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Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans
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Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans
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Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans
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Journal Article
Diclofenac Enables Unprecedented Week-Long Microneedle-Enhanced Delivery of a Skin Impermeable Medication in Humans
2013
Overview
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,
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).
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.
Publisher
Springer US,Springer,Springer Nature B.V
Subject
/ Adult
/ Anti-Inflammatory Agents, Non-Steroidal - metabolism
/ Biological and medical sciences
/ Biomedical and Life Sciences
/ Biomedical Engineering and Bioengineering
/ Drug Delivery Systems - methods
/ Female
/ Humans
/ Male
/ Naltrexone - administration & dosage
/ Narcotic Antagonists - administration & dosage
/ Narcotic Antagonists - blood
/ Needles
/ Pharmacology. Drug treatments
/ Pharmacy
