Design, synthesis, and characterization of Schiffbase bond-linked pH-responsive doxorubicin prodrug based on functionalized mPEG-PCL for targeted cancer therapy
文献类型：期刊论文
| 作者 | Zhai, Yinglei2; Zhou, Xing3; Zhang, Zhiqiang1; Zhang, Lei4; Wang, Dianyu2; Wang, Xinhui2; Sun, Wei2 |
| 刊名 | Polymers
 |
| 出版日期 | 2018-10-11 |
| 卷号 | 10期号:10 |
| ISSN号 | 20734360 |
| DOI | 10.3390/polym10101127 |
| 文献子类 | Article |
| 英文摘要 | The side effects of doxorubicin (DOX) extremely limit its application in the treatment of malignant tumors. Nano-sized polymeric drugs based on the acidic microenvironment of tissular- or intra- tumor have attracted ample attention because of their potential in reducing side effects. In this research, an amphiphilic diblock copolymer based on poly (ethylene glycol) (PEG) and functionalized polycaprolactone (PCL) was synthesized and utilized as the drug carrier. DOX was chemically conjugated with the polymer via acid-cleavable imine bonds to obtain a novel pH-sensitive DOX prodrug (mPEG-PCL-Imi-DOX). mPEG-PCL-Imi-DOX (24.2 wt % DOX content) formed micelles with an average diameter of 125 nm through a simple solvent evaporation method. The in vitro release profile demonstrated that DOX release of the prodrug micelles was pH-responsive and able to be accelerated with the decrease of pH. In vitro cytotoxicity assay tests revealed that the pH-sensitive DOX prodrug micelles exhibited relatively lower toxicity and similar antitumor efficacy towards MCF-7 cells compared with free DOX. Hence, the DOX prodrug micelles with imine bonds can offer a carrier with great potential for chemo-therapeutics. |
| 语种 | 英语 |
| 出版者 | MDPI AG, Postfach, Basel, CH-4005, Switzerland |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266963]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Sun, Wei |
| 作者单位 | 1.Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang; 110016, China; 2.Department of Biomedical Engineering, School of Medical Devices, Shenyang Pharmaceutical University, Shenyang; 110016, China; 3.Hainan Institute of Materia Medica, Haikou; 570311, China; 4.Shanghai Pharma Group 5.Northern Pharmaceutical Co., Ltd., Benxi; 117004, China |
| 推荐引用方式 GB/T 7714 | Zhai, Yinglei,Zhou, Xing,Zhang, Zhiqiang,et al. Design, synthesis, and characterization of Schiffbase bond-linked pH-responsive doxorubicin prodrug based on functionalized mPEG-PCL for targeted cancer therapy[J]. Polymers,2018,10(10). |
| APA | Zhai, Yinglei.,Zhou, Xing.,Zhang, Zhiqiang.,Zhang, Lei.,Wang, Dianyu.,...&Sun, Wei.(2018).Design, synthesis, and characterization of Schiffbase bond-linked pH-responsive doxorubicin prodrug based on functionalized mPEG-PCL for targeted cancer therapy.Polymers,10(10). |
| MLA | Zhai, Yinglei,et al."Design, synthesis, and characterization of Schiffbase bond-linked pH-responsive doxorubicin prodrug based on functionalized mPEG-PCL for targeted cancer therapy".Polymers 10.10(2018). |
入库方式： OAI收割
来源：上海药物研究所
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