Host-guest inclusion complex of desloratadine with 2-(hydroxy)propyl-?-cyclodextrin (HP-?-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.

Solid Dispersions of Gefitinib with D-α-Tocopherol Polyethylene Glycol-1000 Succinate and 2-Hydroxypropyl β-Cyclodextrin Complex Improved Their Solubility, Dissolution and Apoptosis against A549 Cells

“…The binary complex (GEF with TPGS) attributed their stretching vibration to the slight variation in the peak at 3393.71 cm −1 for 2 • -amine of the GEF-pure. This finding exhibited that there was no potential intermolecular interaction between GEF and TPGS in its binary complex, which was also noted in the previous studies such as the complexation of desloratadine with HP β-CD [45], quercetin with methyl-β-CD [46] and fluconazole with β-CD [47]. Halogen peaks were also observed in the binary complex with a drastic change in their stretching vibration peaks at 1462.14 cm −1 for the fluoro and 838.57 cm −1 for chloro group in comparison to the peaks of the GEF pure.…”

“…These findings suggested the feasible manifestation of an inclusion complex between the GEF-TPGS SDs and HP β-CD. Moreover, the diminished sharp melting endotherm of GEF in inclusion complex indicated the amorphous conversion of GEF (in GEF-TPGS SDs) during its complexation with HP β-CD and confirms the formation of the complex, which could be substantiated by previous reports [45,50].…”

“…In contrast, when the GEF SDs were prepared with TPGS as a stabilizer, the thermogram did not show an endothermic peak of GEF at around the melting endotherm of GEF, which was attributed to the good molecular dispersion of GEF in the GEF-TPGS SDs. The broad peak of endotherm for HP β-CD near to 133 • C might be due to its thermal degradation, which was also reported during the development of the HP-β-CD inclusion complex of lipophilic drugs, such as desloratadine [45] and posaconazole [49]. Overall, the reduction in and absence of endothermic peak intensity of GEF in the SDs and HP-β-CD-complex manifested the increased solubilization of the drug due to its amorphous conversion from crystalline state.…”