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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
Enhanced bioavailability of process-induced fast-dissolving ibuprofen cogranulated with beta-cyclodextrin
Mohamed K Ghorab1, Moji Christianah Adeyeye
1Graduate School of Pharmaceutical Sciences, Duquesne University, 441 Mellon Hall of Science, Pittsburgh, Pennsylvania 15282, USA.
Journal of Pharmaceutical Sciences
|July 29, 2003
Summary
Cogranulated ibuprofen (IBU) with beta-cyclodextrin (betaCD) significantly enhanced drug bioavailability compared to a physical mixture. Bile salts further increased IBU solubility, indicating their role in improved drug absorption.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Pharmacokinetics
Background:
- Improving the oral bioavailability of poorly soluble drugs like ibuprofen (IBU) is crucial for effective therapy.
- Beta-cyclodextrin (betaCD) is a common excipient used to enhance drug solubility and dissolution.
- The role of endogenous bile in drug absorption, particularly for complexed drugs, requires further investigation.
Purpose of the Study:
- To compare the bioavailability of cogranulated ibuprofen-beta-cyclodextrin granules versus a physical mixture.
- To investigate the impact of endogenous bile on the bioavailability of ibuprofen-beta-cyclodextrin granules.
- To elucidate the mechanisms behind enhanced ibuprofen bioavailability.
Main Methods:
- In vitro dissolution studies using USP type 2 apparatus.
- In vivo pharmacokinetic studies in bile duct-nonligated and bile duct-ligated rats administered with granules and physical mixtures.
- Phase solubility studies of ibuprofen in beta-cyclodextrin solutions with varying bile salt concentrations.
Main Results:
- Cogranulated ibuprofen-beta-cyclodextrin granules exhibited significantly faster dissolution and higher oral bioavailability (80.6%) compared to the physical mixture (53.1%).
- In bile duct-ligated rats, the bioavailability of the granules was substantially reduced, indicating the importance of bile.
- Phase solubility studies confirmed that bile salts enhance ibuprofen solubility and decrease the ibuprofen-betaCD complex stability constant.
Conclusions:
- Cogranulation with beta-cyclodextrin effectively enhances ibuprofen bioavailability through improved in-solution complex formation.
- Endogenous bile plays a critical role in the enhanced bioavailability of ibuprofen-beta-cyclodextrin formulations via micellar solubilization.
- These findings highlight the synergistic effect of formulation and physiological factors in optimizing drug absorption.
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