Department of Biotechnology, Yonsei University, Seoul, Seodaemun-gu, Korea.
JUVIC Inc, Seoul, Guro-gu, Korea.
Expert Opin Drug Deliv. 2023 Jun;20(6):851-861. doi: 10.1080/17425247.2023.2216450. Epub 2023 May 30.
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.
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.
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.
A novel and safe oral Li-DMNs have potential applications in large animals and clinical trials and would possibly enter the anesthesia market.
利多卡因已被广泛用作一种短效局部麻醉剂，以减轻针插入引起的疼痛。溶解微针（DMN）是微创的，可以通过克服口腔黏膜屏障和缓解患者不适来有效递药。
通过离心光刻法，将利多卡因盐酸盐和透明质酸混合制成利多卡因溶液，用于制备口腔盐酸利多卡因包封 DMN（口腔 Li-DMN）。在猪颌骨中评估口腔 Li-DMN 进入口腔黏膜的溶解、渗透能力和局部黏膜药物传递。使用兔进行药代动力学分析和安全性评估。
口腔 Li-DMN 的插入深度符合安全标准。口腔 Li-DMN 在应用 3 分钟后完全溶解。局部黏膜药物传递、药代动力学和安全性评估表明，口腔 Li-DMN 可以以较低的剂量获得局部麻醉效果，并且在兔中没有口腔黏膜刺激。
新型安全的口腔 Li-DMN 具有在大动物和临床试验中的潜在应用，并可能进入麻醉市场。
