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Drug-coated microneedles for rapid and painless local anesthesia

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Abstract

This study showed that drug-coated PLLA (Poly (L-lactide)) microneedle arrays can induce rapid and painless local anesthesia. Microneedle arrays were fabricated using a micro-molding technique, and the needle tips were coated with 290.6 ± 45.9 μg of lidocaine, the most widely used local anesthetic worldwide. A dip-coating device was newly designed for the coating step using an optimized coating formulation. Lidocaine coated on the arrays was released rapidly into PBS within 2 min, and its stability in storage lasted 3 weeks at 4, 25, and 37°C. Furthermore, the microneedle arrays showed consistent in vitro skin penetration and delivered 200.8 ± 43.9, 224.2 ± 39.3, and 244.1 ± 19.6 μg of lidocaine into the skin 1, 2, and 5 min after application with a high delivery efficiency of 69, 77, and 84%. Compared to a commercially available topical anesthetic EMLA® cream, a 22.0, 13.6, and 14.0-fold higher amount of lidocaine was delivered into the skin. Note, in vitro skin permeation of Lidocaine was also notably enhanced by a 2-min-application of the lidocaine-coated microneedle arrays. Altogether, these results suggest that the biocompatible lidocaine-coated PLLA microneedle arrays could provide significantly rapid local anesthesia in a painless manner without any of the issues from topical applications or hypodermic injections of local anesthetics.

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Acknowledgments

This work was supported financially by Ministry of Science, ICT, and Future Planning (Project No. NRF-2014M3A9E4064580) and grants of the Advanced Biomass R & D Center (ABC) of the Global Frontier Project funded by the Ministry of Science, ICT, and Future Planning (ABC-2011-0031350).

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Authors and Affiliations

  1. Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, Republic of Korea

    Sung-Hyun Baek, Ju-Hyung Shin & Yeu-Chun Kim

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  1. Sung-Hyun Baek
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  2. Ju-Hyung Shin
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  3. Yeu-Chun Kim
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Correspondence to Yeu-Chun Kim.

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Electronic supplementary material

Supplementary Figure 1

Schematic illustration of dip-coating device for 2D PLLA microneedle array. Pristine PLLA microneedle array attached on the plate which the array was hold on. As watched by microscope, the plate with the array was moved down and up to the reservoir in which coating solution was contained for dip-coating with lidocaine on the array. (DOCX 161 kb)

Supplementary Figure 2

The images of PLLA microneeldle array before dip-coating (a) and after dip-coating (b) by newly developed dip-coating device. The array was fictured and observed by USB microscopy (DOCX 794 kb)

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Baek, SH., Shin, JH. & Kim, YC. Drug-coated microneedles for rapid and painless local anesthesia. Biomed Microdevices 19, 2 (2017). https://doi.org/10.1007/s10544-016-0144-1

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