All‐in‐One Heptamethine Cyanine Amphiphiles for Dual Imaging‐Guided Chemo‐Photodynamic‐Photothermal Therapy of Breast Cancer

Author:

Li Yu12,Zhang Jing3,Zhu Lijun4,Jiang Mou12,Ke Changsheng4,Long Hanxiong4,Lin Ruoyun4,Ye Chaohui125,Zhou Xin125,Jiang Zhong‐Xing126ORCID,Chen Shizhen125

Affiliation:

1. State Key Laboratory of Magnetic Resonance and Atomic and Molecular Physics National Center for Magnetic Resonance in Wuhan Wuhan Institute of Physics and Mathematics Innovation Academy for Precision Measurement Science and Technology Chinese Academy of Sciences‐Wuhan National Laboratory for Optoelectronics Wuhan 430071 China

2. University of Chinese Academy of Sciences Beijing 100049 China

3. School of Life Science and Engineering Lanzhou University of Technology Lanzhou 730050 China

4. School of Pharmaceutical Sciences Wuhan University Wuhan 430071 China

5. Optics Valley Laboratory Hubei 430074 China

6. Key Laboratory of Organofluorine Chemistry Shanghai Institute of Organic Chemistry Chinese Academy of Sciences Shanghai 200032 China

Abstract

AbstractDeveloping a theranostic system that integrates multimodal imaging, synergistic therapeutic, and formulation entities is a promising strategy for efficient cancer treatment. However, the complexity and safety concerns of multiple functional entities hinder their clinical translation. Herein, versatile “all‐in‐one” heptamethine cyanine amphiphiles (PEG‐Cy‐Fs) with multiple favorable capabilities, including fluorine‐19 magnetic resonance imaging (19F MRI), near‐infrared fluorescence imaging (NIR FLI), photodynamic therapy (PDT), photothermal therapy (PTT), polyethylene glycolation (PEGylation) and high biocompatibility, are developed for the convenient construction of theranostic platforms. Amphiphiles PEG‐Cy‐Fs are synthesized on a multi‐hundred‐milligram scale with high efficacy, which self‐assembled with a chemotherapy drug tamoxifen (TAM) into monodisperse and stable nanoparticles (SoFoTm/PEG‐Cy‐F18) with “turned on” FLI, sensitive 19F MRI, mitochondria‐targeting ability, high PDT and PTT efficacy, and PEGylation‐optimized pharmacokinetics. The selective accumulation of SoFoTm/PEG‐Cy‐F18 in xenograft MCF‐7 tumor with a long retention time (>10 days) enabled 19F MRI‐NIR FLI‐guided chemo–photodynamic–photothermal therapy (chemo‐PDT‐PTT) of breast cancer with high therapeutical index in mice. The “all‐in‐one” heptamethine cyanine amphiphile may facilitate the convenient and standardized preparation of high‐performance theranostics systems for clinical translation.

Funder

National Natural Science Foundation of China

Publisher

Wiley

Subject

Pharmaceutical Science,Biomedical Engineering,Biomaterials

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