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Development of Lidocaine-Coated Microneedle Product for Rapid, Safe, and Prolonged Local Analgesic Action

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ABSTRACT

Purpose

To demonstrate rapid (~1 min) lidocaine delivery using 3M’s solid microstructured transdermal system (sMTS) for prolonged, local analgesic action.

Methods

Polymeric microneedles were fabricated via injection molding and then dip-coated using an aqueous lidocaine formulation. The amount of lidocaine coated onto the microneedles was determined by high performance liquid chromatography (HPLC). To assess drug delivery and dermal pharmacokinetics, lidocaine-coated microneedles were inserted into domestic swine. Skin punch biopsies were collected and analyzed to determine lidocaine concentration in skin using HPLC-mass spectrometry (LC-MS). Commercial lidocaine/prilocaine EMLA (Eutectic Mixture of Local Anesthetic) cream was used as comparative control.

Results

Lidocaine dissolves rapidly off the microneedles and into skin such that the 1-min wear time achieves or exceeds lidocaine tissue levels needed to cause analgesia. This therapeutic threshold (100 ng/mg) was estimated by measuring the total amount of lidocaine and prilocaine in skin following a 1 h EMLA application. When co-formulated with 0.03 wt% vasoconstrictor-epinephrine, the concentration of lidocaine in tissue was maintained above 100 ng/mg for approximately 90 min.

Conclusions

3M’s sMTS can be used to provide rapid delivery of lidocaine for local analgesia up to 90 min.

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ACKNOWLEDGMENTS & DISCLOSURES

We would like to thank JoAnn Oesterich, Mary Hopp, Chris Webb and Tonya Grunwald for their assistance with the animal studies. The authors would also like to thank Daniel Duan, Jerry Gysbers, Peter Johnson and David Brandwein for valuable technical discussion. The authors thank Ryan Simmers and Ron Krienke for supplying microneedles.

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Authors and Affiliations

  1. 3M Drug Delivery Systems Division, St. Paul, Minnesota, 55144, USA

    Ying Zhang, Ken Brown, Kris Siebenaler, Amy Determan, Daniel Dohmeier & Kris Hansen

Authors
  1. Ying Zhang
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  2. Ken Brown
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  3. Kris Siebenaler
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  4. Amy Determan
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  5. Daniel Dohmeier
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  6. Kris Hansen
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Corresponding author

Correspondence to Kris Hansen.

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Zhang, Y., Brown, K., Siebenaler, K. et al. Development of Lidocaine-Coated Microneedle Product for Rapid, Safe, and Prolonged Local Analgesic Action. Pharm Res 29, 170–177 (2012). https://doi.org/10.1007/s11095-011-0524-4

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  • DOI: https://doi.org/10.1007/s11095-011-0524-4

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