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Two-Layer Sustained-Release Microneedles Encapsulating Exenatide for Type 2 Diabetes Treatment
Han Liu1,2, Suohui Zhang1,3, Zequan Zhou1,2
1Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry of Chinese Academy of Sciences, Beijing 100190, China.
Pharmaceutics
|June 24, 2022
Summary
New microneedle technology offers a convenient, sustained delivery of exenatide (EXT) for diabetes management. These two-layer sustained-release microneedles (TS-MNs) improve drug stability and patient compliance.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Endocrinology
Background:
- Daily injections of exenatide (EXT) for diabetes management pose challenges in patient compliance and convenience.
- Microneedle (MN) technology presents a promising alternative for improved drug administration.
Purpose of the Study:
- To fabricate and evaluate two-layer sustained-release microneedles (TS-MNs) for enhanced exenatide (EXT) delivery.
- To assess the stability, pharmacokinetics, bioavailability, and hypoglycemic efficacy of EXT-loaded TS-MNs.
Main Methods:
- Fabrication of TS-MNs using sodium alginate tips and a calcium alginate matrix encapsulating exenatide.
- In vitro drug release studies and mechanical strength assessment of the microneedles.
- In vivo pharmacokinetic and pharmacodynamic studies in animal models to evaluate sustained release and hypoglycemic effect.
Main Results:
- TS-MNs demonstrated adequate mechanical strength for skin penetration and sustained drug release for 48 hours.
- Exenatide (EXT) retained high activity after long-term storage, with high relative bioavailability (83.04%).
- A single administration of EXT-loaded TS-MNs provided a hypoglycemic effect lasting approximately 24 hours, with sustained efficacy over multiple administrations.
Conclusions:
- Two-layer sustained-release microneedles (TS-MNs) are a viable and promising depot for the sustained delivery of exenatide (EXT).
- This microneedle system enhances drug stability and offers a convenient, effective alternative to daily injections for diabetes management.
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