Enhanced Stability and Transdermal Delivery of Semaglutide Using an L-Arginine Based Dissolving Microneedle System
Priyanka Panchal1, Snehal Daware1, Yi Guo1
1College of Pharmacy and Health Sciences, St. Albert Hall, St. John's University, 8000 Utopia Parkway, Queens, New York, 11439, USA.
This study developed dissolving microneedles (DMNs) for transdermal delivery of Semaglutide (SMG), enhancing peptide stability with L-arginine. The DMNs show promising mechanical strength and drug release for improved diabetes and obesity management.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Engineering
- Drug Delivery Systems
Background:
- Glucagon-like peptide-1 agonists like Semaglutide (SMG) are effective for diabetes and obesity but face bioavailability and adherence issues.
- Injectable formulations limit patient compliance, necessitating alternative delivery methods.
- Transdermal delivery offers a patient-friendly approach to overcome these limitations.
Purpose of the Study:
- To develop and characterize dissolving microneedle (DMN) arrays for transdermal Semaglutide (SMG) delivery.
- To investigate the role of L-arginine as an excipient for enhancing SMG stability within DMNs.
- To evaluate the mechanical properties, insertion capabilities, and drug release profile of the developed SMG-DMNs.
Main Methods:
- Fabrication of DMN arrays using a blend of hyaluronic acid, PETOX, and L-arginine.
- Characterization of SMG-loaded microneedles (SMG-DMNs) including mechanical strength testing and Parafilm M® insertion.
- Assessment of drug release kinetics over 12 hours.
- Ex-vivo porcine skin insertion studies, SEM, confocal microscopy, and agarose dissolution modeling.
- Fluorescence imaging to verify transdermal deposition and penetration.
Main Results:
- SMG-DMNs demonstrated robust mechanical strength (3.47 N/needle) and effective insertion (>50% at 450 μm depth).
- Drug release was sustained over a 12-hour period.
- Characterization confirmed optimized polymeric matrix for SMG delivery and effective transdermal penetration.
- L-arginine incorporation showed potential for enhancing peptide integrity and stability.
Conclusions:
- Dissolving microneedle technology offers a promising, patient-friendly alternative for transdermal peptide delivery.
- The developed SMG-DMNs address limitations of oral bioavailability and injection discomfort.
- Further research is needed to address peptide stability challenges for improved T2DM and obesity management outcomes.
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