# Development of a heated transdermal microneedle naloxone patch as an innovative treatment for opioid overdose

> **NIH NIH R21** · UNIVERSITY OF IOWA · 2021 · $193,125

## Abstract

PROJECT SUMMARY/ABSTRACT
The opioid overdose epidemic is killing Americans at the level of a mass casualty event – Hurricane Katrina killed
1,577 people but the death toll from opioid overdose in 2018 in California alone was 5,348. Synthetic, more
potent opioids such as fentanyl and its derivatives are further increasing the numbers of deaths. Naloxone (NLX),
an opioid antagonist, is the antidote for opioid overdose. NLX works by displacing opioid molecules from
receptors in the body, ultimately reversing the respiratory depression. NLX is administered intravenously (IV),
intramuscularly (IM), subcutaneous (SC), or intranasally. Unfortunately all commercially available dosage forms
have significant shortcomings, making them challenging for pre-hospital settings. Most notably, NLX suffers from
a very short plasma half-life, presenting a risk of overdose relapse if there is a very large amount of opioid in the
plasma. This results in need for repeated NLX doses to be given (known as “rescue” doses) to prevent hypoxia,
and this disadvantage is shared by all routes of delivery and is becoming increasingly common. Additional
challenges include the need for use of needles/syringes with IV/IM/SC delivery, which is very risky in the context
of a potentially combative patient; intranasal delivery is not uniformly effective, and is contraindicated in the
context of intranasal damage that is often seen with use of other illicit substances. In this research we propose
to overcome the shortcomings of current NLX dosage forms through development of a novel self-heating
transdermal patch with microneedles. The long-term goal is to decrease pre-hospital opioid overdose deaths
through development of the novel transdermal NLX dosage form. The intent is to deliver NLX quickly through
the skin, aiming to achieve consistent and therapeutically relevant drug concentrations without need for rescue
doses. The central hypothesis of this proposal is that NLX will rapidly and continuously absorb through epidermal
micropores, and a positive correlation will exist between elevated skin temperature and the rate and extent of
NLX permeation. The patch will include 3 layers: 1) dissolving microneedles, 2) a transdermal NLX gel, and 3) a
heating layer. Each layer fulfills a specific function, with the combined effect of producing NLX skin permeation
that can reach plasma levels appropriate for treating opioid overdose. Dissolving NLX microneedles will
immediately start to deliver NLX as they dissolve, while also creating micropores to allow transdermal NLX
delivery from the gel. The gel will deliver NLX through the micropores for a minimum of 2 hrs after patch
application. The heating layer will rapidly generate heat upon air exposure, increasing skin temperature and
thereby increasing the rate and extent of NLX absorption. The patch is intended to be applied in just one step.
In Aim 1 we will optimize each patch layer in vitro to meet predetermined milestones to provide similar...

## Key facts

- **NIH application ID:** 10351624
- **Project number:** 1R21DA055115-01
- **Recipient organization:** UNIVERSITY OF IOWA
- **Principal Investigator:** Nicole K Brogden
- **Activity code:** R21 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $193,125
- **Award type:** 1
- **Project period:** 2021-09-30 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10351624

## Citation

> US National Institutes of Health, RePORTER application 10351624, Development of a heated transdermal microneedle naloxone patch as an innovative treatment for opioid overdose (1R21DA055115-01). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10351624. Licensed CC0.

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