In-vitro and in-vivo evaluation of taste-masked ibuprofen formulated in oral dry emulsions

Abstract

Objective The aim of this study was to develop a paediatric oral preparation for ibuprofen. Significance Ibuprofen is widely used for defervescence in children, but medication compliance is poor due to its bitter taste. Dry emulsions possess good stability and can be transported and stored in solid form; they can be dispersed into liquid emulsions with water and easily administered to children. Methods In this study, a dry emulsion excipient was prepared by spray drying: a mixture of orange peel and corn oils (3:7, w/w) were used as the oil phase and solvent for ibuprofen; gum arabic and gum tragacanth were chosen as emulsifiers; and maltodextrin was used as a solid carrier. Results The particle sizes of the liquid and reconstituted emulsions were 5.75 μm and 6.11 μm, respectively; the average particle size distribution of the dry emulsion powder was 8.13 μm; scanning electron microscopy showed that the dry emulsion powder was composed of evenly distributed smooth spheres. At a drug loading of 36.52 ± 1.15 mg/g, 90% of ibuprofen was released from the dry emulsion excipient within 30 min. Sensory evaluations using human volunteers, rats and an electronic tongue demonstrated that the emulsion had a taste-masking effect on ibuprofen.It was further corroborated by in vivo studies using rat model that highlighted a 1.76-fold increase in ibuprofen absorption when the drug was administered as a emulsion compared with granules. Conclusions These results indicate that the dry emulsion for taste-masking is promising and valuable in the development of ibuprofen for pediatrics.