α-Mangostin, a xanthone derivative from the pericarp of Garcinia mangostana L., has numerous bioactivities and pharmacological properties. However, α-mangostin has low aqueous solubility and poor target selectivity in the human body. Recently, nanoparticle drug delivery systems have become an excellent technique to improve the physicochemical properties and effectiveness of drugs. Therefore, many efforts have been made to overcome the limitations of α-mangostin through nanoparticle formulations. Our review aimed to summarise and discuss the nanoparticle drug delivery systems for α-mangostin from published papers recorded in Scopus, PubMed and Google Scholar. We examined various types of nanoparticles for α-mangostin to enhance water solubility, provide controlled release and create targeted delivery systems. These forms include polymeric nanoparticles, nanomicelles, liposomes, solid lipid nanoparticles, nanofibers and nanoemulsions. Notably, nanomicelle modification increased α-mangostin solubility increased more than 10,000 fold. Additionally, polymeric nanoparticles provided targeted delivery and significantly enhanced the biodistribution of α-mangostin into specific organs. In conclusion, the nanoparticle drug delivery system could be a promising technique to increase the solubility, selectivity and efficacy of α-mangostin as a new drug candidate in clinical therapy.

No abstract

α-mangostin (αM), a xanthone derivative compound isolated from the extract of mangosteen pericarp (Garcinia mangostana L), has potential anticancer properties for breast cancer. However, it has poor solubility in water and low selectivity towards cancer cells. The polymeric nanoparticle formulation approach can be used to overcome these problems. In this study, a chitosan biopolymer-based αM polymeric nanoparticle formulation was encapsulated using kappa carrageenan (αM-Ch/Cr) as a novel carrier for breast cancer therapy and evaluated for their physicochemical properties, drug release profile, and in vitro cytotoxicity against breast cancer cells (MCF-7). Polymeric nanoparticles formulated with varying concentrations of kappa carrageenan were successfully prepared by ionic gelation and spray pyrolysis techniques. αM-Ch/Cr nanoparticles formed perfectly round particles with a size of 200–400 nm and entrapment efficiency ≥ 98%. In vitro release studies confirmed that αM-Ch/Cr nanoparticles had a sustained release system profile. Interestingly, the formulation of polymeric nanoparticles significantly (p < 0.05) increased the cytotoxicity of αM against MCF-7 cell with IC50 value of 4.7 μg/mL compared to the non-nanoparticle with IC50 of 8.2 μg/mL. These results indicate that αM-Ch/Cr nanoparticles have the potential to improve the physicochemical properties and cytotoxicity effects of αM compounds as breast cancer therapy agents.