Preparation and Evaluation of Alginate–Chitosan Microspheres loaded Hard Gelatin Capsule for Antidiabetic activity
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Abstract
Objective: This research focuses on the development and evaluation of sustained-release (SR) alginate–chitosan microspheres encapsulating glipizide, intended for oral administration via hard gelatin capsules to enhance diabetes management.
Methodology: Microspheres were synthesized using an ionic gelation approach. Aqueous solutions of sodium alginate and chitosan were gently stirred with glipizide, and the resulting mixture was extruded into a 5% calcium chloride solution to form microspheres. This method aimed to ensure controlled drug release and reduce the gastric irritation typically associated with single-unit glipizide formulations. Transitioning to a multi-unit dosage form allows the drug to be evenly distributed across the gastrointestinal tract, potentially minimizing irritation and enhancing absorption.
Results: The prepared microspheres exhibited particle sizes ranging from 200 to 500 µm. Among the formulations, GCS7 demonstrated the highest mucoadhesion at 89.3 ± 0.51% and a swelling index of 28.0%, while GCS6 achieved the highest drug entrapment efficiency at 90.2 ± 0.29%. In vitro drug release for formulations GCS1 and GCS2 ranged from 81% to 91%, indicating efficient sustained release. In vivo studies showed that formulation GCS3 achieved a 50–60% reduction in plasma glucose levels compared to standard formulations.
Conclusion: This study also explored various factors influencing the performance of microspheres in oral delivery systems. Sustained-release formulations are particularly useful for drugs like glipizide, which have a short half-life and are rapidly cleared from systemic circulation. By providing controlled drug release in the gastrointestinal tract, the developed microspheres help maintain more consistent plasma drug levels over an extended period.
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References
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