Aptamer-Conjugated Micelles for Targeted Photodynamic Therapy Via Photoinitiated Polymerization-Induced Self-Assembly

Here, we report photoinitiated polymerization-induced self-assembly (photo-PISA) mediated by Rose Bengal methacrylate (RBMA) to reproducibly construct nanoparticles in one pot, on a large scale, for photodynamic therapy (PDT). In this work, we take advantage of the multifunctionality of RBMA by applying the monomer as a photocatalyst for self-catalyzed PISA, a singlet oxygen (O-1(2)) generator for PDT, and a fluorophore for imaging. Covalent incorporation of Rose Bengal (RB) into nanostructures by the polymerizable methacrylate moiety permitted quantitative and controlled loading. When activated by visible light in aqueous solution, the RB within the cores of micelles yielded O-1(2) more efficiently than free RB. Post-PISA modification of the RB-loaded nanocarriers with a DNA aptamer enhanced internalization by HCT116 cells and significantly inhibited tumor cell proliferation when exposed to yellow light. Such aptamer-labeled nanoparticles, prepared for PDT, extend the practical biomedical applications of PISA and are potential candidates for clinical cancer treatment.

Automated summary

This study introduces a photoinitiated polymerization-induced self-assembly method mediated by Rose Bengal methacrylate for reproducibly constructing nanoparticles in large scale for photodynamic therapy. The multifunctionality of this method allows for covalent incorporation of Rose Bengal into nanostructures and enhancement of internalization by tumor cells through DNA aptamer modification. The aptamer-labeled nanoparticles prepared for PDT can potentially be used for clinical cancer treatment.