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用于肿瘤细胞内实时成像和 pH 触发 DOX 递药的基于 CD 的绝对“开-关”型荧光纳米诊疗一体化试剂。

Absolutely "off-on" fluorescent CD-based nanotheranostics for tumor intracellular real-time imaging and pH-triggered DOX delivery.

机构信息

State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China.

出版信息

J Mater Chem B. 2020 Sep 21;8(35):8002-8009. doi: 10.1039/d0tb01596b. Epub 2020 Aug 6.

DOI:10.1039/d0tb01596b
PMID:32761044
Abstract

Carbon dots (CDs) have attracted intense attention in tumor nanotheranostics recently; however, those nanotheranostics exhibited similar fluorescence in both normal and tumor tissues, limiting their practical application. In the present work, absolutely "off-on" fluorescent CD-based nanotheranostics was designed for tumor intracellular real-time imaging and pH-triggered DOX delivery via both static quenching by the crosslinking of benzaldehyde-containing diblock copolymers and dynamic quenching because of the surrounding conjugated DOX molecules. The proposed PPEGMA-b-PFPMA-(CDs)-DOX nanotheranostics did not exhibit fluorescence in a normal physiological medium, while strong fluorescence recovery occurred in the tumor intracellular microenvironment due to pH-triggered disintegration, releasing the CDs and DOX. The pH-triggered DOX release and absolute "off-on" fluorescence make the proposed nanotheranostics promising for tumor-specific pH-triggered DOX delivery and imaging.

摘要

碳点 (CDs) 最近在肿瘤纳米治疗学中引起了强烈的关注; 然而,这些纳米治疗剂在正常组织和肿瘤组织中表现出相似的荧光,限制了它们的实际应用。在本工作中,通过含苯甲醛的两亲嵌段共聚物的交联进行静态猝灭和由于周围共轭 DOX 分子的动态猝灭,设计了绝对“关-开”荧光 CD 基纳米治疗剂,用于肿瘤细胞内实时成像和 pH 触发的 DOX 递送。所提出的 PPEGMA-b-PFPMA-(CDs)-DOX 纳米治疗剂在正常生理介质中不显示荧光,而在肿瘤细胞内微环境中由于 pH 触发的崩解而发生强烈的荧光恢复,释放出 CDs 和 DOX。pH 触发的 DOX 释放和绝对“关-开”荧光使所提出的纳米治疗剂有望用于肿瘤特异性 pH 触发的 DOX 递送和成像。

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