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A novel sustained-release formulation of insulin with dramatic reduction in initial rapid release
Mitsuko Takenaga1, Yoko Yamaguchi, Aki Kitagawa
1Institute of Medical Science, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae-ku, 216-8512, Kawasaki, Japan. m2take@marianna-u.ac.jp
Summary
This study developed insulin-loaded poly(lactic-co-glycolic) acid microcapsules for controlled release. Adding glycerin significantly reduced initial insulin burst, enabling sustained therapeutic effects in hyperglycemic rats.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Diabetes mellitus requires precise insulin management.
- Current insulin therapies face challenges with controlled release.
- Biodegradable polymers offer potential for advanced drug delivery.
Purpose of the Study:
- To design and prepare insulin-loaded microcapsules for strictly controlled insulin release.
- To evaluate the impact of additives on microcapsule performance.
- To assess the in vivo efficacy of the developed microcapsules.
Main Methods:
- Insulin-loaded microcapsules were fabricated using poly(D,L-lactic-co-glycolic) acid (PLGA).
- Scanning electron microscopy was used for morphological characterization.
- Subcutaneous administration in streptozotocin-induced hyperglycemic rats assessed in vivo performance.
- Effect of additives (glycerin, ethanol, distilled water) on release profiles was investigated.
Main Results:
- Spherical PLGA microcapsules with diameters of 15-30 microm were successfully prepared.
- Subcutaneous injection of insulin-loaded microcapsules in rats demonstrated sustained plasma insulin levels and hypoglycemic effects.
- Incorporation of glycerin dramatically reduced the initial insulin burst compared to controls.
- Formulations with glycerin showed sustained insulin levels (36.2-140.7 microU/ml) from day 1 to day 9.
Conclusions:
- PLGA microcapsules provide a viable platform for controlled insulin delivery.
- Glycerin addition is a key formulation strategy to mitigate initial burst release.
- This approach holds promise for improving insulin therapy in diabetes management.