β-Cyclodextrin Inclusion Complexes of Budesonide with Enhanced Bioavailability for COPD Treatment

Abstract

Chronic obstructive pulmonary disease (COPD) is a life-threatening disease of the respiratory system, affecting many patients worldwide. Budesonide (BUD), a synthetic glucocorticosteroid applied for the treatment of COPD patients, is a hydrophobic compound with low bioavailability. The formation of inclusion complexes of hydrophobic compounds with β-cyclodextrin (CD) through the solvent evaporation technique is an appealing method for the amelioration of the compounds’ in vitro release behavior. In the present study, CD–BUD complexes were prepared through the solvent evaporation technique. The effect of the applied solvent was evaluated through FTIR, scanning electron microscopy (SEM), X-ray diffraction (XRD) analysis, and in vitro release behavior measurements. It was found that the optimum complexes with the minimum degree of crystallinity and the optimum in vitro release behavior are prepared in the solvent ratio H2O/EtOH 80/20 v/v. In a further step, the formation of CD–BUD complexes containing different amounts of BUD was prepared. Through XRD measurements, the degree of crystallinity of the samples was calculated confirming the diminished crystallinity of BUD in CD complexes. The in vitro release of the samples showed the improved release behavior of BUD from the complexes in comparison to neat BUD while a direct correlation between the degree of crystallinity and in vitro release behavior was demonstrated.

Novel 3D-Printed Dressings of Chitosan–Vanillin-Modified Chitosan Blends Loaded with Fluticasone Propionate for Treatment of Atopic Dermatitis

“…The solubility and dissolution rate are the most important factors [50]. According to a previous study of our group, higher crystallinity results in a lower dissolution rate [51]. Consequently, the loading of FLU should occur in its amorphous state.…”

“…Noteworthy is the fact that, by increasing the percentage of the FLU present in the patches, the in vitro release ability decreased. This inverted correlation between drug content and drug release behavior is typical for poorly water-soluble drugs and is attributed to the formation of hydrophobic interactions among the molecules of the drugs [51,58].…”

Preparation, Characterization and Molecular Dynamics Simulation of Rutin–Cyclodextrin Inclusion Complexes

“…The most widely used method to improve the water solubility of insoluble compounds is the cyclodextrin inclusion method [ 9 ]. Cyclodextrins have a cone-shaped structure with a cavity in the middle [ 10 ], as shown in Figure 1 b, and they possess the property of “hydrophobic inside and hydrophilic outside” [ 11 ].…”