Assessment of the Antigenotoxic Activity of Poly(d,l-lactic-co-glycolic acid) Nanoparticles Loaded with Caffeic Acid Phenethyl Ester Using the Ames Salmonella/Microsome Assay

Abstract

In the present study, the antigenotoxic activity of poly(d,l-lactic- co-glycolic acid) (PLGA) nanoparticles (NPs) loaded with caffeic acid phenethyl ester (CAPE) was investigated in comparison to free CAPE using the Ames Salmonella/microsome assay. Additionally, to elucidate the impacts of the type of solvent effect on antigenotoxic activity, the following systems were tested: CAPE in water (poor solvent), ethyl alcohol (good solvent), and PLGA NPs (unknown). The effect of the NP system on solubility was investigated for the first time by assessing the antigenotoxic potential. In this study, the CAPE/PLGA NPs were synthesized using an oil-in-water (o/w) single-emulsion solvent evaporation method with an average size of 206.2 ± 1.2 nm, ζ potential of -19.8 ± 2.5 mV, encapsulation efficiency of 87.2 ± 2.5%, and drug loading of 53.3 ± 1.8%. According to the results of the antigenotoxic activity, the highest antimutagenic activity in both applied strains was found for CAPE in ethanol, and the lowest activity was detected for CAPE in water. Our study has shown that NP systems exhibit high antigenotoxic activity, which is similar to the results of CAPE dissolved in ethanol. These results have shown that NP systems increase biological activity of hydrophobic substances by increasing their solubility and that the use of PLGA instead of organic solvents in drug production may provide an increase in their medical utility.

FA-97, a New Synthetic Caffeic Acid Phenethyl Ester Derivative, Ameliorates DSS-Induced Colitis Against Oxidative Stress by Activating Nrf2/HO-1 Pathway

“…As a phenolic constituent derived from honeybee propolis, CAPE possesses great anti-inflammatory activities and can suppress the proinflammatory cytokines production and enhance epithelial barrier function, which could be a potential therapeutic agent for IBD (17,18). However, the unstable chemical property, low water solubility and the poor bioavailability of CAPE limit its efficacy (19)(20)(21). Therefore, in order to enhance the water solubility, chemical stability and pharmacological activity of CAPE, FA-97 was newly synthesized by introducing a D-glucose into CAPE to construct a glucosidic bond (Figure 1).…”

“…It has been reported that the application of CAPE in vivo is also under restrictions due to the low water solubility (20). Moreover, the poor bioavailability of CAPE limit its efficacy and the half-life of CAPE is 20-28 min independent of the dose after intragastric administration (21).…”

Comparative evaluation of hesperetin loaded nanoparticles for anticancer activity against C6 glioma cancer cells

“…Encapsulation efficiency and drug-loading capacity were determined by indirect method via spectrophotometric evalution of supernatant obtained after centrifugation [24]. The amount of unentrapped hesperetin in external solution was determined using UV-Vis spectroscopy at 374 nm and the hesperetin concentration was calculated using previously constructed standard calibration curve.…”

Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems

“…CAPE-loaded particles exerted antimutagenic activity, in a comparable extent to CAPE in ethanolic solution. It was measured by means of the Ames bacterial reverse mutation assay (Arasoğlu and Derman 2018). Furthermore, CAPE-loaded PLGA NPs were shown to have antiparasitic effects towards both forms of L. infantum with better efficacy against amastigotes (Abamor 2017).…”