Amorphous Solid Dispersion of α-Mangosteen with PVP K30 Enhances Solubility and Antiproliferative Activity against DU145 Prostate Cancer Cells

Abstract

Prostate cancer is one of the leading causes of cancer-related death in men worldwide. The natural compound α-Mangosteen (AM), a xanthone derivative from the fruit rind of Garcinia mangostana L., is known to have strong anticancer activity. However, its clinical use is still limited due to its very low water solubility and bioavailability. This study aims to compare the antiproliferative activity of pure AM and amorphous solid dispersion (ASD-AM) against DU145 prostate cancer cells. Amorphous solid dispersions were prepared using the carrier polymer polyvinylpyrrolidone (PVP) K30 via the solvent evaporation method. Physicochemical characterization was performed using Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), and Fourier-Transform Infrared Spectroscopy (FTIR). Cytotoxicity tests against DU145 prostate cancer cells and normal Vero cells were performed using the MTT method to determine the IC₅₀ value and selectivity index (SI). The results showed that ASD-AM had an IC₅₀ value of 22.19 µg/mL, which was lower than pure AM (47.34 µg/mL), with SI values of 1.99 and 2.15, respectively. The increased antiproliferative activity of ASD-AM is associated with a change in physicochemical properties to an amorphous form, which enhances solubility and dissolution rate.

Overall, the amorphous AM solid dispersion formulation has the potential to enhance its biological effectiveness as a natural anticancer agent for the development of prostate cancer therapy.