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Integrating Pillar[5]arene and BODIPY for a Supramolecular Nanoplatform To Achieve Synergistic Photodynamic Therapy and Chemotherapy
Authors:Hui Quan  Yuying Huang  Jiacheng Xia  Jiawen Yang  Prof. Bing Lu  Prof. Peisheng Liu  Prof. Yong Yao
Affiliation:1. School of Science, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019 P. R. China

College of Chemistry and Chemical Engineering, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019 P. R. China;2. College of Chemistry and Chemical Engineering, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019 P. R. China;3. School of Science, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019 P. R. China

Abstract:BODIPY photosensitizers have been integrated with a hypoxia-activated prodrug to achieve synergistic photodynamic therapy (PDT) and chemotherapy. A novel BODIPY derivative BDP-CN was designed and synthesized. It had two cyano groups to make it complex well with a water-soluble pillar[5]arene. Their association constant was calculated to be (6.8±0.9)×106 M−1. After self-assembly in water, regular spherical nanocarriers can be formed; these were used to encapsulate the hypoxia-activated prodrug tirapazamine (TPZ). BDP-CN displayed excellent photodynamic activity to complete PDT. In this process, O2 can be continuously consumed to activate TPZ to allow it to be converted to a benzotriazinyl (BTZ) radical with high cytotoxicity to complete chemotherapy. As a result, the formed nanoparticles showed excellent synergistic photodynamic therapy and chemotherapy efficacy. The synergistic therapy mechanism is discussed in detail.
Keywords:BODIPY  chemotherapy  host–guest interactions  pillararenes  photodynamic therapy
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