systemic toxicity of doxorubicin (DOX) in multi-drug resistant tumor bearing mice[J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,2015,76:95-101.
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