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MPEG-phenylboronic acid modified doxorubicin as the efficient pathological pH-responsive nanoplatform for potential anti-cancer delivery

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Abstract

Chemotherapy is the main strategy for inhibiting the tumor growth. However, during the therapy, the side effect of anti-cancer drug will injure normal cells. For reducing the toxic of the free drug, stimuli responsive nanoparticles (NPs) have been prepared base on the pathological acidic environment around tumor for safe and efficient anti-tumor applications. In this study, we fabricated the phenylboronic acid (PBA) modified monomethoxy polyethylene glycol (MEPG) for encapsulating doxorubicin (DOX NPs). In the drug delivery system (DDS), the pH-responsive boric ester could be stable during drug delivery, and enhance DOX rapidly release in tumor lesion under the acidic stimuli. In vitro studies further demonstrated that DOX NPs could efficiently endocytose by tumor cells, and exhibit the similar anti-tumor activity as the free DOX resulting from the pH-responsive drug release profiles under tumor acidic stimuli. In summary, DOX NPs could be a feasible candidate to improve the safe and efficient DOX delivery for improving the potential anti-tumor applications.

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Acknowledgements

This work was supported by grants from the National Natural Science Foundation of China (31971301, 32171324), Natural Science Foundation of Chongqing (cstc2021jcyj-msxmX0149), and Fundamental Research Funds for Central Universities (2020CDJQY-A061, 2018CDHB1B08). In addition, some large instruments and equipment were provided by the Analysis and Testing Center of Chongqing University.

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  1. Jiyu Li and Li Zhu have contributed equally to this article.

Authors and Affiliations

  1. Key Laboratory for Biorheological Science and Technology of Ministry of Education, State and Local Joint Engineering Laboratory for Vascular Implants, Bioengineering College of Chongqing University, Chongqing, 400044, China

    Jiyu Li, Li Zhu, Shuai Wu, Guixue Wang, Yidan Chen & Wei Wu

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WW and JL did the conception and design of the work. LZ did the acquisition and analysis of the data. SW interpreted the data. JL and LZ drafted the manuscript. YC and GW substantively revised the manuscript. All authors read and approved the final manuscript.

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Correspondence to Yidan Chen or Wei Wu.

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Li, J., Zhu, L., Wu, S. et al. MPEG-phenylboronic acid modified doxorubicin as the efficient pathological pH-responsive nanoplatform for potential anti-cancer delivery. Macromol. Res. 31, 181–191 (2023). https://doi.org/10.1007/s13233-022-00106-5

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