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用于口腔黏膜局部麻醉的利多卡因负载透明质酸黏附微针贴剂

Lidocaine-Loaded Hyaluronic Acid Adhesive Microneedle Patch for Oral Mucosal Topical Anesthesia.

作者信息

Zhu Tingting, Yu Xixi, Yi Xin, Guo Xiaoli, Li Longhao, Hao Yuanping, Wang Wanchun

机构信息

School of Stomatology of Qingdao University, Qingdao 266003, China.

Qingdao Stomatological Hospital Affiliated to Qingdao University, Qingdao 266001, China.

出版信息

Pharmaceutics. 2022 Mar 22;14(4):686. doi: 10.3390/pharmaceutics14040686.

Abstract

The pain and fear caused by direct local injection of anesthetic or the poor experience with surface anesthetic cream increase the difficulty of clinical treatment for oral diseases. To address this problem, a hyaluronic acid microneedle patch (Li-HAMNs) that consists of fast-dissolving lidocaine hydrochloride (LDC)-loaded tips and a wet-adhesive backing layer made of polyvinyl alcohol (PVA)/carboxymethylcellulose sodium (CMC-Na) was fabricated to explore its potential use in dental topical anesthesia. Li-HAMNs could puncture the stratum corneum with an insertion depth of about 279 μm in the isolated porcine oral mucosal. The fast-dissolving tips could release LDC to improve the patients' convenience and compliance. Importantly, the backing layer, which has good adhesion ability and water-absorbing properties, could surmount the contraction and extension of oral masticatory muscles and the saliva scour. In the tail flick test, the topical anesthesia efficacy of the Li-HAMNs group was much better than clinical lidocaine cream (EMLA cream, LDC, 1.2 mg) in spite of a relatively lower LDC dose with Li-HAMNs (LDC, 0.5 mg). It is believed that the proposed adhesive microneedle patch could enhance transmucosal delivery of anesthetics and thus open a new chapter in the painless treatment of oral diseases.

摘要

局部直接注射麻醉剂所引起的疼痛和恐惧,或表面麻醉乳膏带来的不佳体验,增加了口腔疾病临床治疗的难度。为解决这一问题,制备了一种透明质酸微针贴片(Li-HAMNs),其由快速溶解的载有盐酸利多卡因(LDC)的尖端和由聚乙烯醇(PVA)/羧甲基纤维素钠(CMC-Na)制成的湿粘性背衬层组成,以探索其在牙科局部麻醉中的潜在用途。Li-HAMNs能够在离体猪口腔黏膜中穿刺角质层,插入深度约为279μm。快速溶解的尖端可释放LDC,提高患者的便利性和依从性。重要的是,具有良好粘附能力和吸水性能的背衬层能够克服口腔咀嚼肌的收缩和伸展以及唾液冲刷的影响。在甩尾试验中,尽管Li-HAMNs的LDC剂量相对较低(LDC,0.5mg),但其局部麻醉效果比临床利多卡因乳膏(EMLA乳膏,LDC,1.2mg)要好得多。据信,所提出的粘性微针贴片可增强麻醉剂的透粘膜递送,从而为口腔疾病的无痛治疗开启新篇章。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c724/9025765/9dea1bb8a090/pharmaceutics-14-00686-sch001.jpg

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