Date of Award
M.S. in Pharmaceutical Science
Michael A Repka
Michael A Repka
University of Mississippi
Curcumin has been known to have a variety of biological activities in different diseases, including inflammation, cancer, and diabetes. The limited bioavailability of curcumin is due to its low solubility and extensive metabolism, rendering curcumin unusable as an oral therapeutic agent. The aim of the study is to enhance the solubility and bioavailability of curcumin by preparing curcumin-piperine solid dispersion (SD) utilizing the hot-melt extrusion technique. Three physical mixtures with different ratios were prepared as following: F1 (5% w/w piperine, 15% w/w curcumin, 80% w/w Soluplus®), F2 (10% w/w piperine, 30% w/w curcumin, 60% w/w Soluplus®), and F3 (15% w/w piperine, 45% w/w curcumin, 40% w/w Soluplus®). The extrusion process was conducted using two different extrusion temperatures, 130 °C and 140 °C, to study the effect of temperature on physicochemical properties. Differential scanning calorimetry (DSC) was used to obtain the thermal characterization of the extrudates with a heating rate of 10 °C/min, ranging 20 to 200 °C. Additionally, Fourier transform infrared spectroscopy (FTIR) was performed to evaluate the chemical interaction between the components. Surface morphologies of the extrudates were analyzed utilizing the scanning electron microscope. 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 the hot-melt extrusion technology. 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 formation of hydrogen bonds between the components was observed in the FTIR spectra. Results from drug release studies showed enhancements in curcumin release profiles for up to 9-folds in the formulations, compared to pure curcumin.
Althobaiti, Abdulmajeed, "Formulation Development Of Curcumin-Piperine Solid Dispersion Via Hot-Melt Extrusion To Enhance Solubility And Bioavailability Of Curcumin" (2020). Electronic Theses and Dissertations. 1839.
Available for download on Tuesday, August 31, 2021