Mangiferin-Loaded Polymeric Nanoparticles: Optical Characterization, Effect of Anti-topoisomerase I, and Cytotoxicity

Abstract

Mangiferin is an important xanthone compound presenting various biological activities. The objective of this study was to develop, characterize physicochemical properties, and evaluate the anti-topoisomerase activity of poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing mangiferin. The nanoparticles were developed by the emulsion solvent evaporation method and the optimal formulation was obtained with a response surface methodology (RSM); this formulation showed a mean size of 176.7 ± 1.021 nm with a 0.153 polydispersibility index (PDI) value, and mangiferin encapsulation efficiency was about 55%. The optimal conditions (6000 rpm, 10 min, and 300 μg of mangiferin) obtained 77% and the highest entrapment efficiency (97%). The in vitro release profile demonstrated a gradual release of mangiferin from 15 to 180 min in acidic conditions (pH 1.5). The fingerprint showed a modification in the maximum absorption wavelength of both the polymer and the mangiferin. Results of anti-toposiomerase assay showed that the optimal formulation (MG4, 25 µg/mL) had antiproliferative activity. High concentrations (2500 µg/mL) of MG4 showed non-in vitro cytotoxic effect on BEAS 2B and HEPG2. Finally, this study showed an encapsulation process with in vitro gastric digestion resistance (1.5 h) and without interfering with the metabolism of healthy cells and their biological activity.

Mangiferin as New Potential Anti-Cancer Agent and Mangiferin-Integrated Polymer Systems—A Novel Research Direction

“…Most recently, Francisco Fabian Razura-Carmona and colleagues reported on the physical and chemical properties as well as evaluation of the anti-topoisomerase activity of poly (lactic-co-glycolic) nanoparticles (PLGA) containing mangiferin [ 149 ]. By design, 15 mg of PLGA (75:25) was integrated with different amounts of mangiferin.…”

Anti-Angiogenic Properties of Ginsenoside Rg3 Epimers: In Vitro Assessment of Single and Combination Treatments

“…The optimal combination was determined using response surface methodology (RSM), a statistical and experiment design modelling process, which aims at reducing the number of experiments and costs associated with the experiment design [ 20 ]. In recent years, RSM has gained popularity in drug design [ 21 ], drug interaction [ 22 ], and combination therapy in cancer treatment studies [ 23 ]. It describes a three-dimensional dose–response surface, measures drug interactions, and defines the optimised combination of two drugs [ 24 ].…”

Copper Oxide Nanoparticle Diameter Mediates Serum‐Sensitive Toxicity in BEAS‐2B Cells

“…[ 20,21 ] Even so, many studies with BEAS‐2B cells and nanotoxicity utilize over 2% serum in the cell culture medium, potentially causing conflicting results ( Figure 1 ). [ 22–44 ]…”