Theranostic supramolecular polymers formed by the self-assembly of a metal-chelating prodrug.,Biomaterials Science

当前位置： X-MOL 学术 › Biomater. Sci. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Theranostic supramolecular polymers formed by the self-assembly of a metal-chelating prodrug.
Biomaterials Science ( IF 5.8 ) Pub Date : 2020-06-25 , DOI: 10.1039/d0bm00827c
Hao Su ₁ , Yonggang Cui , Feihu Wang , Weijie Zhang , Chunli Zhang , Rongfu Wang , Honggang Cui

Affiliation

Therapeutic constructs with imaging modalities hold great promise for improving the treatment efficacy for cancer and many other diseases. We report here the design and synthesis of a self-assembling prodrug (SAPD) by the direct linkage of camptothecin (CPT), an anticancer drug, to a metal-chelating agent, DOTA. We found that under physiological conditions the DOTA-conjugated CPT prodrug can self-assemble into tubular supramolecular polymers (SPs) with a length of several micrometers. Our studies also suggest that the resultant assemblies were stable in biological environments and exhibited a fast drug release rate in the presence of intracellular glutathione. Furthermore, the SAPD exhibited remarkable in vitro efficacy against various cancer cell lines and effectively inhibited the growth of tumor spheroids. We believe that the design and optimization of self-assembling theranostic conjugates could provide a robust yet simple platform for the development of new imaging-guided drug delivery systems.

中文翻译：

通过金属螯合前药的自组装形成的治疗型超分子聚合物。

具有成像方式的治疗构造具有改善癌症和许多其他疾病的治疗效果的巨大希望。我们在这里报告了喜树碱（CPT）（一种抗癌药）与金属螯合剂（DOTA）的直接连接，从而设计和合成了自组装前药（SAPD）。我们发现在生理条件下，DOTA偶联的CPT前药可以自组装成长度为几微米的管状超分子聚合物（SP）。我们的研究还表明，所得的组装物在生物环境中是稳定的，并且在细胞内谷胱甘肽存在的情况下表现出快速的药物释放速率。此外，SAPD在体外表现出卓越的表现对抗各种癌细胞的功效，并有效抑制肿瘤球体的生长。我们相信，自组装治疗药物偶联物的设计和优化可以为开发新的影像引导药物递送系统提供一个强大而简单的平台。

更新日期：2020-07-13

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11