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学科主题: 药学
题名:
Poly(2-ethyl-2-oxazoline)-Doxorubicin Conjugate-Based Dual Endosomal pH-Sensitive Micelles with Enhanced Antitumor Efficacy
作者: Li, Jinwen; Zhou, Yanxia; Li, Chengwei; Wang, Dishi; Gao, Yajie; Zhang, Chao; Zhao, Lei; Li, Yushu; Liu, Yan; Li, Xinru
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2015
DOI: 10.1021/bc5004718
卷: 26, 期:1, 页:110-119
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]: IN-VIVO EVALUATION ; POLYMERIC MICELLES ; DRUG-DELIVERY ; BIOMEDICAL APPLICATIONS ; HYDRAZONE LINKER ; DOXORUBICIN ; BIODISTRIBUTION ; THERAPEUTICS ; HYDROGELS ; RELEASE
英文摘要:

Dual endosomal pH-sensitive micelles were designed and fabricated to deliver doxorubicin (DOX) for treating breast cancer based on a poly(2-ethyl-2-oxazoline) (PEOz)-DOX (PEOz-hyd-DOX) conjugate. PEOz-hyd-DOX was successfully synthesized by connecting DOX to PEOz via an acid cleavable hydrazone linker and self-assembled into nanosized micelles, which further physically encapsulated DOX. The conjugate and DOX-loaded conjugate micelles displayed faster release of DOX at pH 5.0 than at pH 7.4. This pH-dependent release behavior might assist the quick diffusion of DOX from acidic endosomes or lysosomes and the intracellular transfer into the nucleus after internalization, which was confirmed by confocal laser scanning microscopy images. As expected, PEOz-hyd-DOX conjugate and DOX-loaded conjugate micelles maintained cytotoxicity of DOX. In addition, the dual endosomal pH-sensitive micelles were found to substantially enhance antitumor efficacy and reduce side effects compared with free DOX. Therefore, PEOz-hyd-DOX conjugate-based micelles might be potential drug delivery vehicles of DOX for safe and effective breast cancer therapy.

语种: 英语
所属项目编号: 81172990 ; 2015CB932100 ; BMU20110263
项目资助者: National Natural Science Foundation of China ; National Key Science Research Program of China (973 Program) ; Ministry of Education
WOS记录号: WOS:000348483200012
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65650
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China

Recommended Citation:
Li, Jinwen,Zhou, Yanxia,Li, Chengwei,et al. Poly(2-ethyl-2-oxazoline)-Doxorubicin Conjugate-Based Dual Endosomal pH-Sensitive Micelles with Enhanced Antitumor Efficacy[J]. BIOCONJUGATE CHEMISTRY,2015,26(1):110-119.
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