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Engineering Quick- and Long-acting Naloxone Delivery Systems for Treating Opioid Overdose.
Farrokh Sharifi1, Yazan J Meqbil2, Andrew Otte1
1Purdue University, Weldon School of Biomedical Engineering, West Lafayette, Indiana, 47907, USA.
Pharmaceutical Research
|June 11, 2021
Summary
This study developed long-acting naloxone microparticles to combat opioid overdose deaths. The novel poly(lactide-co-glycolide) delivery system effectively extended naloxone
Area of Science:
- Biomaterials Science
- Pharmacology
- Drug Delivery
Background:
- Opioids are a leading cause of overdose deaths in the United States.
- Current naloxone treatments provide only short-term opioid effect mitigation.
- There is a need for extended-release naloxone formulations as an opioid antidote.
Purpose of the Study:
- To develop and characterize naloxone-loaded poly(lactide-co-glycolide) (PLGA) microparticles for extended opioid antagonism.
- To create both quick- and long-acting naloxone delivery systems.
- To evaluate the efficacy of these microparticle systems in vitro.
Main Methods:
- Naloxone-PLGA microparticles were fabricated using an emulsification solvent extraction method.
- Polymer formulations varied in lactide:glycolide (L:G) ratios (50:50 and 75:25) and drug loading (21-51%).
- Microparticle sizes (23 μm and 50 μm) were controlled, and formulations were characterized for encapsulation efficiency, release profiles, and in vitro pharmacodynamics using β-arrestin recruitment assays.
Main Results:
- Encapsulation efficiency ranged from 70-85% and was optimized by increasing drug loading, using a 75:25 L:G ratio, and reducing particle size to 23 μm.
- In vitro release duration extended from 4 to 35 days.
- Smaller microparticles (23 μm) demonstrated a steady-state release profile, eliminating the initial lag phase.
Conclusions:
- Naloxone released from the developed microparticles effectively inhibited synthetic opioid peptide (DAMGO)-induced β-arrestin 2 recruitment.
- The PLGA microparticle system demonstrated adequate opioid reversal capabilities throughout the naloxone release duration.
- This formulation represents a promising advancement in extended-release naloxone delivery for opioid overdose management.
Keywords:
DAMGOPLGA microparticlesdrug loadingencapsulation efficiencynaloxoneopioid overdosezero-order releaseβ-arrestin 2 inhibitionMore Related Videos
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