Abstract: | Helicene-based therapeutic agents for organelle-targeted photodynamic therapy (PDT) involving both type I and II are challenging and still underexplored. Herein, water-soluble nanoparticles containing twisted double 7]carbohelicene (D7H-NPs) are prepared through self-assembly with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(polyethylene glycol)-2000] by a nanoprecipitation method. D7H-NPs display high water solubility with an average size of 46 ± 2 nm. Notably, D7H-NPs can generate efficient singlet oxygen (1O2) and superoxide anion (O2· ?) upon white light irradiation, forming the basis of PDT. Moreover, the typical accumulation in lysosomes of 4T1 cancer cells paves the way to use D7H-NPs for lysosome-targeted cancer phototherapeutics. This paper reports a promising helicene-based phototherapeutic agent involving both type I and II PDT for organelle-targeted biotherapy. |