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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MDPI AG
2020-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/12/4/366 |
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| author | Byeong-Min Lee Chisong Lee Shayan Fakhraei Lahiji Ui-Won Jung Gehoon Chung Hyungil Jung |
| author_facet | Byeong-Min Lee Chisong Lee Shayan Fakhraei Lahiji Ui-Won Jung Gehoon Chung Hyungil Jung |
| author_sort | Byeong-Min Lee |
| collection | DOAJ |
| 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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| format | Article |
| id | doaj.art-431e16c4dcc84430a89b1399eb61a243 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T20:25:00Z |
| publishDate | 2020-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-431e16c4dcc84430a89b1399eb61a2432023-11-19T21:52:48ZengMDPI AGPharmaceutics1999-49232020-04-0112436610.3390/pharmaceutics12040366Dissolving Microneedles for Rapid and Painless Local AnesthesiaByeong-Min Lee0Chisong Lee1Shayan Fakhraei Lahiji2Ui-Won Jung3Gehoon Chung4Hyungil Jung5Department of Oral Physiology and Program in Neurobiology, School of Dentistry, Seoul National University, Seoul 08826, KoreaDepartment of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, KoreaDepartment of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, KoreaDepartment of Periodontology, Research Institute for Periodontal Regeneration, Yonsei University College of Dentistry, Seoul 03722, KoreaDepartment of Oral Physiology and Program in Neurobiology, School of Dentistry, Seoul National University, Seoul 08826, KoreaDepartment of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, KoreaMicroneedles 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.https://www.mdpi.com/1999-4923/12/4/366dissolving microneedleslidocainelocal anesthesiacentrifugal lithographycarboxymethyl cellulose |
| spellingShingle | Byeong-Min Lee Chisong Lee Shayan Fakhraei Lahiji Ui-Won Jung Gehoon Chung Hyungil Jung Dissolving Microneedles for Rapid and Painless Local Anesthesia Pharmaceutics dissolving microneedles lidocaine local anesthesia centrifugal lithography carboxymethyl cellulose |
| 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 | dissolving microneedles lidocaine local anesthesia centrifugal lithography carboxymethyl cellulose |
| url | https://www.mdpi.com/1999-4923/12/4/366 |
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