SN38-based albumin-binding prodrug for efficient targeted cancer chemotherapy
文献类型：期刊论文
| 作者 | Huang, Ying1; Wang, Lei1; Cheng, Zhiyang1; Yang, Biyu2; Yu, Jiahui1; Chen, Yi2 ; Lu, Wei1
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| 刊名 | JOURNAL OF CONTROLLED RELEASE
 |
| 出版日期 | 2021-11-10 |
| 卷号 | 339页码:297-306 |
| 关键词 | Antitumour Chemotherapy SN38 Drug delivery systems Albumin |
| ISSN号 | 0168-3659 |
| DOI | 10.1016/j.jconrel.2021.09.040 |
| 通讯作者 | Wang, Lei(lwang@chem.ecnu.edu.cn) ; Chen, Yi(ychen@simm.ac.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn) |
| 英文摘要 | Developing new therapeutic strategies that damage tumour cells without harming normal tissues is among the primary obstacles in chemotherapy. In this study, a novel 13-glucuronidase-sensitive albumin-binding prodrug was designed and synthesized to selectively deliver the drug SN38 to tumour sites and maximize its efficacy. After intravenous administration, the prodrug Mal-glu-SN38 covalently bound to plasma albumin through the Michael addition, enabling it to accumulate in the tumour and release SN38 when triggered by extracellular 13-glucuronidase. Compared to irinotecan, Mal-glu-SN38 displayed a slower plasma clearance and increased drug exposure over time. Moreover, Mal-glu-SN38 caused an increase in tumour-site accumulation of both the albumin-prodrug conjugate and free SN38 released from albumin conjugate when compared with irinotecan. After administration of multiple doses, Mal-glu-SN38 also significantly delayed the tumour growth, resulting in an impressive reduction or even disappearance of tumours (67% of mice cured) without causing any observable side effects. |
| WOS关键词 | TOPOISOMERASE-I INHIBITORS ; DRUG-DELIVERY ; NANOPARTICLES ; DOXORUBICIN ; EFFICACY ; CONJUGATE ; THERAPY ; VIVO |
| 资助项目 | Fundamental Research Funds for the Central Universities ; National Natural Science Foundation of China[22077034] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000707425500003 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/298433]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Wang, Lei; Chen, Yi; Lu, Wei |
| 作者单位 | 1.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, Shanghai 200062, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, Ying,Wang, Lei,Cheng, Zhiyang,et al. SN38-based albumin-binding prodrug for efficient targeted cancer chemotherapy[J]. JOURNAL OF CONTROLLED RELEASE,2021,339:297-306. |
| APA | Huang, Ying.,Wang, Lei.,Cheng, Zhiyang.,Yang, Biyu.,Yu, Jiahui.,...&Lu, Wei.(2021).SN38-based albumin-binding prodrug for efficient targeted cancer chemotherapy.JOURNAL OF CONTROLLED RELEASE,339,297-306. |
| MLA | Huang, Ying,et al."SN38-based albumin-binding prodrug for efficient targeted cancer chemotherapy".JOURNAL OF CONTROLLED RELEASE 339(2021):297-306. |
入库方式： OAI收割
来源：上海药物研究所
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