A Red Light Activatable Multifunctional Prodrug for Image-Guided Photodynamic Therapy and Cascaded Chemotherapy

作者：Liu, Li-Han; Qiu, Wen-Xiu; Bin Li; Zhang, Chi; Sun, Lin-Fei; Wan, Shuang-Shuang; Rong, Lei; Zhang, Xian-Zheng^*

来源：Advanced Functional Materials, 2016, 26(34): 6257-6269.

DOI：10.1002/adfm.201602541

• TARGETED CANCER-THERAPY
• SINGLET OXYGEN
• DRUG-DELIVERY
• RESPONSIVE PRODRUG
• CONTROLLED-RELEASE
• IN-VIVO
• GEMCITABINE
• NANOPARTICLES
• NANOPLATFORM
• POLYMER

A multifunctional prodrug, designated as TPP-L-GEM, is fabricated to realize image-guided in situ tumor photodynamic therapy (PDT) with red light activatable chemotherapy. Gemcitabine is conjugated with a fluorescent photosensitizer, meso-tetraphenylporphyrin (TPP), by a reactive oxygen species cleavable thioketal linker. Under the irradiation of low-energy red light, TPP can generate singlet oxygen and damage tumor cells by photodynamic therapy. Simultaneously, the thioketal linkage can be cleaved by singlet oxygen and result in a cascaded gemcitabine release, causing sustained cell damage by chemotherapy. With the combination of PDT and cascaded chemotherapy, TPP-L-GEM shows significant tumor therapeutic efficacy in vitro and in vivo. Furthermore, the inherent fluorescent property of TPP endows the TPP-L-GEM prodrug with noninvasive drug tracking capability, which is favorable for image-guided tumor therapy.

• 出版日期2016-9-13
• 单位武汉大学