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Fabrication of lidocaine-loaded polymer dissolving microneedles for rapid and prolonged local anesthesia

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Abstract

There is an urgent need for research into effective interventions for pain management to improve patients’ life quality. Traditional needle and syringe injection were used to administer the local anesthesia. However, it causes various discomforts, ranging from brief stings to trypanophobia and denial of medical operations. In this study, a dissolving microneedles (MNs) system made of composite matrix materials of polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and sodium hyaluronate (HA) was successfully developed for the loading of lidocaine hydrochloride (LidH). The morphology, size and mechanical properties of the MNs were also investigated. After the insertion of MNs into the skin, the matrix at the tip of the MNs was swelled and dissolved by absorption of interstitial fluid, leading to a rapid release of loaded LidH from MNs’ tips. And the LidH in the back patching was diffused into deeper skin tissue through microchannels created by MNs insertion, forming a prolonged anesthesia effect. In addition, the back patching of MNs could be acted as a drug reservoir to form a prolonged local anesthesia effect. The results showed that LidH MNs provided a superior analgesia up to 8 h, exhibiting a rapid and long-lasting analgesic effects. Additionally, tissue sectioning and in vitro cytotoxicity tests indicated that the MNs patch we developed had a favorable biosafety profile.

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Data availability

The data cannot be made publicly available upon publication because no suitable repository exists for hosting data in this field of study. The data that support the findings of this study are available upon reasonable request from the author.

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Acknowledgements

This work was supported by the Huadong Medicine Joint Funds of the Zhejiang Provincial Natural Science Foundation of China (LHDMZ23H300003), National Natural Science Foundation of China (51873194), and Science and Technology Planning Project of Hangzhou Health Commission (20220919Y011), the General Program Foundation from the Science and Technology Bureau of Hangzhou City (20171226Y17), and the General Program Foundation from the Hangzhou City Health Bureau (A20210250).

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Authors and Affiliations

  1. School of Materials Science and Engineering, Zhejiang Sci-Tech University, Hangzhou, 310018, China

    Yanan Mao, Chao Zhong & Guohua Jiang

  2. International Scientific and Technological Cooperation Base of Intelligent Biomaterials and Functional Fibers of Zhejiang Province, Hangzhou, 310018, China

    Yanan Mao, Chao Zhong & Guohua Jiang

  3. Department of Colorectal Surgery, Hangzhou Third People’s Hospital, Hangzhou, 310009, China

    Xiufeng Zhang & Zhong Shen

  4. College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou, 310018, China

    Yanfang Sun

  5. College of Life Sciences, Xinyang Normal University, Xinyang, 464000, China

    Lei Nie

  6. Université libre de Bruxelles (ULB), École polytechnique de Bruxelles, 3BIO-BioMatter, Avenue F.D. Roosevelt, 50 - CP 165/61, Brussels, 1050, Belgium

    Amin Shavandi

  7. Institute of Polymer Chemistry and Physics, Uzbekistan Academy of Sciences, Tashkent, 100128, Uzbekistan

    Khaydar E. Yunusov

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  1. Yanan Mao
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Contributions

Y. M. and C. Z.: prepared MNs and operated experiments. Y. M. and G. J.: analyzed results and wrote the manuscript. G. J. and Y. S.: designed the project and guided the work and founded the research. Z. S. and X. Z.: designed the animal experiment and discussed the results of animal experiment. L. N., A. S. and K. E. Y.: supported the suggestion and observed and reviewed on the manuscript.

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Correspondence to Guohua Jiang.

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Mao, Y., Zhang, X., Sun, Y. et al. Fabrication of lidocaine-loaded polymer dissolving microneedles for rapid and prolonged local anesthesia. Biomed Microdevices 26, 9 (2024). https://doi.org/10.1007/s10544-024-00695-1

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