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Aim <p>The present study aimed to design, develop, and optimise a gastroretentive, floating microsphere-based drug delivery system for metformin hydrochloride and glyburide to demonstrate the feasibility of prolonged gastric retention and controlled drug release, thereby improving the management of Type 2 Diabetes Mellitus.</p> Methodology <p>Floating microspheres were prepared using the emulsion–solvent evaporation technique employing ethyl cellulose and Eudragit polymers. A Box–Behnken design was applied to optimise formulation variables, including drug ratio, polymer concentration, and stirring speed, with respect to particle size, entrapment efficiency, and drug release. The prepared microspheres were evaluated for particle size, surface morphology, drug entrapment efficiency, in vitro buoyancy, and drug release. Characterisation studies using FTIR, DSC, SEM, and UV–Vis spectrophotometry assessed drug compatibility, thermal behaviour, and morphology, with a focus on their influence on drug delivery performance.</p> Results <p>The optimised formulation (F-17) produced uniform spherical microspheres with an average particle size of 135.4&#xa0;μm, a high entrapment efficiency (89.1%), and a satisfactory drug loading (21.0%). FTIR and DSC studies confirmed the compatibility and stability of both drugs within the polymeric matrix, reassuring the system’s reliability for improved therapy.</p> Conclusion <p>The developed gastroretentive floating microspheres of metformin hydrochloride and glyburide successfully achieved prolonged gastric retention and sustained drug release, offering a promising approach to improve bioavailability, reduce dosing frequency, and enhance patient compliance in the management of Type 2 Diabetes Mellitus.</p> Graphical Abstract <p></p>

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Formulation, Optimization and Evaluation of Floating Microspheres of Glyburide and Metformin: A Novel Approach for Type 2 Diabetes Therapy

  • 期刊论文

  • 发表日期：

    2026年3月19日

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  • Deepak Khatkar,
  • Anupama Setia,
  • Mohit Chugh,
  • Chetan Sabharwal,
  • Diksha Jindal

摘要

Aim

The present study aimed to design, develop, and optimise a gastroretentive, floating microsphere-based drug delivery system for metformin hydrochloride and glyburide to demonstrate the feasibility of prolonged gastric retention and controlled drug release, thereby improving the management of Type 2 Diabetes Mellitus.

Methodology

Floating microspheres were prepared using the emulsion–solvent evaporation technique employing ethyl cellulose and Eudragit polymers. A Box–Behnken design was applied to optimise formulation variables, including drug ratio, polymer concentration, and stirring speed, with respect to particle size, entrapment efficiency, and drug release. The prepared microspheres were evaluated for particle size, surface morphology, drug entrapment efficiency, in vitro buoyancy, and drug release. Characterisation studies using FTIR, DSC, SEM, and UV–Vis spectrophotometry assessed drug compatibility, thermal behaviour, and morphology, with a focus on their influence on drug delivery performance.

Results

The optimised formulation (F-17) produced uniform spherical microspheres with an average particle size of 135.4 μm, a high entrapment efficiency (89.1%), and a satisfactory drug loading (21.0%). FTIR and DSC studies confirmed the compatibility and stability of both drugs within the polymeric matrix, reassuring the system’s reliability for improved therapy.

Conclusion

The developed gastroretentive floating microspheres of metformin hydrochloride and glyburide successfully achieved prolonged gastric retention and sustained drug release, offering a promising approach to improve bioavailability, reduce dosing frequency, and enhance patient compliance in the management of Type 2 Diabetes Mellitus.

Graphical Abstract