Oxidation-Responsive Micelles for Drug Release Monitoring and Bioimaging of Inflammation Based on FRET Effect in vitro and in vivo

Purpose: A new approach to monitor drug release and image inflammatory reactions in vitro and in vivo based on FRET mechanism was reported. Methods: In this study, mixed micelles containing a synthesized fluorescent donor DAN-PPS-mPEG and its quencher DAB-PPS-mPEG were prepared. Their stabilities, self-assembling and oxidation-responsiveness towards oxidants were tested in vitro and in vivo. Results: The conjugated polymers were synthesized and the morphological change and the fluorescent spectra of the prepared micellar system were measured. After incubating the DAN/DAB-PPS-mPEG mixed micelles with stimulated L929 fibroblast cells, the result of confocal laser microscopy showed fluorescence restoration of the micelles. Furthermore, an acute inflammatory injury mouse model was used to test the micelles in vivo. The micelles showed its ability to visualize the inflammatory site in the abdomen of the mice. Conclusion: The results confirmed that DAN/DAB-PPS-mPEG mixed micelles can respond to oxidants and release encapsulated cargos with corresponding fluorescence restoration, and visualize the inflammatory cells in vitro and inflammatory reactions in vivo.