Solubility and Dissolution Enhancement of Dexibuprofen with Hydroxypropylbetacyclodextrin (HPβCD) and Poloxamers (188/407) Inclusion Complexes: Preparation and In Vitro Characterization

The objective of this study was to improve the dissolution and solubility of dexibuprofen (DEX) using hydroxypropyl beta cyclodextrin (HP beta CD) inclusion complexes and also to evaluate the effect of presence of hydrophilic polymers on solubilization efficiency of HP beta CD. Three different methods (physical trituration, kneading and solvent evaporation) were used to prepare binary inclusion complexes at various drug-to-cyclodextrin weight ratios. An increase in solubility and drug release was observed with the kneading (KN) method at a DEX/HP beta CD (1:4) weight ratio. The addition of hydrophilic polymers poloxamer-188 (PXM-188) and poloxamer-407 (PXM-407) at 2.5, 5.0, 10.0 and 20% w/w enhanced the complexation efficiency and solubility of DEX/HP beta CD significantly. Fourier-transform infrared (FTIR) analysis revealed that DEX was successfully incorporated into the cyclodextrin cavity. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) revealed less crystallinity of the drug and its entrapment in the cyclodextrin molecular cage. The addition of PXM-188 or PXM-407 reduced the strength of the DEX endothermic peak. With the addition of hydrophilic polymers, sharp and intense peaks of DEX disappeared. Finally, it was concluded that PXM-188 at a weight ratio of 10.0% w/w was the best candidate for improving solubility, stability and release rate of DEX.

Automated summary

This study aimed to improve the dissolution and solubility of dexibuprofen (DEX) using hydroxypropyl beta cyclodextrin (HP beta CD) inclusion complexes, and evaluate the effect of hydrophilic polymers on the solubilization efficiency of HP beta CD. The kneading method at a DEX/HP beta CD (1:4) weight ratio showed the highest solubility and drug release. The addition of hydrophilic polymers, poloxamer-188 (PXM-188) and poloxamer-407 (PXM-407) significantly enhanced the complexation efficiency and solubility of DEX/HP beta CD. It was concluded that PXM-188 at a weight ratio of 10.0% w/w was the best candidate for improving solubility, stability, and release rate of DEX.