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Controlling the Size, Shape and Stability of Supramolecular Polymers in Water
Published on: August 2, 2012
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Supramolecular structure of glibenclamide and β-cyclodextrins complexes
David Lucio1, Juan Manuel Irache2, María Font3
1Department of Chemistry, Faculty of Sciences, University of Navarra, Irunlarrea s/n, Pamplona 31080, Navarra, Spain.
International Journal of Pharmaceutics
|August 7, 2017
Summary
Glibenclamide (GB) solubility and bioavailability were improved by forming inclusion complexes with cyclodextrins (CDs). Amorphous complexes significantly enhanced GB dissolution rates compared to crystalline forms.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Glibenclamide (GB), an antidiabetic drug, suffers from poor bioavailability due to low solubility.
- Cyclodextrins (CDs) are explored as complexing agents to enhance drug solubility and dissolution.
Purpose of the Study:
- To investigate the formation and characterization of Glibenclamide-beta-cyclodextrin (GB-βCD) inclusion complexes.
- To evaluate the impact of different preparation methods, CD derivatives, and ratios on complex structure and dissolution properties.
Main Methods:
- Complexation using various methods (freeze-drying, coevaporation, kneading).
- Characterization by molecular modeling, X-ray diffraction, and differential thermal analysis.
- Dissolution studies comparing inclusion complexes with pure GB.
Main Results:
- Dimeric inclusion complexes formed with varying CD orientations depending on the derivative (βCD, HPβCD, RMβCD).
- Amorphous complexes achieved via freeze-drying or ammonia-water coevaporation showed significantly increased GB dissolution.
- Crystalline complexes formed by kneading or ethanol/water coevaporation exhibited slower GB release, influenced by structural arrangement (cage vs. channel) and porosity.
Conclusions:
- Amorphous GB-βCD inclusion complexes effectively enhance Glibenclamide dissolution and release rates.
- The preparation method and resulting solid-state structure (amorphous vs. crystalline) critically influence the dissolution performance of Glibenclamide-cyclodextrin complexes.
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