Drug-coated microneedles for rapid and painless local anesthesia

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• 作者：Sung-Hyun Baek ; Ju-Hyung Shin ; Yeu-Chun Kim
• 关键词：Transdermal drug delivery ; Coated ; microneedles ; Local anesthesia ; Lidocaine ; Poly (L ; lactide)
• 刊名：Biomedical Microdevices
• 出版年：2017
• 出版时间：March 2017
• 年：2017
• 卷：19
• 期：1
• 全文大小：
• 刊物类别：Engineering
• 刊物主题：Biomedical Engineering; Biological and Medical Physics, Biophysics; Nanotechnology; Engineering Fluid Dynamics;
• 出版者：Springer US
• ISSN：1572-8781
• 卷排序：19

文摘

This study showed that drug-coated PLLA (Poly (L-lactide)) microneedle arrays can induce rapid and painless local anesthesia. Microneedle arrays were fabricated using a micro-molding technique, and the needle tips were coated with 290.6 ± 45.9 μg of lidocaine, the most widely used local anesthetic worldwide. A dip-coating device was newly designed for the coating step using an optimized coating formulation. Lidocaine coated on the arrays was released rapidly into PBS within 2 min, and its stability in storage lasted 3 weeks at 4, 25, and 37°C. Furthermore, the microneedle arrays showed consistent in vitro skin penetration and delivered 200.8 ± 43.9, 224.2 ± 39.3, and 244.1 ± 19.6 μg of lidocaine into the skin 1, 2, and 5 min after application with a high delivery efficiency of 69, 77, and 84%. Compared to a commercially available topical anesthetic EMLA® cream, a 22.0, 13.6, and 14.0-fold higher amount of lidocaine was delivered into the skin. Note, in vitro skin permeation of Lidocaine was also notably enhanced by a 2-min-application of the lidocaine-coated microneedle arrays. Altogether, these results suggest that the biocompatible lidocaine-coated PLLA microneedle arrays could provide significantly rapid local anesthesia in a painless manner without any of the issues from topical applications or hypodermic injections of local anesthetics.