Host-guest inclusion complex of desloratadine with 2- (hydroxy)propyl-β-cyclodextrin (HP-β-CD): Preparation, binding behaviors and dissolution properties

Abstract

Desloratadine (DSL) is an anti-allergic agent that diminishes nasal and non-nasal allergic marks of seasonal allergic rhinitis. However, its efficiency of DSL is restricted with its low dissolution rate and aqueous solubility. The influence of 2-(hydroxy)propyl-β-cyclodextrin (HP-β-CD) on the DSL solubility was evaluated in respect of the phase solubility method. Following the formulation of inclusion complexes of DSL and HP-β-CD with various strategies (freeze-drying, spray-drying and kneading) (FD, SD and KN), compounds were investigated to evaluate the possibility of altering the physicochemical properties (solubility, release, stability, morphology) of DSL after complexation that are critical for subsequent formulation studies including the complexes prepared. Changes in DSC thermograms, FT-IR spectra and NMR spectra confirmed the constitution of a DSL-HP-β-CD complexes. In vitro release from inclusion complexes was compared to pure DSL by dialysis method. It was found that solubility enhancements of DSL-HP-β-CD complexes relies on the sort of the formulation technique. Higher release of DSL from complexes compared to pure DSL was ascribed to the interactive relations between HP-β-CD and DSL, high energetic amorphous status and inclusion complex constitution.

Keywords

• Desloratadine; 2-(hydroxy)propyl-β-cyclodextrin
• inclusion complex
• phase solubility diagram
• in vitro dissolution
• improved solubility

References

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