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Oral delivery of insulin using pH-responsive complexation gels.
A M Lowman1, M Morishita, M Kajita
1Biomaterials and Drug Delivery Laboratories, School of Chemical Engineering, Purdue University, West Lafayette, Indiana 47907, USA.
Journal of Pharmaceutical Sciences
|September 10, 1999
Summary
New pH-responsive hydrogels protect oral insulin from stomach acid, enabling effective glucose lowering in rats. This breakthrough offers a promising alternative to insulin injections.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Endocrinology
Background:
- Oral insulin delivery faces challenges due to proteolytic degradation in the gastrointestinal tract.
- Existing delivery methods often fail to protect insulin effectively, necessitating frequent injections.
- Developing stable oral insulin formulations is crucial for improving diabetes management.
Purpose of the Study:
- To investigate the efficacy of pH-responsive poly(methacrylic-g-ethylene glycol) hydrogels as oral insulin delivery vehicles.
- To assess the protective capabilities of these hydrogels against proteolytic degradation in the stomach.
- To evaluate the hypoglycemic effect and duration of orally administered insulin encapsulated in these hydrogels.
Main Methods:
- Insulin was loaded into pH-responsive poly(methacrylic-g-ethylene glycol) hydrogels.
- Polymeric microspheres containing insulin were orally administered to healthy and diabetic Wistar rats.
- The behavior of the hydrogels in different gastrointestinal pH environments was observed.
- Blood glucose levels and hypoglycemic effects were monitored over time.
Main Results:
- Hydrogels remained unswollen in the acidic stomach environment, protecting insulin from degradation.
- In the intestine, hydrogels swelled in neutral/basic pH, releasing insulin effectively.
- A strong, dose-dependent hypoglycemic effect was observed within 2 hours in both healthy and diabetic rats.
- The hypoglycemic effects persisted for up to 8 hours post-administration.
Conclusions:
- pH-responsive poly(methacrylic-g-ethylene glycol) hydrogels are effective vehicles for oral insulin delivery.
- These hydrogels successfully protect insulin from degradation and enable controlled release in the intestine.
- The study demonstrates a promising non-invasive approach for insulin delivery with significant therapeutic potential.