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

Nasrul Wathoni,Yedi Herdiana,Keiichi Motoyama,Camelia Panatarani,Muchtaridi Muchtaridi,Ahmed Fouad Abdelwahab Mohammed,Ronny Lesmana,Lisna Meylina,Agus Rusdin,I Made Joni,Dorandani Tirtamie

doi:10.3390/polym13111681

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.

Highlights

Upon morphological characterization of the three αM chitosan (αM-Ch)/Cr nanoparticle formulas, it was observed that all formulations formed spherical shapes
The particle size, entrapment efficiency, and drug loading of the polymeric nanoparticles are shown in Figure 3 and Table 2
Entrapment efficiency, and drug loading of polymeric nanoparticles (Table 2), it can be seen in each formula that there is no real correlation between variations of kappa carrageenan concentration and particle size or entrapment efficiency

Summary

Introduction

Breast cancer is currently treated with local treatment (surgery and radiation) and systemic treatment (chemotherapy, hormone therapy, targeted drug therapy, and immunotherapy) [2]. These therapeutic methods have many side effects. Despite its potent cytotoxic effect and anticancer activity, αM has limitations in physicochemical properties that need to be considered, including low solubility and its non-selectivity to cancer cells [6,7]. These properties reduce its effectiveness in treatment of cancer

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Conclusion