Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans

Nicole Brogden; Stan Banks; Leslie Crofford; Audra Stinchcomb

doi:10.1007/s11095-013-1036-1

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Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans

Journal article

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Peer reviewed

Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans

Nicole Brogden, Stan Banks, Leslie Crofford and Audra Stinchcomb

Pharmaceutical research, Vol.30(8), pp.1947-1955

08/2013

DOI: 10.1007/s11095-013-1036-1

PMCID: PMC3773937

PMID: 23761054

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Abstract

Microneedles applied to the skin create micropores, allowing transdermal drug delivery of skin-impermeable compounds. The first human study with this technique demonstrated delivery of naltrexone (an opioid antagonist) for two to three days. Rapid micropore closure, however, blunts the delivery window. Application of diclofenac (an anti-inflammatory) allows seven days of naltrexone delivery in animals. The purpose of the current work was to demonstrate delivery of naltrexone for seven days following one microneedle treatment in humans.Human subjects were treated with microneedles, diclofenac (or placebo), and naltrexone. Impedance measurements were used as a surrogate marker to measure micropore formation, and plasma naltrexone concentrations were measured for seven days post-microneedle application.Impedance dropped significantly from baseline to post-microneedle treatment, confirming micropore formation. Naltrexone was detected for seven days in Group 1 (diclofenac + naltrexone, n = 6), vs. 72 h in Group 2 (placebo + naltrexone, n = 2). At study completion, a significant difference in impedance was observed between intact and microneedle-treated skin in Group 1 (confirming the presence of micropores).This is the first study demonstrating week-long drug delivery after one microneedle application, which would increase patient compliance and allow delivery of therapies for chronic diseases.

Biochemistry, general

Biomedical Engineering

microneedle

naltrexone

Biomedicine

transdermal

Pharmacy

Medical Law

Pharmacology/Toxicology

diclofenac

Details

Title: Subtitle: Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans
Creators: Nicole Brogden - Department of Pharmaceutical Sciences & Experimental Therapeutics The University of Iowa College of Pharmacy Iowa City Iowa USA
Stan Banks - AllTranz Inc., Lexington Kentucky USA
Leslie Crofford - Department of Internal Medicine University of Kentucky Lexington Kentucky USA
Audra Stinchcomb - Department of Pharmaceutical Sciences University of Maryland School of Pharmacy 20 N. Pine Street Baltimore Maryland USA
Resource Type: Journal article
Publication Details: Pharmaceutical research, Vol.30(8), pp.1947-1955
DOI: 10.1007/s11095-013-1036-1
PMID: 23761054
PMCID: PMC3773937
NLM abbreviation: Pharm Res
ISSN: 0724-8741
eISSN: 1573-904X
Publisher: Springer US; Boston
Language: English
Date published: 08/2013
Academic Unit: Dermatology; Pharmaceutical Sciences and Experimental Therapeutics; Physical Therapy and Rehabilitation Science
Record Identifier: 9984025417902771

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