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Photo-Cross-Linkable Polymer Dots with Stable Sensitizer Loading and Amplified Singlet Oxygen Generation for Photodynamic Therapy

Tang, Ying, Chen, Haobin, Chang, Kaiwen, Liu, Zhihe, Wang, Yu, Qu, Songnan, Xu, Hong, Wu, Changfeng
ACS Applied Materials & Interfaces 2017 v.9 no.4 pp. 3419-3431
adenocarcinoma, chlorins, cytotoxicity, energy transfer, irradiation, leaching, mice, nanoparticles, neoplasm cells, photochemotherapy, photosensitizing agents, polymers, semiconductors, singlet oxygen, spectral analysis
Photodynamic therapy (PDT) is a promising treatment modality for clinical cancer therapy. However, the therapeutic effect of PDT is strongly dependent on the property of photosensitizer. Here, we developed photo-cross-linkable semiconductor polymer dots doped with photosensitizer Chlorin e6 (Ce6) to construct a nanoparticle platform for photodynamic therapy. Photoreactive oxetane groups were attached to the side chains of the semiconductor polymer. After photo-cross-linking reaction, the Ce6-doped Pdots formed an interpenetrated structure to prevent Ce6 leaching out from the Pdot matrix. Spectroscopic characterizations revealed an efficient energy transfer from the polymer to Ce6 molecules, resulting in amplified generation of singlet oxygen. We evaluated the cellular uptake, cytotoxicity, and photodynamic effect of the Pdots in gastric adenocarcinoma cells. In vitro photodynamic experiments indicated that the Ce6-doped Pdots (∼10 μg/mL) effectively killed the cancer cells under low dose of light irradiation (∼60 J/cm²). Furthermore, in vivo photodynamic experiments were carried out in tumor-bearing nude mice, which indicated that the Pdot photosensitizer apparently suppressed the growth of solid tumors. Our results demonstrate that the photo-cross-linkable Pdots doped with photosensitizer are promising for photodynamic cancer treatment.