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Dissolving Microneedles for Rapid and Painless Local Anesthesia

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 asses...

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Autores principales: Lee, Byeong-Min, Lee, Chisong, Lahiji, Shayan Fakhraei, Jung, Ui-Won, Chung, Gehoon, Jung, Hyungil
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7238259/
https://www.ncbi.nlm.nih.gov/pubmed/32316406
http://dx.doi.org/10.3390/pharmaceutics12040366
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author Lee, Byeong-Min
Lee, Chisong
Lahiji, Shayan Fakhraei
Jung, Ui-Won
Chung, Gehoon
Jung, Hyungil
author_facet Lee, Byeong-Min
Lee, Chisong
Lahiji, Shayan Fakhraei
Jung, Ui-Won
Chung, Gehoon
Jung, Hyungil
author_sort Lee, Byeong-Min
collection PubMed
description 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.
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spelling pubmed-72382592020-06-02 Dissolving Microneedles for Rapid and Painless Local Anesthesia Lee, Byeong-Min Lee, Chisong Lahiji, Shayan Fakhraei Jung, Ui-Won Chung, Gehoon Jung, Hyungil Pharmaceutics Article 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. MDPI 2020-04-17 /pmc/articles/PMC7238259/ /pubmed/32316406 http://dx.doi.org/10.3390/pharmaceutics12040366 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lee, Byeong-Min
Lee, Chisong
Lahiji, Shayan Fakhraei
Jung, Ui-Won
Chung, Gehoon
Jung, Hyungil
Dissolving Microneedles for Rapid and Painless Local Anesthesia
title Dissolving Microneedles for Rapid and Painless Local Anesthesia
title_full Dissolving Microneedles for Rapid and Painless Local Anesthesia
title_fullStr Dissolving Microneedles for Rapid and Painless Local Anesthesia
title_full_unstemmed Dissolving Microneedles for Rapid and Painless Local Anesthesia
title_short Dissolving Microneedles for Rapid and Painless Local Anesthesia
title_sort dissolving microneedles for rapid and painless local anesthesia
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7238259/
https://www.ncbi.nlm.nih.gov/pubmed/32316406
http://dx.doi.org/10.3390/pharmaceutics12040366
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