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Purpose <p>This study aimed to develop a gastroretentive mucoadhesive multiparticulate system (GMMS) containing metformin hydrochloride (Met HCl) to prolong gastric residence and provide controlled drug release within a narrow absorption window. Mini-tablets were selected because they offer high drug loading and robust compression similar to tablets, but are distributed widely throughout the gastrointestinal tract, similar to pellets.</p> Methods <p>A three-level full factorial design was used to screen mucoadhesive polymers and identify significant factors influencing drug release and adhesion. A central composite design was used to optimize the levels of hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP). Mini-tablets were prepared by wet granulation and evaluated for their physical properties, mucoadhesive force, mucoadhesive strength using a texture analyzer, and dissolution behavior using 20 units (equivalent to 500&#xa0;mg of Met HCl) attached to the vessel wall to simulate gastric adhesion.</p> Results <p>Both dissolution behavior and mucoadhesive performance were primarily governed by the HPMC content, as higher levels formed a stronger hydrated gel that slowed drug diffusion and enhanced adhesive retention. Analysis of variance confirmed the statistically significant model terms without a lack of fit. The optimized formulation (40% HPMC, 4% PVP) released 53.3% of the drug in 30&#xa0;min and achieved 90% release at approximately 2&#xa0;h, exhibiting slower release than the conventional tablet. The mucoadhesion time exceeded 150&#xa0;min and the predicted responses agreed well with the experimental results.</p> Conclusion <p>The optimized GMMS demonstrated the potential to enhance metformin delivery by enabling gastric retention and controlled release. This approach can be extended to other drugs with narrow absorption windows.</p> Graphical Abstract <p></p>

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Design of Experiment (DoE) Approach to Develop a Gastroretentive and Mucoadhesive Multiparticulate System Containing Metformin HCl: An In Vitro Study Perspective

  • 期刊论文

  • 发表日期：

    2026年2月26日

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  • Ye-Eun Ko,
  • Dong-Wook Kim,
  • Jun-Bom Park,
  • Kwon-Yeon Weon

摘要

Purpose

This study aimed to develop a gastroretentive mucoadhesive multiparticulate system (GMMS) containing metformin hydrochloride (Met HCl) to prolong gastric residence and provide controlled drug release within a narrow absorption window. Mini-tablets were selected because they offer high drug loading and robust compression similar to tablets, but are distributed widely throughout the gastrointestinal tract, similar to pellets.

Methods

A three-level full factorial design was used to screen mucoadhesive polymers and identify significant factors influencing drug release and adhesion. A central composite design was used to optimize the levels of hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP). Mini-tablets were prepared by wet granulation and evaluated for their physical properties, mucoadhesive force, mucoadhesive strength using a texture analyzer, and dissolution behavior using 20 units (equivalent to 500 mg of Met HCl) attached to the vessel wall to simulate gastric adhesion.

Results

Both dissolution behavior and mucoadhesive performance were primarily governed by the HPMC content, as higher levels formed a stronger hydrated gel that slowed drug diffusion and enhanced adhesive retention. Analysis of variance confirmed the statistically significant model terms without a lack of fit. The optimized formulation (40% HPMC, 4% PVP) released 53.3% of the drug in 30 min and achieved 90% release at approximately 2 h, exhibiting slower release than the conventional tablet. The mucoadhesion time exceeded 150 min and the predicted responses agreed well with the experimental results.

Conclusion

The optimized GMMS demonstrated the potential to enhance metformin delivery by enabling gastric retention and controlled release. This approach can be extended to other drugs with narrow absorption windows.

Graphical Abstract