ABSTRACT
Background
Lidocaine has been widely used as a short-acting local anesthetic agent to reduce the pain caused by needle insertion. Dissolving microneedles (DMNs), which are minimally invasive, can effectively deliver drugs by overcoming the oral mucosal barrier and relieving patient discomfort.
Methods
Lidocaine solution prepared by mixing lidocaine-HCl and hyaluronic acid was used to fabricate oral lidocaine HCl-encapsulated DMNs (oral Li-DMNs) via centrifugal lithography. The dissolution, penetration ability, and local transmucosal drug delivery of oral Li-DMNs into the oral mucosa were evaluated in porcine jaws. Pharmacokinetic analysis and safety assessment were performed using rabbits.
Results
The insertion depth of the oral Li-DMNs satisfies the safety standard. The oral Li-DMNs were completely dissolved after 3 min of application. The local transmucosal drug delivery, pharmacokinetic, and safety evaluations showed that the oral Li-DMNs can obtain a local anesthesia effect at a relatively lower dose, and there was no oral mucosal irritation in rabbits.
Conclusions
A novel and safe oral Li-DMNs have potential applications in large animals and clinical trials and would possibly enter the anesthesia market.
Acknowledgments
The authors would like to thank Editage (www.editage.co.kr) for editing and reviewing this manuscript for English language.
Declaration of interest
Hyungil Jung has submitted patents that have been or may be licensed to Juvic Inc. and is a founder/shareholder at Juvic Inc., developing microneedle-based products. These potential conflicts of interest have been disclosed and are being managed by Yonsei University. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
Author contributions
Hyunkyu Lee†: Conceptualization, Sample preparation, Formal analysis, Investigation, Writing−original draft, Writing−review & editing. Hye Su Min†: Sample preparation, Formal analysis, Investigation, Visualization, Writing−original draft, Writing−review & editing. Mingyu Jang: Conceptualization, Methodology, Software, Investigation. Geonwoo Kang: Conceptualization, Methodology, Software, Investigation. Seongdae Gong: Sample preparation, Investigation. Chisong Lee: Methodology, Software, Sample preparation, Investigation. Young Woo Song: Methodology, Investigation, Writing−review & editing. Ui-Won Jung: Conceptualization, Methodology, Software, Funding acquisition, Supervision. Somin Lee: Sample preparation, Investigation. Hyeon Yeol Ryu: Sample preparation, Investigation. Huisuk Yang*: Conceptualization, Methodology, Software, Funding acquisition, Supervision. Hyungil Jung*: Conceptualization, Methodology, Writing−review and editing, Funding acquisition, Supervision. All authors have read and agreed to the author contribution statements.
Reviewer disclosures
A reviewer on this manuscript has stated that have a financial interest in microneedle technology as a consultant, inventor and shareholder/founder of companies and this conflict of interest is managed by Georgia Institute of Technology. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.
Correction Statement
This article has been republished with minor changes. These changes do not impact the academic content of the article.