Glibenclamide is an oral hypoglycaemic drug which has limited water solubility, resulting in slow dissolution in the stomach and reduced absorption. This study aimed to enhance the dissolution rate of Glibenclamide using natural polymers, such as chitosan, and the excipient Neusilin to develop a free-flowing formulation. The formulations were prepared by encapsulating Glibenclamide in chitosan with different Neusilin ratios (1%, 2%, 3%, and 5%) and were designated C1N1, C1N2, C1N3, and C1N5, respectively. The flow properties, moisture content and particle size of the formulations were characterised along with their structural and thermal behaviour. Furthermore, drug content, in-vitro drug release, entrapment efficiency, and stability over two months have been assessed. All formulations showed improved dissolution rates and sustained-release effects. C1N5 showed the most significant effect on drug release and flow properties, suggesting that higher Neusilin concentrations can improve both dissolution rate and flowability. Overall, the chitosan-Neusilin combination enhances the dissolution of Glibenclamide, with a higher performance observed at higher Neusilin concentrations.

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Preparation & Characterisation of Free-Flowing Freeze-Dried Glibenclamide Microcapsules Using a Combination of Chitosan and Neusilin

  • Aida Qaisara Ahmad Azam,
  • Loh Yi Teng,
  • Mohamad Dayoob,
  • Appalaraju Velaga,
  • Ghazi Al Jabal,
  • Salah A. Alshehade,
  • Wan Hamirul Bahrin,
  • Azren Aida Asmawi,
  • Saifullizan Mohamad

摘要

Glibenclamide is an oral hypoglycaemic drug which has limited water solubility, resulting in slow dissolution in the stomach and reduced absorption. This study aimed to enhance the dissolution rate of Glibenclamide using natural polymers, such as chitosan, and the excipient Neusilin to develop a free-flowing formulation. The formulations were prepared by encapsulating Glibenclamide in chitosan with different Neusilin ratios (1%, 2%, 3%, and 5%) and were designated C1N1, C1N2, C1N3, and C1N5, respectively. The flow properties, moisture content and particle size of the formulations were characterised along with their structural and thermal behaviour. Furthermore, drug content, in-vitro drug release, entrapment efficiency, and stability over two months have been assessed. All formulations showed improved dissolution rates and sustained-release effects. C1N5 showed the most significant effect on drug release and flow properties, suggesting that higher Neusilin concentrations can improve both dissolution rate and flowability. Overall, the chitosan-Neusilin combination enhances the dissolution of Glibenclamide, with a higher performance observed at higher Neusilin concentrations.