Volume 16, Issue 23 2001059
Full Paper

A Highly-Efficient Type I Photosensitizer with Robust Vascular-Disruption Activity for Hypoxic-and-Metastatic Tumor Specific Photodynamic Therapy

Dapeng Chen

Dapeng Chen

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

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Qing Yu

Qing Yu

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

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Xuan Huang

Xuan Huang

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

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Hanming Dai

Hanming Dai

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

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Tao Luo

Tao Luo

Department of Hepatobiliary Surgery, Guangxi Medical University Cancer Hospital, 71 Hedi Road, Nanning, 530021 P. R. China

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Jinjun Shao

Corresponding Author

Jinjun Shao

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

E-mail: [email protected], [email protected], [email protected]

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Peng Chen

Peng Chen

School of Chemical and Biomedical Engineering, Nanyang Technological University, 62 Nanyang Drive, Singapore, 637459 Singapore

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Jie Chen

Corresponding Author

Jie Chen

Department of Hepatobiliary Surgery, Guangxi Medical University Cancer Hospital, 71 Hedi Road, Nanning, 530021 P. R. China

E-mail: [email protected], [email protected], [email protected]

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Wei Huang

Wei Huang

Shaanxi Institute of Flexible Electronics (SIFE), Northwestern Polytechnical University (NPU), Xi'an, 710072 China

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Xiaochen Dong

Corresponding Author

Xiaochen Dong

Key Laboratory of Flexible Electronics (KLOFE) and Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211800 P. R. China

School of Chemistry and Materials Science, Nanjing University of Information Science and Technology, Nanjing, 210044 P. R. China

E-mail: [email protected], [email protected], [email protected]

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First published: 06 May 2020
Citations: 154

Abstract

Hypoxia severely impedes photodynamic therapy (PDT) efficiency. Worse still, considerable tumor metastasis will occur after PDT. Herein, an organic superoxide radical (O2∙−) nano-photogenerator as a highly effcient type I photosensitizer with robust vascular-disrupting efficiency to combat these thorny issues is designed. Boron difluoride dipyrromethene (BODIPY)-vadimezan conjugate (BDPVDA) is synthesized and enwrapped in electron-rich polymer-brushes methoxy-poly(ethylene glycol)-b-poly(2-(diisopropylamino) ethyl methacrylate) (mPEG- PPDA) to afford nanosized hydrophilic type I photosensitizer (PBV NPs). Owing to outstanding core–shell intermolecular electron transfer between BDPVDA and mPEG-PPDA, remarkable O2∙− can be produced by PBV NPs under near-infrared irradiation even in severe hypoxic environment (2% O2), thus to accomplish effective hypoxic-tumor elimination. Simultaneously, the efficient ester-bond hydrolysis of BDPVDA in the acidic tumor microenvironment allows vadimezan release from PBV NPs to disrupt vasculature, facilitating the shut-down of metastatic pathways. As a result, PBV NPs will not only be powerful in resolving the paradox between traditional type II PDT and hypoxia, but also successfully prevent tumor metastasis after type I PDT treatment (no secondary-tumors found in 70 days and 100% survival rate), enabling enhancement of existing hypoxic-and-metastatic tumor treatment.

Conflict of Interest

The authors declare no conflict of interest.

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