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Preparation and characterization of pioglitazone cyclodextrin inclusion complexes
1Department of Pharmaceutics, Al Ameen College of Pharmacy, Bangalore, India.
Journal of Young Pharmacists : JYP
|January 7, 2012
Summary
Pioglitazone
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Pioglitazone, a Biopharmaceutical Classification System class II drug, exhibits poor water solubility and slow dissolution.
- This can lead to subtherapeutic plasma drug levels and potential therapeutic failure.
Purpose of the Study:
- To enhance the water solubility and dissolution rate of pioglitazone using cyclodextrin complexation.
- To investigate the complexation capability of different cyclodextrins with pioglitazone.
Main Methods:
- Phase solubility studies were conducted with beta-cyclodextrin, methyl-beta-cyclodextrin, and gamma-cyclodextrin.
- Binary systems were prepared using kneading and spray-drying methods.
- Complexes were characterized using solubility studies, in vitro dissolution, FTIR, SEM, DSC, and XRPD.
Main Results:
- All cyclodextrins formed 1:1 stoichiometric inclusion complexes with pioglitazone.
- Complexation capability followed the order: methyl-beta > beta > gamma-cyclodextrin.
- Spray-dried methyl-beta-cyclodextrin complexes showed significantly higher solubility (2.29 mg/ml) compared to pure pioglitazone (0.0714 mg/ml).
Conclusions:
- Cyclodextrin complexation effectively improves pioglitazone's solubility and dissolution rate.
- Spray-dried methyl-beta-cyclodextrin complexes offer a promising approach for enhancing pioglitazone bioavailability.
- This strategy could overcome therapeutic failures associated with poorly soluble drugs.
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