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

Abstract

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.

Thioether-based poly(2-oxazoline)s: from optimized synthesis to advanced ROS-responsive nanomaterials

“…18 Invariably, these hydrophilic polymers contain oxidation-sensitive moieties, such as sulfides, diselenides, thioketals, aryl boronic esters, and thioethers. 19,20 Thioether-containing polymer systems have demonstrated potential in ROS-responsive applications due to the unique reactivity of sulfur to ROS. 21 Polymers incorporating thioether groups can be designed to be responsive to ROS, such as glutathione, by undergoing a hydrophobic-hydrophilic phase transition from thioethers with low dipole moments to a hydrophilic sulfoxide or sulfone in response to ROS, leading to an efficient disassembly of the materials.…”

“…18 Invariably, these hydrophilic polymers contain oxidation–sensitive moieties, such as sulfides, diselenides, thioketals, aryl boronic esters, and thioethers. 19,20…”