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Drug-coated microneedles for rapid and painless local anesthesia

Article

Abstract

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.

Keywords

Transdermal drug delivery Coated-microneedles Local anesthesia Lidocaine Poly (L-lactide) 

Notes

Acknowledgments

This work was supported financially by Ministry of Science, ICT, and Future Planning (Project No. NRF-2014M3A9E4064580) and grants of the Advanced Biomass R & D Center (ABC) of the Global Frontier Project funded by the Ministry of Science, ICT, and Future Planning (ABC-2011-0031350).

Compliance with ethical standards

Conflict of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Supplementary material

10544_2016_144_MOESM1_ESM.docx (161 kb)
Supplementary Figure 1 Schematic illustration of dip-coating device for 2D PLLA microneedle array. Pristine PLLA microneedle array attached on the plate which the array was hold on. As watched by microscope, the plate with the array was moved down and up to the reservoir in which coating solution was contained for dip-coating with lidocaine on the array. (DOCX 161 kb)
10544_2016_144_MOESM2_ESM.docx (794 kb)
Supplementary Figure 2 The images of PLLA microneeldle array before dip-coating (a) and after dip-coating (b) by newly developed dip-coating device. The array was fictured and observed by USB microscopy (DOCX 794 kb)

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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  1. 1.Department of Chemical and Biomolecular EngineeringKorea Advanced Institute of Science and Technology (KAIST)DaejeonRepublic of Korea

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