Related Experiment Videos
Cyclodextrins in acetazolamide eye drop formulations
H O Ammar1, S A El-Nahhas, R M Khalil
1Department of Pharmaceutical Sciences, National Research Centre, Dokki, Cairo, Egypt.
Die Pharmazie
|September 19, 1998
Summary
Acetazolamide complexation with cyclodextrins (CDs) enhances its solubility and permeation. This study shows CDs significantly improve acetazolamide
Area of Science:
- Pharmaceutical Sciences
- Physical Chemistry
- Drug Delivery
Background:
- Acetazolamide is a carbonic anhydrase inhibitor used to treat glaucoma and epilepsy.
- Cyclodextrins (CDs) are cyclic oligosaccharides known for their ability to form inclusion complexes with various drugs.
- Improving acetazolamide's solubility and bioavailability is crucial for effective therapeutic outcomes.
Purpose of the Study:
- To investigate the complexation of acetazolamide with different cyclodextrins (beta-CD, DM-beta-CD, TM-beta-CD).
- To evaluate the impact of cyclodextrins on acetazolamide's solubility, membrane permeation, and topical delivery.
- To assess the effect of cyclodextrins on acetazolamide's bioavailability and pharmacological performance in vivo.
Main Methods:
- Spectrophotometric analysis to monitor complex formation and determine binding constants.
- Solubility studies to quantify the increase in apparent solubility of acetazolamide with varying CD concentrations.
- In vitro permeation studies using semi-permeable membranes to assess drug penetration.
- In vivo studies in rabbits measuring intraocular pressure to evaluate bioavailability and pharmacological effects.
Main Results:
- Equimolar complexes of acetazolamide with beta-CD, DM-beta-CD, and TM-beta-CD were formed.
- Acetazolamide's apparent solubility in water increased linearly with cyclodextrin concentration.
- Optimal cyclodextrin concentrations were determined for maximum acetazolamide penetration.
- Cyclodextrin complexation significantly enhanced acetazolamide's intensity, bioavailability, and duration of action in rabbits.
Conclusions:
- Cyclodextrins effectively form inclusion complexes with acetazolamide, enhancing its aqueous solubility.
- Complexation with cyclodextrins improves acetazolamide's permeation and topical delivery characteristics.
- Cyclodextrin-mediated delivery of acetazolamide leads to augmented pharmacological effects and improved bioavailability, offering a promising strategy for drug formulation.