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Article

Dissolving Microneedles for Rapid and Painless Local Anesthesia

1
Department of Oral Physiology and Program in Neurobiology, School of Dentistry, Seoul National University, Seoul 08826, Korea
2
Dental Research Institute, Seoul National University, Seoul 08826, Korea
3
Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Korea
4
Department of Periodontology, Research Institute for Periodontal Regeneration, Yonsei University College of Dentistry, Seoul 03722, Korea
5
Juvic Biotech, Inc., No. 208, Digital-ro 272, Guro-gu, Seoul 08389, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2020, 12(4), 366; https://doi.org/10.3390/pharmaceutics12040366
Received: 14 March 2020 / Revised: 13 April 2020 / Accepted: 15 April 2020 / Published: 17 April 2020
(This article belongs to the Special Issue Advances in Microneedle-Based Drug Delivery Systems)
Microneedles are emerging drug delivery methods for painless treatment. The current study tested dissolving microneedles containing lidocaine (Li-DMN) for use in local anesthesia. An Li-DMN patch was fabricated by centrifugal lithography with carboxymethyl cellulose as a structural polymer and assessed for physical properties by optical microscopy and a fracture force analyzer. The biocompatibility was evaluated by a histology section in vitro and by ear thickness in vivo. The efficacy of the Li-DMN patch was assessed by electrophysiological recordings in primary cultured sensory neurons in vitro and a von Frey test on rats’ hind paws in vivo. The physical properties of the microneedle showed enough rigidity for transdermal penetration. The maximal capacity of lidocaine-HCl in the Li-DMN patch was 331.20 ± 6.30 µg. The cytotoxicity of the dissolving microneedle to neuronal cells was negligible under an effective dose of lidocaine for 18 h. Electrophysiological recordings verified the inhibitory effect of the voltage-gated sodium channel current by the Li-DMN patch in vitro. A skin reaction to the edema test and histologic analysis of the rats’ ears after application of the Li-DMN patch were negligible. Also, the application of the Li-DMN patch reduced the nocifensive behavior of the rats almost immediately. In conclusion, the dissolving microneedle patch with carboxymethyl cellulose is a promising candidate method for the painless delivery of lidocaine-HCl. View Full-Text
Keywords: dissolving microneedles; lidocaine; local anesthesia; centrifugal lithography; carboxymethyl cellulose dissolving microneedles; lidocaine; local anesthesia; centrifugal lithography; carboxymethyl cellulose
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MDPI and ACS Style

Lee, B.-M.; Lee, C.; Lahiji, S.F.; Jung, U.-W.; Chung, G.; Jung, H. Dissolving Microneedles for Rapid and Painless Local Anesthesia. Pharmaceutics 2020, 12, 366. https://doi.org/10.3390/pharmaceutics12040366

AMA Style

Lee B-M, Lee C, Lahiji SF, Jung U-W, Chung G, Jung H. Dissolving Microneedles for Rapid and Painless Local Anesthesia. Pharmaceutics. 2020; 12(4):366. https://doi.org/10.3390/pharmaceutics12040366

Chicago/Turabian Style

Lee, Byeong-Min, Chisong Lee, Shayan F. Lahiji, Ui-Won Jung, Gehoon Chung, and Hyungil Jung. 2020. "Dissolving Microneedles for Rapid and Painless Local Anesthesia" Pharmaceutics 12, no. 4: 366. https://doi.org/10.3390/pharmaceutics12040366

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