Photocaged prodrug under NIR light-triggering with dual-channel fluorescence: in vivo real-time tracking for precise drug delivery  

作　　者：Zhiqian Guo Yaguang Ma Yajing Liu Chenxu Yan Ping Shi He Tian Wei-Hong Zhu 

机构地区：[1]Key Laboratory for Advanced Materials and Institute of Fine Chemicals, Shanghai Key Laboratory of Functional Materials Chemistry, School of Chemistry and Molecular Engineering, East China University of Science and Technology [2]State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology

出　　处：《Science China Chemistry》2018年第10期1293-1300,共8页中国科学（化学英文版）

基　　金：supported by The National Natural Science Foundation of China (21788102, 21421004, 21636002, 21622602);National Key Research and Development Program (2016YFA0200300);Scientific Committee of Shanghai (14ZR1409700, 15XD1501400);Fok Ying Tong Education Foundation (142014);Program of Introducing Talents of Discipline to Universities (B16017)

摘　　要：Light-triggered drug delivery system is an effective strategy for precise diagnosis and therapy in cancer treatment. However, it suffers from difficultly balancing the dosimetry of drug with light dose and a lack of in vivo models for validating their clinical benefits. Here we report an unprecedented near-infrared(NIR) light photocaged cyanine-based prodrug Cy-CPT-Biotin with dual-channel fluorescence mode, enabling NIR light to precisely regulate where, when and how the intact and active prodrugs are delivered. The synergy of photochemical reaction and modulation in π-conjugated polyene backbone of cyanine can fully perform distinct dual-channel fluorescence changes in a NIR light-mediated manner. The prodrug has striking characteristics of excellent tumor-targeting ability, real-time monitoring of the in vivo behaviors by dual-channel mode and NIR-light triggering,especially for achieving fine regulation and on-demand drug release in the precise dosimetry of drug with light dose in living animals. This optical orthogonality strategy that conjuncts with NIR light-triggered and dual-channel fluorescence in vivo imaging provides a powerful tool for in vivo real-time tracking and finely tuning the prodrug release for precise drug delivery.Light-triggered drug delivery system is an effective strategy for precise diagnosis and therapy in cancer treatment. However, it suffers from difficultly balancing the dosimetry of drug with light dose and a lack of in vivo models for validating their clinical benefits. Here we report an unprecedented near-infrared（NIR） light photocaged cyanine-based prodrug Cy-CPT-Biotin with dual-channel fluorescence mode, enabling NIR light to precisely regulate where, when and how the intact and active prodrugs are delivered. The synergy of photochemical reaction and modulation in π-conjugated polyene backbone of cyanine can fully perform distinct dual-channel fluorescence changes in a NIR light-mediated manner. The prodrug has striking characteristics of excellent tumor-targeting ability, real-time monitoring of the in vivo behaviors by dual-channel mode and NIR-light triggering,especially for achieving fine regulation and on-demand drug release in the precise dosimetry of drug with light dose in living animals. This optical orthogonality strategy that conjuncts with NIR light-triggered and dual-channel fluorescence in vivo imaging provides a powerful tool for in vivo real-time tracking and finely tuning the prodrug release for precise drug delivery.

关 键 词：near-infrared cyaninc dye dual-channel fluorescence DRUG-RELEASE photocage tumor targeting 

分 类 号：TQ460.1[化学工程—制药化工]