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A novel method for fabrication of coated microneedles with homogeneous and controllable drug dosage for transdermal drug delivery

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Abstract

Over the years, scientists have been focused on the development of microneedle coating process to coat a broad range of therapeutic agents onto the surface of the solid microneedles for effective drug delivery. The precise dose control, content uniformity as well as large-scale production of coated microneedles are still the core issues that have been the interest of researchers in this topic. To this end, a repeatable method that involved a micro-molding process was demonstrated for mass fabrication of coated microneedles with homogeneous and controllable drug loading under mild conditions. In this system, the dissolvable drug carriers with precise dosage were first mounted onto the solid microneedles and then exposed to the high moisture condition to finally obtain the coated microneedle with uniform and precise drug loading. Using the microneedle molds with the volume of 4.71 nL, 8.24 nL, 10.47 nL, and 12.56 nL per cavity, the drug loadings were precisely controlled at 4.8 ng, 6.4 ng, 9.3 ng, and 13.5 ng per needle, with the standard deviation of 0.09, 0.01, 0.07, and 0.53%, respectively. Mechanical property tests showed that the coated microneedles are strong enough for reliable skin insertion, and with in vivo trials in diabetic mice, we further confirmed the similar hypoglycaemic effect of insulin-coated microneedles to subcutaneous injection. Taken together, the micro-molding-based fabrication process has practical merits in the mass production of coated microneedles with homogeneous and controllable drug loading, facilitating the clinical translation of the microneedle technique.

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Data availability

The data are available from the corresponding author on reasonable request.

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Funding

This work was financially supported by the National Natural Science Foundation of China (51873015), the Joint Project of BRC-BC (Biomedical Translational Engineering Research Center of BUCT-CJFH) (XK2020-05, RZ2020-01), and the long-term subsidy mechanism from the Ministry of Finance and the Ministry of Education of PRC.

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Authors and Affiliations

  1. Beijing Laboratory of Biomedical Materials, College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, People’s Republic of China

    Bo Zhi Chen, Meng Chan He, Xiao Peng Zhang & Xin Dong Guo

  2. Department of Dermatology, China-Japan Friendship Hospital, East Street Cherry Park, Chaoyang District, Beijing, 100029, People’s Republic of China

    Wen Min Fei & Yong Cui

  3. Graduate School, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, 100730, China

    Wen Min Fei & Yong Cui

Authors
  1. Bo Zhi Chen
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  2. Meng Chan He
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  4. Wen Min Fei
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  5. Yong Cui
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  6. Xin Dong Guo
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Contributions

B.Z.C. and M.C.H. performed experimental measurements. B.Z.C. and M.C.H. drafted the paper. B.Z.C., X.P.Z and W.M.F. contributed to the data interpretation. Y. C. and X.D.G. directed the research and provided financial support.

Corresponding authors

Correspondence to Yong Cui or Xin Dong Guo.

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Ethics approval and consent to participate

The study was approved by the institutional animal care committee of China-Japan Friendship Hospital, and all procedures performed were in accordance with the ethical standards of our institution.

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Not applicable.

Conflict of interest

The authors declare no competing interests.

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Bo Zhi Chen and Meng Chan He contributed equally.

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Chen, B.Z., He, M.C., Zhang, X.P. et al. A novel method for fabrication of coated microneedles with homogeneous and controllable drug dosage for transdermal drug delivery. Drug Deliv. and Transl. Res. 12, 2730–2739 (2022). https://doi.org/10.1007/s13346-022-01123-8

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