Abstract
Introduction: More than 40% of the newly developed drugs pose a problem of aqueous insolubility which is a major challenge for pharmaceutical scientists since in this form; drug doesn’t show required bioavailability and hence sufficient therapeutics effect.
Objective: The improvement of dissolution rate of ibuprofen (IBF) (poorly water-soluble drug) by formulating its solid dispersions using milk as generally recommended as safe carrier was the goal and purpose of this study.
Method: For this, milk containing 1.5% fat (named yellow milk due to yellow-colored pack) and milk containing 4.5% fat (named green milk due to green-colored pack) were used. Initially, both types of milk were rota evaporated to obtain free flowing powdered form. Then, the physical mixtures were prepared in different ratios by simple mixing and solid dispersions were formulated in different ratios by solvent evaporation method using hot air oven. Various techniques were used to evaluate and characterize the physical mixtures and solid dispersions, which included melting point determination, solubility studies, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, X-ray diffraction (XRD), in vitro dissolution studies, and scanning electron microscopy (SEM).
Results: DSC and XRD studies showed reduction in peak intensity of drug indicating the conversion of crystalline drug into amorphous form. SEM studies indicated that the agglomerates formed were smaller and denser with a smooth surface. In vitro dissolution studies showed that the quantity of drug solubilized and the rate of dissolution increase after formulation into the solid dispersions.
Conclusion: The milk powder was found to enhance the solubility of IBF due to the presence of casein which entrapped the hydrophobic drug by forming micelles.
Objective: The improvement of dissolution rate of ibuprofen (IBF) (poorly water-soluble drug) by formulating its solid dispersions using milk as generally recommended as safe carrier was the goal and purpose of this study.
Method: For this, milk containing 1.5% fat (named yellow milk due to yellow-colored pack) and milk containing 4.5% fat (named green milk due to green-colored pack) were used. Initially, both types of milk were rota evaporated to obtain free flowing powdered form. Then, the physical mixtures were prepared in different ratios by simple mixing and solid dispersions were formulated in different ratios by solvent evaporation method using hot air oven. Various techniques were used to evaluate and characterize the physical mixtures and solid dispersions, which included melting point determination, solubility studies, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, X-ray diffraction (XRD), in vitro dissolution studies, and scanning electron microscopy (SEM).
Results: DSC and XRD studies showed reduction in peak intensity of drug indicating the conversion of crystalline drug into amorphous form. SEM studies indicated that the agglomerates formed were smaller and denser with a smooth surface. In vitro dissolution studies showed that the quantity of drug solubilized and the rate of dissolution increase after formulation into the solid dispersions.
Conclusion: The milk powder was found to enhance the solubility of IBF due to the presence of casein which entrapped the hydrophobic drug by forming micelles.
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Copyright
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