Diclofenac delays micropore closure following microneedle treatment in human subjects.

Brogden NK, Milewski M, Ghosh P, Hardi L, Crofford LJ, Stinchcomb AL
J Control Release. 2012 163 (2): 220-9

PMID: 22929967 · PMCID: PMC3725617 · DOI:10.1016/j.jconrel.2012.08.015

Drugs absorbed poorly through the skin are commonly delivered via injection with a hypodermic needle, which is painful and increases the risk of transmitting infectious diseases. Microneedles (MNs) selectively and painlessly permeabilize the outermost skin layer, allowing otherwise skin-impermeable drugs to cross the skin through micron-sized pores and reach therapeutic concentrations. However, rapid healing of the micropores prevents further drug delivery, blunting the clinical utility of this unique transdermal technique. We present the first human study demonstrating that micropore lifetime can be extended following MN treatment. Subjects received one-time MN treatment and daily topical application of diclofenac sodium. Micropore closure was measured with impedance spectroscopy, and area under the admittance-time curve (AUC) was calculated. AUC was significantly higher at MN+diclofenac sodium sites vs. placebo, suggesting slower rates of micropore healing. Colorimetry measurements confirmed the absence of local erythema and irritation. This mechanistic human proof-of-concept study demonstrates that micropore lifetime can be prolonged with simple topical administration of a non-specific cyclooxygenase inhibitor, suggesting the involvement of subclinical inflammation in micropore healing. These results will allow for longer patch wear time with MN-enhanced delivery, thus increasing patient compliance and expanding the transdermal field to a wider variety of clinical conditions.

Copyright © 2012 Elsevier B.V. All rights reserved.

MeSH Terms (16)

Administration, Cutaneous Adult Anti-Inflammatory Agents, Non-Steroidal Cyclooxygenase Inhibitors Diclofenac Dielectric Spectroscopy Female Humans Male Microinjections Middle Aged Needles Porosity Skin Transdermal Patch Young Adult

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