Lidocaine-loaded dissolving microneedle for safe local anesthesia on oral mucosa for dental procedure.

IF 5 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Hyunkyu Lee, Hye Su Min, Mingyu Jang, Geonwoo Kang, Seongdae Gong, Chisong Lee, Young Woo Song, Ui-Won Jung, Somin Lee, Hyeon Yeol Ryu, Huisuk Yang, Hyungil Jung
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引用次数: 2

Abstract

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.
载利多卡因溶解微针用于口腔黏膜安全局部麻醉。
背景:利多卡因作为一种短效局麻药已被广泛用于减轻针刺引起的疼痛。溶解微针(DMNs)具有微创性,可以克服口腔黏膜屏障,有效给药,减轻患者不适。方法:采用利多卡因-盐酸与透明质酸混合制备利多卡因溶液,离心光刻法制备口服利多卡因-盐酸包封DMNs(口服Li-DMNs)。研究了口服Li-DMNs在猪口腔黏膜的溶出度、渗透能力和局部经黏膜给药性能。用家兔进行药代动力学分析和安全性评价。结果:口腔Li-DMNs的插入深度满足安全标准。口服Li-DMNs在施用3min后完全溶解。局部经黏膜给药、药代动力学和安全性评价表明,口服Li-DMNs在较低剂量下可获得局部麻醉效果,且对家兔口腔粘膜无刺激作用。结论:一种新型、安全的口服Li-DMNs在大型动物和临床试验中具有潜在的应用前景,并有可能进入麻醉市场。
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来源期刊
CiteScore
11.10
自引率
3.00%
发文量
104
审稿时长
3 months
期刊介绍: Expert Opinion on Drug Delivery (ISSN 1742-5247 [print], 1744-7593 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles covering all aspects of drug delivery research, from initial concept to potential therapeutic application and final relevance in clinical use. Each article is structured to incorporate the author’s own expert opinion on the scope for future development.
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