Glutathione Triggered Near Infrared Fluorescence Imaging-Guided Chemotherapy by Cyanine Conjugated Polypeptide

Precise detection of the tumor environment for cancer diagnosis has been strongly demanded for further therapies. Here, a redox-responsive fluorescence switch off/on system PCQ was designed and synthesized conjugated with near-infrared (NIR) cyanine dyes (Cy5.5) and relevant quencher (FQ) in mixed polymeric micelles (PCy and PFQ). The mixed PCQ micelles were prepared with two kinds of polymers with poly(oligo (ethylene glycol) methacrylate) (POEGMA) as the hydrophilic shell, in which fluorescence emission was quenched by fluorescence resonance energy transfer (FRET) effect. The FQ was conjugated with POEGMA by disulfide linkage, which could be broken with a redox environment such as high glutathione (GSH) concentration in tumor cells. After the PCQ micelles got into tumor cells, PFQ blocks in PCQ would be disassembled to recompose PCy micelles. During that process, drugs like doxorubicin (DOX) could be loaded inside and formed PCQ@DOX nanoparticles and then released for accurate NIR bioimaging and drug delivery instantly.