Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Physical Chemistry

Background:

• Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID) with limited aqueous solubility, impacting its oral bioavailability.
• Developing advanced drug delivery systems is crucial for improving the efficacy of poorly soluble drugs like ibuprofen.

Purpose of the Study:

• To create a novel ibuprofen-loaded solid dispersion using cycloamylose to enhance ibuprofen's bioavailability.
• To investigate the impact of cycloamylose on ibuprofen's solubility and physicochemical properties.

Main Methods:

• Solid dispersions were prepared using spray-drying techniques at a 1:1 weight ratio of ibuprofen to cycloamylose.
• Physicochemical characterization involved scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD).
• In vivo studies in rats assessed dissolution profiles and oral bioavailability, comparing the solid dispersion to pure ibuprofen powder.

Main Results:

• The ibuprofen-loaded solid dispersion demonstrated a 14-fold increase in aqueous solubility compared to ibuprofen powder.
• Physicochemical analyses indicated that ibuprofen remained in an unchanged crystalline state within the solid dispersion.
• Cycloamylose acted as a solubilizing agent, and the solid dispersion resulted in a 2-fold higher area under the drug concentration-time curve (AUC) in rats.

Conclusions:

• The developed ibuprofen-cycloamylose solid dispersion effectively enhances ibuprofen's aqueous solubility and oral bioavailability.
• The formulation is a promising approach for improving ibuprofen delivery without causing crystalline changes.
• This solid dispersion technology offers a viable strategy for enhancing the therapeutic potential of ibuprofen.