The Potential Cytotoxic Activity Enhancement of α-Mangostin in Chitosan-Kappa Carrageenan-Loaded Nanoparticle against MCF-7 Cell Line

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.

Alpha-Mangostin-Loaded Transferrin-Conjugated Lipid-Polymer Hybrid Nanoparticles: Development and Characterization for Tumor-Targeted Delivery

“…In another study, the cytotoxicity of water-soluble β -cyclodextrin-coated α -mangostin polymeric nanoparticles on A549 lung cancer cells was enhanced by 2.1-fold in comparison with free α -mangostin [ 39 ]. Wathoni and colleagues have demonstrated that α -mangostin chitosan-loaded kappa carrageenan nanoparticles (IC 50 of 4.7 µ g/mL) exhibited a higher antiproliferative activity on MCF-7 cells than drug solution (IC 50 of 8.2 µ g/mL) [ 40 ], in line with our results.…”

Nanoformulations of α-Mangostin for Cancer Drug Delivery System

“…Cytotoxicity in MCF-7 cells showed an increase in nanoparticle activity compared to free α-mangostin. The IC 50 of α-mangostin, α-mangostin-chitosan nanoparticle, and α-mangostin-chitosan-kappa carrageenan was 8.2, 6.7, and 4.7 g/mL, respectively [79].…”

Cytotoxicity Enhancement in MCF-7 Breast Cancer Cells with Depolymerized Chitosan Delivery of α-Mangostin

“…The physicochemical and biological characteristics of CSNPs are strongly influenced by their MW and surface charge [ 22 , 23 , 24 , 25 ]. The surface charge of the NPs impacts the accumulation of NPs at the target site, stability, cellular uptake, protein adsorption applications, and distribution throughout the body.…”

“…Modified CS can be made into multilayer composites by combining with polymers and other parts to change the properties of CS for certain biomedical applications, such as sodium alginate and chitosan [ 31 ]. CS can be encapsulated using kappa carrageenan [ 22 ] and Diethyl curcumin disuccinate [ 32 ]. CS–NPs were modified with either biotin or biotin and avidin [ 33 ].…”

“…CS coating can improve the physical stability of NPs [ 34 ] and overcome poor solubility in water and low selectivity against cancer cells. AMG in CS-kappa carrageenan can increase potential cytotoxic activity [ 22 ]. Modification of MW–CS affect the molecular weight, size, surface smoothness, porosity, shape, and charge of CSNPs, then change the kinetics of the effect of increasing permeability and retention (EPR), increasing AMG cytotoxicity ( Scheme 1 ).…”