Development and Characterization of Solid Dispersion System for Enhancing the Solubility and Dissolution Rate of Dietary Capsaicin

Abstract

Background:Capsaicin is a pungent component of chili peppers that suppresses the growth of various cancer cell lines including breast cancer. However, it shows extremely low oral bioavailability due to its poor water solubility.Objective:The objective of the present work was to improve the solubility and dissolution rate of capsaicin.Methods:Solid dispersions were prepared by the solvent evaporation method using different molar ratios of capsaicin and urea (1:1, 1:2, and 1:3). Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD) study were used to characterize the solid dispersion. Solid dispersions were evaluated for solubility, dissolution rate and in vitro cytotoxicity in breast cancer cell lines.Results:XRD and DSC studies exhibited the reduced crystallinity of a drug in solid dispersion. Phase solubility study shows that the drug solubility increased by increasing carrier concentration. In vitro release study of the solid dispersion showed the faster dissolution of a drug with increasing carrier concentration. Solid dispersion formulation effectively inhibited the growth of MCF-7 human breast cancer and MDA-MB-231 triple negative human breast cancer cells in an MTT assay that measures metabolic activity, but only slightly decreased cell viability when compared to capsaicin alone.Conclusion:The present study demonstrated that solid dispersion of capsaicin in PEG 6000 overcomes the problems related to the poor aqueous solubility of this drug and improving its dissolution rate.