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Microneedles permit transdermal delivery of a skin-impermeant medication to humans

Daniel P. Wermeling, Stan L. Banks, David A. Hudson, Harvinder S. Gill, Jyoti Gupta, Mark R. Prausnitz, and Audra L. Stinchcomb
PNAS February 12, 2008 105 (6) 2058-2063; published ahead of print February 4, 2008 https://doi.org/10.1073/pnas.0710355105
Daniel P. Wermeling
Departments of *Pharmacy Practice and Science and
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  • For correspondence: dwermel@uky.edu
Stan L. Banks
‡Pharmaceutical Sciences, College of Pharmacy; and
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David A. Hudson
§Department of Psychiatry, College of Medicine, University of Kentucky, Lexington, KY 40536; and
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Harvinder S. Gill
¶Wallace H. Coulter Department of Biomedical Engineering and
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Jyoti Gupta
‖School of Chemical and Biomolecular Engineering, Georgia Institute of Technology, Atlanta, GA 30332
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Mark R. Prausnitz
¶Wallace H. Coulter Department of Biomedical Engineering and ‖School of Chemical and Biomolecular Engineering, Georgia Institute of Technology, Atlanta, GA 30332
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Audra L. Stinchcomb
‡Pharmaceutical Sciences, College of Pharmacy; and
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  1. Edited by Robert Langer, Massachusetts Institute of Technology, Cambridge, MA, and approved December 21, 2007 (received for review October 31, 2007)

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    Fig. 1.

    Mean (SD) NTX plasma concentrations for 72 h of patch application. (Inset) Early sampling points.

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    Fig. 2.

    Mean (SD) NTXOL plasma concentrations for 72 h of patch application. (Inset) Early sampling points.

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    Fig. 3.

    MN patch for TD delivery. (A) Image of a 50-MN patch resting on the tip of a human thumb. (B) Image of human skin after insertion of a 50-MN patch and staining with gentian violet, a dye that selective stained sites of skin perforation. (C) NTX TD patch and covering.

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    Table 1.

    NTX and NTXOL exposure after MN-enhanced TD delivery

    ParametersNTXNTXOL
    Css, ng/ml2.5 (1.0)0.6 (0.5)
    Tlag, h1.8 (1.1)1.4 (1.4)
    Cmax, ng/ml4.5 (2.4)1.9 (1.3)
    Tmax,h8.8 (7.6)37.5 (31.3)
    AUC0-t, ng·h/ml142.9 (43.9)39.7 (25.9)
    Clast, ng/ml1.8 (1.0)0.4 (0.6)
    • Results are expressed as means ± SD (in parentheses) for six MN-treated subjects. Css = concentration at steady-state condition; Tlag = time to reach steady-state condition; Cmax = maximum concentration achieved; Tmax = time to achieve maximum concentration; AUC0-t = area under the concentration-time curve from time 0 to 72 h; Clast = concentration at time of patch removal after 72 h of application.

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Microneedles permit transdermal delivery of a skin-impermeant medication to humans
Daniel P. Wermeling, Stan L. Banks, David A. Hudson, Harvinder S. Gill, Jyoti Gupta, Mark R. Prausnitz, Audra L. Stinchcomb
Proceedings of the National Academy of Sciences Feb 2008, 105 (6) 2058-2063; DOI: 10.1073/pnas.0710355105

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Microneedles permit transdermal delivery of a skin-impermeant medication to humans
Daniel P. Wermeling, Stan L. Banks, David A. Hudson, Harvinder S. Gill, Jyoti Gupta, Mark R. Prausnitz, Audra L. Stinchcomb
Proceedings of the National Academy of Sciences Feb 2008, 105 (6) 2058-2063; DOI: 10.1073/pnas.0710355105
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