“A~A+B ₃ ~” strategy to construct redox-responsive core-crosslinked copolymers as potential drug carrier

Redox-responsive core-crosslinked copolymers were synthesized based on poly(ε-caprolactone) (PCL) and poly(ethylene glycol) (PEG) via “A~A + B ₃ ~” strategy and Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. It is a feasible method for large-scale preparing redox-responsive core-crosslinked copolymers by crosslinking PCL-based disulfide bond-containing A-PCL-A macromonomers and PEG-based telechelic B ₃ ~ macromonomers. The core-crosslinked copolymers can form stable micelles through self-assembly in aqueous solution and exhibit reduction-cleavage responsibility in reductive medium. Further, their doxorubicin (DOX)-loaded micelles exhibit desirable reduction-triggered release performance in vitro. The cellular proliferation inhibition against A549 cells indicates their enhanced anticancer activity in comparison to free DOX. The redox-responsive core-crosslinked copolymers are expected to be used in smart delivery vehicles of anti-cancer drugs.