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Optimum formulation for sustained-release insulin
Mitsuko Takenaga1, Yoko Yamaguchi, Aki Kitagawa
1Institute of Medical Science, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae-ku, Kawasaki, Japan. m2take@marianna-u.ac.jp
International Journal of Pharmaceutics
|May 8, 2004
Summary
This study optimized sustained-release insulin formulations using poly(lactic-co-glycolic) acid (PLGA) microcapsules. Key findings include the importance of zinc addition, smaller insulin particle size, and specific microcapsule dimensions for effective, long-lasting insulin delivery.
Area of Science:
- Biomaterials Science
- Pharmaceutical Technology
- Drug Delivery Systems
Background:
- Developing effective sustained-release insulin formulations is crucial for diabetes management.
- Biodegradable polymers like poly(lactic-co-glycolic) acid (PLGA) offer potential for controlled drug delivery.
Purpose of the Study:
- To optimize a sustained-release insulin formulation using PLGA microcapsules.
- To investigate the impact of various formulation parameters on insulin release kinetics.
Main Methods:
- Preparation of PLGA microcapsules containing insulin with varying parameters.
- Subcutaneous administration of microcapsules to diabetic rats.
- Monitoring of plasma insulin levels to assess release profiles.
Main Results:
- Glycerin and water were suitable injectable formulation additives.
- Zinc compounds (six-fold molar excess ZnO) were essential to reduce rapid insulin release.
- Smaller insulin particle size and larger microcapsule size (approx. 30 microm) promoted sustained release.
- PLGA molecular weight around 6000 was optimal for in vivo release.
Conclusions:
- An optimal sustained-release insulin formulation was successfully prepared.
- Formulation parameters significantly influence insulin release, enabling controlled delivery.
- The developed formulation maintains insulin's biological activity.