Glutathione Activatable Photosensitizer-Conjugated Pseudopolyrotaxane Nanocarriers for Photodynamic Theranostics

Photodynamic theranostics has recently been extensively explored as a promising approach for precise localization and therapy. Herein, glutathione (GSH) activatable photosensitizer (PS)‐conjugated pseudopolyrotaxane nanocarriers (α‐CD‐ss‐Ce6 NPs) are reported for enhanced photodynamic theranostics by taking advantage of the noncovalent interactions between α‐cyclodextrin (α‐CD) and poly(ethylene glycol). The designed α‐CD‐ss‐Ce6 NPs are nonactivated and stable during circulation but exhibited strong photodynamic theranostics through GSH activating after arriving at tumor site. More importantly, compared to free chlorin e6 (Ce6), such kind of pseudopolyrotaxane nanocarrier can dramatically enhance Ce6 accumulation in tumor and prolong its tumor retention time, demonstrating excellent therapeutic effects after light irradiation. Overall, the designed GSH activatable PS‐conjugated pseudopolyrotaxane nanocarrier possessing high‐performance photodynamic therapeutic efficacy together with reduced side effects offers a promising alternative for photodynamic theranostics. A glutathione activatable chlorin e6 (Ce6)‐conjugated pseudopolyrotaxane nanocarrier for photodynamic theranostics is prepared through host–guest interaction. The designed nanocarrier is nonactivatable during circulation but becomes activated by glutathione activating after arriving at tumor site to induce cell death. Compared with free Ce6, this nanocarrier has excellent photodiagnostics capability without compromising the photodynamic therapy efficacy and is suitable for in vivo photodynamic theranostics.