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Published on: June 1, 2012
Chitosan microspheres with hydrocortisone and hydrocortisone-hydroxypropyl-beta-cyclodextrin inclusion complex
J Filipović-Grcić1, D Voinovich, M Moneghini
1Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovacica 1, 10000, Zagreb, Croatia. jelena.filipovic-grcic@fbf.tel.hr
This study developed a hydrocortisone acetate (HC) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion complex using spray-drying. The complex significantly enhanced HC dissolution rates from chitosan microspheres, showing great industrial potential.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Hydrocortisone acetate (HC) exhibits poor water solubility, limiting its therapeutic efficacy.
- Cyclodextrin complexation is a strategy to enhance the solubility and bioavailability of poorly soluble drugs.
Purpose of the Study:
- To prepare and characterize a hydrocortisone acetate-hydroxypropyl-beta-cyclodextrin (HC-HPbetaCD) inclusion complex.
- To formulate HC and its inclusion complex into chitosan microspheres using spray-drying.
- To evaluate the in vitro drug release and dissolution rate enhancement of HC from the microspheres.
Main Methods:
- Preparation of HC-HPbetaCD inclusion complex via spray-drying.
- Incorporation of HC and HC-HPbetaCD complex into chitosan microspheres by spray-drying.
- Characterization using X-ray powder diffractometry and differential scanning calorimetry (DSC).
- Assessment of particle size distribution, drug content, and in vitro drug release.
Main Results:
- The HC-HPbetaCD inclusion complex demonstrated improved water solubility compared to HC alone.
- Chitosan microspheres containing the HC-HPbetaCD complex exhibited significantly enhanced HC dissolution rates.
- Approximately 25-40% of HC was released within the first hour from microspheres, versus ~5% for pure HC.
- Drug release rate was inversely correlated with drug loading in microspheres.
Conclusions:
- Spray-drying is an effective and simple method for preparing HC-HPbetaCD inclusion complexes and chitosan microspheres.
- The developed formulation significantly improves the dissolution rate of hydrocortisone acetate.
- This approach holds considerable potential for industrial-scale production of enhanced drug delivery systems.
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