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.
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Lupeol (LP) and Mangiferin (MG) have beneficial effects on health, however, their pharmacokinetic properties can affect their bioavailability by oral administration, therefore, their incorporation in a hybrid matrix of ZnO and PLGA could contribute as a vehicle to improve bioavailability.
Methods:
Therefore, the objective of this study was to develop this matrix and evaluate its optical and bioactive properties obtained by the solvent emulsion and evaporation method, which were subjected to processes to evaluate their bioactivity as the effect of topoisomerase.
Results:
Functionalized treatment number 15 (TF15) showed the best results in studies of controlled release and encapsulation efficiency of lupeol (LP) and mangiferin (MG) (60.01 ± 1.24% and 57.71 ± 1.94%), the best treatment showed behaviors as a topoisomerase II inhibitor (18.60 ± 1.55). The nanoparticles developed in this study did not show a cytotoxic effect on BEAS-2B, while for HepG2 it showed a decrease in viability (IC50 1549.96 ± 174.62 µg/mL). On the other hand, although the hemolytic activity is not shown at 1 h of exposure, morphological alterations caused by TF15 are observed at concentrations of 2500 and 1250 µg/mL.
Conclusion:
In this context, the TF15 treatment shown by maintain its biological activity, does not present cytotoxicity for healthy cells, and decreases the growth of cancer cells.
In recent years, interest in the development of nanometric materials with specific characteristics has grown; however, there are few scientific contributions that associate encapsulation methodologies and matrices with the particle objective (metabolic directions, type of administration, biological impact, and biocompatibility). This review focuses on describing the benefits and disadvantages of different techniques for designing custom particles and alternatives for the biofunctionalization nanomaterials regarding the biological impact of a nanomaterial with potential use in foods known as nutraceuticals. The study of optical properties, physicochemical factors, and characteristics such as rheological can predict its stability in the application matrix; however, not only should the characterization of a nanocomposite with applications in food be considered, but also the biological impact that it may present.
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