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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Formulation and biological evaluation of glimepiride-cyclodextrin-polymer systems
H O Ammar1, H A Salama, M Ghorab
1Department of Pharmaceutical Technology, National Research Center, Dokki, Cairo, Egypt. husseinammar@hotmail.com
International Journal of Pharmaceutics
|December 27, 2005
Summary
This study enhanced glimepiride
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Glimepiride, a third-generation sulfonylurea, is used for type 2 diabetes.
- Poor aqueous solubility and dissolution rate of glimepiride can lead to therapeutic failure.
- Enhancing glimepiride's solubility and dissolution is crucial for reproducible clinical outcomes.
Purpose of the Study:
- To improve the biological performance of glimepiride by enhancing its solubility and dissolution rate.
- To prepare and characterize inclusion complexes of glimepiride with cyclodextrins and polymers.
- To evaluate the therapeutic efficacy of the optimized glimepiride formulation.
Main Methods:
- Preparation of glimepiride inclusion complexes using beta-cyclodextrin (beta-CyD), hydroxypropyl-beta-cyclodextrin (HP-beta-CyD), and sulfobutylether-beta-cyclodextrin (SBE-beta-CyD) via the kneading method.
- Characterization of binary systems using thermogravimetric analysis, IR spectroscopy, and X-ray diffractometry.
- Evaluation of phase solubility diagrams and dissolution efficiency of various ternary systems, including glimepiride-HP-beta-CyD-PEG 4000.
Main Results:
- Phase solubility studies indicated an increase in glimepiride solubility with cyclodextrin addition, showing A(p) type plots indicative of high-order complexation.
- Ternary systems containing beta-CyD or HP-beta-CyD demonstrated significantly higher dissolution efficiency compared to binary systems.
- The glimepiride-HP-beta-CyD-PEG 4000 ternary system exhibited the most rapid dissolution and significantly improved the hypoglycemic effect in diabetic rats.
Conclusions:
- The association of water-soluble polymers with glimepiride-cyclodextrin systems greatly enhances dissolution rate.
- The optimized ternary system leads to an increased duration of action and improved therapeutic efficacy of glimepiride.
- This approach offers a promising strategy for overcoming the bioavailability challenges of poorly soluble drugs like glimepiride.
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