Microneedle patch-based transnasal delivery of naloxone

Area of Science:

• Pharmacology
• Biomaterials Science
• Drug Delivery Systems

Background:

• Conventional naloxone (NAL) intranasal sprays require frequent redosing, especially for long-acting opioids.
• Transdermal NAL delivery faces limitations in efficacy and absorption rates.
• Opioid overdose treatment necessitates efficient and rapid NAL administration.

Purpose of the Study:

• To evaluate dissolving microneedle (MN) patches for transnasal naloxone (NAL) delivery.
• To compare the efficacy of MN patches with transdermal and conventional intranasal NAL delivery.
• To optimize MN patch design for sustained and efficient NAL permeation.

Main Methods:

• Fabrication and testing of polyvinylpyrrolidone (PVP) and PVP/Chitosan MN patches on porcine nasal mucosa.
• Quantification of cumulative NAL permeation over 1 and 24 hours for transnasal vs. transdermal delivery.
• Mathematical modeling to simulate drug dissolution, permeation dynamics, and plasma concentration kinetics.

Main Results:

• Transnasal MN patches demonstrated significantly higher 1-hour and 24-hour cumulative NAL permeation compared to transdermal application.
• PVP MN patches showed superior 1-hour permeation (7295.12 µg/cm²) over transdermal (103 µg/cm²).
• Sustained delivery was observed when drug was loaded in both MN tips and base, unlike tip-only loading.

Conclusions:

• Dissolving MN patches provide a viable, sustained transnasal delivery system for naloxone (NAL).
• This technology offers a promising alternative for efficient opioid overdose treatment, potentially reducing redosing frequency.
• Optimized MN patch design can achieve therapeutic plasma profiles comparable to existing administration routes.