Formulation development of curcumin-piperine solid dispersion via hot-melt extrusion

Abstract

Curcumin is one of the major ingredients derived from turmeric (Curcuma Longa Linn). For many years, curcumin was used in Indian traditional medicine to treat several diseases. It has anti-inflammatory, anti-cancer, and anti-diabetic activities. In addition, curcumin has a low aqueous solubility of 0.00575 mg/mL, which has been associated with its poor release profile. The aim of this study is to improve the release profile of curcumin utilizing the hot-melt extrusion technique (HME) to prepare curcumin-piperine solid dispersion (SD). Three physical mixtures of curcumin, piperine, and Soluplus® were prepared with different ratios between the compositions. Two different extrusion temperatures (130 °C and 140 °C) were applied during the extrusion step. Drug release studies for the pure compounds and the extrudates were performed using the USP apparatus II, and the samples were analyzed using high-performance liquid chromatography (HPLC). Curcumin-piperine solid dispersion was successfully prepared by hot-melt extrusion technology. Differential scanning calorimetry (DSC) results showed the presence of endothermic peaks, one for curcumin at 179 °C, and another for piperine at 132 °C. However, these peaks were not observed in the extrudates thermograms, indicating the solubilization of curcumin and piperine within the polymeric carrier at an amorphous state. The release studies revealed significant improvement in curcumin release profiles for up to 9-folds in the formulations, compared to pure curcumin.