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Comparative study of ibuproxam complexation with amorphous beta-cyclodextrin derivatives in solution and in the solid
Paola Mura1, Naima Zerrouk, M Faucci
1Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia, Università di Firenze, Florence, Italy. mura@farmfi.scifarth.unifi.it
Summary
Beta-cyclodextrin derivatives enhanced the solubility and dissolution of the anti-inflammatory drug ibuproxam. Despite reduced complexation, their amorphizing properties improved drug release from solid systems, with colyophilized forms being most effective.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Poor water solubility of anti-inflammatory agents like ibuproxam limits bioavailability.
- Beta-cyclodextrins (betaCd) are known excipients for improving drug solubility and dissolution.
- Randomly substituted amorphous beta-cyclodextrin derivatives offer potential for enhanced drug delivery.
Purpose of the Study:
- To investigate the complexing, solubilizing, and amorphizing abilities of beta-cyclodextrin derivatives towards ibuproxam.
- To compare the performance of methyl- (MebetaCd), hydroxyethyl- (HEbetaCd), and hydroxypropyl- (HPbetaCd) beta-cyclodextrins with parent beta-cyclodextrin.
- To evaluate the dissolution behavior of solid binary systems prepared by various methods.
Main Methods:
- Preparation of equimolar drug-cyclodextrin solid systems via blending, cogrinding, coevaporation, and colyophilization.
- Phase solubility analysis for liquid state interactions.
- Differential scanning calorimetry (DSC), X-ray powder diffractometry, Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM) for solid-state characterization.
- Dissolution efficiency evaluation using the dispersed amount method.
Main Results:
- All betaCd derivatives exhibited superior solubilizing efficacy for ibuproxam compared to parent beta-cyclodextrin.
- A decrease in complexing ability was observed for derivatives, attributed to steric hindrance from substituents.
- Despite reduced complexation, solid systems showed improved dissolution, with colyophilized forms demonstrating the highest dissolution efficiencies.
- Dissolution efficiencies of coground and coevaporated systems were significantly higher than physical mixtures and pure drug.
Conclusions:
- Randomly substituted amorphous beta-cyclodextrin derivatives effectively enhance ibuproxam solubility and dissolution.
- The amorphizing properties of betaCd derivatives play a crucial role in improving drug release from solid systems.
- Colyophilization is the most effective method for preparing ibuproxam-betaCd systems with superior dissolution performance.