In order to design a water soluble polymeric photosensitizer (WPS) with controllable photoactivity, a nano-photosensitizer (NPS) was prepared from a polyelectrolyte complex between polyethylene glycol-polyethylenimine-chlorine e6 conjugate (PEG-PEI-Ce6) and Black Hole Quencher-3 chondroitin sulfate conjugate (BHQ-3-CS). NPSs have a unimodal size distribution below 100 nm. Photoquenching of the NPS was dependent on the weight ratio of BHQ-3-CS/WPS. This phenomenon was maintained in a salt condition up to 300 mm, indicating that the photoactivity of the NPS disappears in the normal blood stream of the body. The quenched photoactivity was restored by the enzyme degradation of BHQ-3-CS after esterase treatment. In a HCT-116 (human colon cancer) cell test, the rapid cellular internalization of the NPS without any other ligands was observed by confocal imaging. Upon light irradiation after internalization, phototoxicity was detected via MTT colorimetric assay. Also, when the NPS was subcutaneously injected in both tumoral and normal regions of HCT-116 tumor-bearing mice, the fluorescence signal in the tumors rapidly increased compared to the normal region due to the enzymatic-triggered dissociation of the NPS in vivo. These results suggest that the NPS can provide both tumor diagnosis and therapy simultaneously, and has great potential for biological studies and clinical treatments of various tumors.
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