Tumor microenvironment(TME)-activatable probes have been proven to effectively increase signal-tobackground ratios(SBRs)and improve the success rate of complete tumor resection.However,many fluorescence probes have to...Tumor microenvironment(TME)-activatable probes have been proven to effectively increase signal-tobackground ratios(SBRs)and improve the success rate of complete tumor resection.However,many fluorescence probes have to be loaded into a nanocarrier for tumor targeted delivery,which consequently encounters poor drug loading,heterogeneous composition and non-encapsulated drug aggregates occurred during nanoformulation fabrications.Herein,a nitroreductase(NTR)-activated“OFF-ON”near-infrared fluorescence nanoprobe,named Nano Bodipy,was synthesized by the spontaneous self-assembling of NTRresponsive dye-polyethylene glycol(PEG)amphiphilic polymer in water.The NTR-responsive dye acted as the hydrophobic segment in the amphiphilic polymer,yielding a homogeneous composition and a high loading of 12.2 wt%(according to calculation)in the synthesized Nano Bodipy.The synthesized Nano Bodipy can efficiently accumulate in tumors via the enhanced permeability and retention(EPR)effect,enabling non-invasive tumor-targeted fluorescence imaging and guiding complete tumor resection.Once the synthesized Nano Bodipy entered the tumor cells,they dissociated and were activated by overexpressed NTR.With the real-time fluorescence guide of Nano Bodipy,complete tumor resection surgery was performed successfully.展开更多
基金supported by the National Natural Science Foundation of China(Nos.51903201,82172798)the Natural Science Foundation of Shaanxi Province(No.2023-YBSF-270)+1 种基金the Open Program of NHC Key Laboratory of Nuclear Medicine and Jiangsu Key Laboratory of Molecular Nuclear Medicine(No.KF202203)Horizontal Project of the First Affiliated Hospital of Xi'an Jiaotong University(No.202304174)。
文摘Tumor microenvironment(TME)-activatable probes have been proven to effectively increase signal-tobackground ratios(SBRs)and improve the success rate of complete tumor resection.However,many fluorescence probes have to be loaded into a nanocarrier for tumor targeted delivery,which consequently encounters poor drug loading,heterogeneous composition and non-encapsulated drug aggregates occurred during nanoformulation fabrications.Herein,a nitroreductase(NTR)-activated“OFF-ON”near-infrared fluorescence nanoprobe,named Nano Bodipy,was synthesized by the spontaneous self-assembling of NTRresponsive dye-polyethylene glycol(PEG)amphiphilic polymer in water.The NTR-responsive dye acted as the hydrophobic segment in the amphiphilic polymer,yielding a homogeneous composition and a high loading of 12.2 wt%(according to calculation)in the synthesized Nano Bodipy.The synthesized Nano Bodipy can efficiently accumulate in tumors via the enhanced permeability and retention(EPR)effect,enabling non-invasive tumor-targeted fluorescence imaging and guiding complete tumor resection.Once the synthesized Nano Bodipy entered the tumor cells,they dissociated and were activated by overexpressed NTR.With the real-time fluorescence guide of Nano Bodipy,complete tumor resection surgery was performed successfully.