Fe^III-Doped Two-Dimensional C₃N₄ Nanofusiform: A New O₂-Evolving and Mitochondria-Targeting Photodynamic Agent for MRI and Enhanced Antitumor Therapy

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• 作者：Zhifang Ma ; Mengchao Zhang ; Xiaodan Jia ; Jing Bai ; Yudi Ruan ; Chao Wang ; Xuping Sun and Xiue Jiang
• 刊名：Small
• 出版年：2016
• 出版时间：October 19, 2016
• 年：2016
• 卷：12
• 期：39
• 页码：5477-5487
• 全文大小：2563K
• ISSN：1613-6829

文摘

Local hypoxia in tumors, as well as the short lifetime and limited action region of ¹O₂, are undesirable impediments for photodynamic therapy (PDT), leading to a greatly reduced effectiveness. To overcome these adversities, a mitochondria-targeting, H₂O₂-activatable, and O₂-evolving PDT nanoplatform is developed based on Fe^III-doped two-dimensional C₃N₄ nanofusiform for highly selective and efficient cancer treatment. The ultrahigh surface area of 2D nanosheets enhances the photosensitizer (PS) loading capacity and the doping of Fe^III leads to peroxidase mimetics with excellent catalytic performance towards H₂O₂ in cancer cells to generate O₂. As such tumor hypoxia can be overcome and the PDT efficacy is improved, whilst at the same time endowing the PDT theranostic agent with an effective T ₁-weighted in vivo magnetic resonance imaging (MRI) ability. Conjugation with a mitochondria-targeting agent could further increase the sensitivity of cancer cells to ¹O₂ by enhanced mitochondria dysfunction. In vitro and in vivo anticancer studies demonstrate an outstanding therapeutic effectiveness of the developed PDT agent, leading to almost complete destruction of mouse cervical tumor. This development offers an attractive theranostic agent for in vivo MRI and synergistic photodynamic therapy toward clinical applications.