Surface Solid Dispersion of Ketoconazole on Trehalose Dihydrate using Spray Drying to Achieve Enhanced Dissolution Rate

Ketoconazole (K) is a poorly water-soluble drug that faces significant challenges in achieving therapeutic efficacy. This study aimed to enhance the dissolution rate of ketoconazole by depositing spray-dried ketoconazole (SK) onto the surface of ground trehalose dihydrate (T) using spray drying. Ketoconazole-trehalose surface solid dispersions (SKTs) were prepared in ratios of 1:1 (SK1T1), 1:4 (SK1T4), and 1:10 (SK1T10), and characterized them using particle size analysis, scanning electron microscopy, powder X-ray diffraction, and in vitro dissolution studies.

Results showed that the dissolution rates of the dispersions were significantly higher than those of pure ketoconazole, with the 1:10 ratio showing the highest dissolution rate. The improved dissolution was attributed to the formation of a new crystalline phase and better dispersion of ketoconazole particles. These findings suggest that the surface solid dispersion approach could be a valuable method for enhancing the bioavailability of poorly water-soluble drugs.

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Materials

Ketoconazole (≥ 98% purity) was obtained from Janssen Pharmaceutica (Beerse, Belgium. Trehalose dihydrate (99% purity) was purchased from BSTC (Norwich, England). Monobasic potassium phosphate (≥ 99.5%) and dichloromethane (≥ 99.8%) were purchased from Merck (Darmstadt, Germany).

Weecharangsan, W., Lee, R.J. Surface Solid Dispersion of Ketoconazole on Trehalose Dihydrate using Spray Drying to Achieve Enhanced Dissolution Rate. AAPS PharmSciTech 25, 220 (2024). https://doi.org/10.1208/s12249-024-02941-4

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