Diclofenac enables unprecedented week-long microneedle-enhanced delivery of a skin impermeable medication in humans.

Brogden NK, Banks SL, Crofford LJ, Stinchcomb AL
Pharm Res. 2013 30 (8): 1947-55

PMID: 23761054 · PMCID: PMC3773937 · DOI:10.1007/s11095-013-1036-1

PURPOSE - 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.

METHODS - 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.

RESULTS - Impedance dropped significantly from baseline to post-microneedle treatment, confirming micropore formation. Naltrexone was detected for seven days in Group 1 (diclofenac + naltrexone, nā€‰=ā€‰6), vs. 72 h in Group 2 (placebo + naltrexone, nā€‰=ā€‰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).

CONCLUSION - 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.

MeSH Terms (14)

Administration, Cutaneous Adult Anti-Inflammatory Agents, Non-Steroidal Diclofenac Drug Delivery Systems Female Humans Male Microinjections Naltrexone Narcotic Antagonists Needles Skin Absorption Young Adult

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