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Effect of chitosan on progesterone release from hydroxypropyl-beta-cyclodextrin complexes.
T Cerchiara1, B Luppi, F Bigucci
1Department of Pharmaceutical Sciences, University of Bologna, via S. Donato 19/2, 40127, Bologna, Italy.
International Journal of Pharmaceutics
|May 20, 2003
Summary
This study developed a progesterone (Prog) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion complex, enhancing solubility and drug release. Chitosan incorporation further controlled the release of progesterone.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Progesterone (Prog) is a vital hormone with limited oral bioavailability due to poor water solubility.
- Cyclodextrins, particularly hydroxypropyl-beta-cyclodextrin (HPbetaCD), are widely used to improve the solubility and stability of poorly soluble drugs.
- Chitosan, a natural polymer, is recognized for its biocompatibility and potential in controlled drug release systems.
Purpose of the Study:
- To prepare and characterize an inclusion complex of progesterone with hydroxypropyl-beta-cyclodextrin.
- To investigate the effect of chitosan on the dissolution and release profile of the progesterone-HPbetaCD complex.
- To evaluate the thermodynamic parameters governing the inclusion complex formation.
Main Methods:
- Preparation of progesterone-HPbetaCD inclusion complexes using spray-drying and freeze-drying techniques.
- Incorporation of the inclusion complex into chitosan matrices via spray-drying and freeze-drying.
- Characterization using Infrared (IR) spectroscopy and Differential Scanning Calorimetry (DSC).
- Solubility studies using phase solubility diagrams and determination of stability constants at various temperatures (10, 25, 37°C) and pH 7.4.
Main Results:
- The progesterone-HPbetaCD inclusion complex exhibited significantly enhanced water solubility compared to progesterone alone.
- Phase solubility studies revealed complex formation, with stability constants determined at different temperatures.
- Drug release studies demonstrated a marked improvement in the dissolution rate of progesterone from the inclusion complex, with chitosan enabling controlled release.
Conclusions:
- The spray-drying and freeze-drying methods successfully produced progesterone-HPbetaCD inclusion complexes with improved solubility.
- The presence of chitosan effectively modulated the release kinetics, suggesting its utility in developing sustained-release progesterone formulations.
- The thermodynamic data provides insights into the mechanism of inclusion complex formation.