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Amphiphilic polymer–drug conjugates based on acid-sensitive 100% hyperbranched polyacetals for cancer therapy

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Abstract

A new type of acid-sensitive 100% hyperbranched polyacetals (HBPA) was synthesized, which could be completely degraded into small molecules under acidic environment and avoid the accumulative toxicity in vivo. The AB2 monomer was synthesized by 4-carboxybenzaldehyde and 2-bromoethanol. The bulk polycondensation was carried out in vacuum environment to remove water byproduct. The massive terminal aldehyde groups of HBPA were conjugated with mPEG-NH2 and doxorubicins to form amphiphilic acid-sensitive polymer–drug conjugates (DOX-HBPA-PEG). The stability of the micelles of DOX-HBPA-PEG was evaluated by DLS at different pH value in phosphate buffer saline (PBS). The DOX release in vitro showed that the cumulative release rate was 14.51% in pH 7.4 PBS after 24 h and the cumulative release rate was 48.56% in pH 6.0 PBS after 24 h. The results of cell viability of DOX-HBPA-PEG and HBPA-PEG showed that the polymer–DOX conjugates were effective drug delivery systems. The uptake process of DOX-HBPA-PEG by A549 cells showed that the micelle was totally swallowed in 1 h later. The controllable drug release nature, stability, biocompatibility and completely degradable structures (acid-sensitive) make them to be promising drug delivery systems.

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Acknowledgements

The financial support from National Natural Science Foundation of China (21374089/81400765) is acknowledged.

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Authors and Affiliations

  1. MOE Key Laboratory of Space Applied Physics and Chemistry, Shaanxi Key Laboratory of Macromolecular Science and Technology, School of Science, Northwestern Polytechnical University, Xi’an, 710072, People’s Republic of China

    Xiao Duan, Mengsi Ma, Junjie Du, Shan Zhang, Heng Chen & Jie Kong

  2. PLA No. 323 Hospital, Xi’an, Shaanxi Province, 710054, People’s Republic of China

    Yalan Wu

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  1. Xiao Duan
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Correspondence to Jie Kong.

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Duan, X., Wu, Y., Ma, M. et al. Amphiphilic polymer–drug conjugates based on acid-sensitive 100% hyperbranched polyacetals for cancer therapy. J Mater Sci 52, 9430–9440 (2017). https://doi.org/10.1007/s10853-017-1135-1

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  • DOI: https://doi.org/10.1007/s10853-017-1135-1

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