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Aspirin microcrystals deposited on high-density microneedle tips for the preparation of soluble polymer microneedles

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Abstract

To reduce mucosal damage in the gastrointestinal tract caused by aspirin, aspirin microcrystals were loaded in soluble polymeric microneedle (MN) tips. Aspirin was prepared into aspirin microcrystals by jet milling. Aspirin microcrystals with particle sizes of 0.5–5 μm were loaded on MN tips with a height of 250 µm or 300 µm. The aspirin microcrystals suspended in a polymer solution were concentrated in the MN tips under negative pressure. The aspirin microcrystals had high stability in the MNs since they were not dissolved in solution during the fabrication process. The MN patch packaged in an aluminum-plastic bag containing silica gel desiccant can be stored at 4 °C. The MN tips implanted in the skin of Institute of Cancer Research (ICR) mice dissolved within 30 min. Isolated porcine ear skin was punctured by MNs with heights of 300 μm and 250 μm to depths of 130 μm and 90 μm, respectively. The fluorescent red (FR) release from MNs reached 98.59% within 24 h. The MNs delivered aspirin microcrystals to the epidermis and dermis, providing a smooth plasma concentration in rats. The MNs loaded with aspirin microcrystals did not evoke primary irritation on the dorsal skin of Japanese white rabbits. In summary, MNs loaded with aspirin microcrystals provide a new approach to improve the stability of aspirin in MN patches.

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Acknowledgements

The authors are grateful to the Antimicrobial Testing Center of the Technical Institute of Physics and Chemistry, CAS, for guiding us in conducting in vivo animal imaging.

Funding

This research was funded by the STS Project of the Chinese Academy of Sciences (grant number KFJ-STS-QYZD-182).

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Authors and Affiliations

  1. Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry of Chinese Academy of Sciences, Beijing, 100190, China

    Baorui Wang, Han Liu, Suohui Zhang, Aguo Cheng, Chenxin Yan, Bo Xu & Yunhua Gao

  2. School of Future Technology, University of Chinese Academy of Sciences, Beijing, 100049, China

    Baorui Wang, Bo Xu & Yunhua Gao

  3. Beijing CAS Microneedle Technology Ltd, Beijing, 102609, China

    Suohui Zhang & Yunhua Gao

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  1. Baorui Wang
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  2. Han Liu
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  3. Suohui Zhang
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  4. Aguo Cheng
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  5. Chenxin Yan
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  6. Bo Xu
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Contributions

The manuscript was written by Baorui Wang. Baorui Wang, Han Liu, Aguo Cheng, Chenxin Yan, and Bo Xu all contributed to the experiments. Suohui Zhang and Yunhua Gao supervised the project.

Corresponding author

Correspondence to Yunhua Gao.

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Ethics approval and consent to participate

All animal study protocols were approved by the Institutional Animal Care and Utilization Committee of the Technical Institute of Physics and Chemistry, CAS (approval numbers—IACUC-IPC-22045, IACUC-IPC-22053, and IACUC-IPC-22061; approval dates—25 June 2022, 16 August 2022, and 30 August 2022).

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Wang, B., Liu, H., Zhang, S. et al. Aspirin microcrystals deposited on high-density microneedle tips for the preparation of soluble polymer microneedles. Drug Deliv. and Transl. Res. 13, 2639–2652 (2023). https://doi.org/10.1007/s13346-023-01343-6

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