Construction of pH-responsive core crosslinked micelles via thiol-yne click reaction

Polycarbonate-based micelles possessed enormous potential for hydrophobic drug delivery. To improve micelle stability and prevent premature leakage during blood circulation, photo-induced thiol-yne click reaction was utilized to construct polycarbonate-based core crosslinked micelles (CCLMs), which avoided the use of toxic copper catalyst. The introduced beta-thiopropionate linkage in the core was demonstrated to endow the CCLMs with pH-responsiveness. The obtained CCLMs showed good dilution stability against DMF and water. Further MTT assays demonstrated excellent biocompatibility and low toxicity of the CCLMs in HeLa/MCF-7 cells. Moreover, DOX-encapsulated CCLMs showed good anticancer effects and excellent internalization efficiency in HeLa cells. The pH-responsive polycarbonate-based CCLMs by thiol-yne click reaction have potential used as smart delivery systems for controlled drug release.

Automated summary

Polycarbonate-based core crosslinked micelles (CCLMs) were constructed using photo-induced thiol-yne click reaction to improve stability and prevent premature leakage. The CCLMs exhibited pH-responsiveness and showed excellent biocompatibility and low toxicity in biological tests. DOX-encapsulated CCLMs demonstrated good anticancer effects and high internalization efficiency.