Water-Soluble Nanoparticles with Twisted Double [7]Carbohelicene for Lysosome-Targeted Cancer Photodynamic Therapy.

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 (1 O2 ) 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.