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Effects of gold core size on regulating the performance of doxorubicin-conjugated gold nanoparticles

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Abstract

Studies on the influence of one critical parameter (e.g., size), targeting a specific disease, while keeping other factors unchanged, are important for improving understanding and application of the molecular design of biomedical nanomaterials. In this study, we used doxorubicin (Dox)-conjugated gold nanoparticles (GNPs) to investigate the effects of the size of the gold core (10, 20, or 60 nm) on the performance of their conjugates. We found that all three conjugates differed slightly in their physicochemical properties, facilitating a direct and accurate assessment of the size effects of GNP-Dox conjugates on their in vitro and in vivo performance. The cytological properties (the cell penetration rate and efficiency, as well as the cytotoxicity) and antitumor performance (the intratumoral penetration, treatment efficacy, and biodistribution) were highly correlated to the size of the inorganic core. Among all test groups, although the conjugate with a 60-nm gold core had the highest drug loading and release efficiency, the conjugate with a 10-nm gold core displayed the best antitumor efficacy toward the liver cancer models. This was because it showed the deepest tumor permeability and the highest tumor cell-killing ability of Dox transported by the relatively small GNPs. This study provides important evidence for better understanding the effect of size on in vitro and in vivo properties of potential therapeutic nanosystems and their structure design.

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Acknowledgements

This work was financially supported by the National Natural Science Foundation of China (Nos. 31470916, 31500769, 51672010, and 81421004), the Fundamental Research Funds for the Central Universities (Nos. 2015PT036 and 2016PT014), the Priority Academic Program Development of Jiangsu Higher Education Institutions, and the Open Project Program of MOE Key Laboratory of Drug Quality Control and Pharmacovigilance (No. DQCP2015MS01).

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  1. Dongyan Wu and Huaisong Wang contributed equally to this work.

Authors and Affiliations

  1. State Key Laboratory of Natural Medicines, Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, 210009, China

    Dongyan Wu, Huaisong Wang, Xiaoshuang Hou, Yu Ma & Ya Ding

  2. Department of Biochemistry, School of Life Science and Technology, China Pharmaceutical University, Nanjing, 210009, China

    Huan Chen

  3. Beijing Key Laboratory for Magnetoelectric Materials and Devices (BKLMMD), Beijing Innovation Center for Engineering Science and Advanced Technology (BIC-ESAT), Department of Materials Science and Engineering, College of Engineering, Peking University, Beijing, 100871, China

    Yanglong Hou

  4. Key Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing, 210009, China

    Jin Hong

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  1. Dongyan Wu
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Correspondence to Yanglong Hou or Ya Ding.

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Wu, D., Wang, H., Hou, X. et al. Effects of gold core size on regulating the performance of doxorubicin-conjugated gold nanoparticles. Nano Res. 11, 3396–3410 (2018). https://doi.org/10.1007/s12274-017-1963-y

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  • DOI: https://doi.org/10.1007/s12274-017-1963-y

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