Avaliação da ação quimiopreventiva de formulação nanoestruturada contendo quercetina contra efeitos genotóxicos e mutagênicos

Abstract

The skin's antioxidant defense mechanism against UV radiation is not sufficient to eliminate the free radicals produced. This, the importance of using antioxidant substances is unquestionable. Among the chemopreventive agents, it is possible to highlight natural substances, such as quercetin. However, the low water solubility, reduced half-life, chemical instability and low permeability through the skin makes its topical application difficult. This, the nanoencapsulation of this active is a promising alternative. This, the present work aimed to develop nanostructured lipid carriers for the encapsulation of quercetin (CLN-QCT) with the aim of chemoprevention against the harmful effects of UVA radiation. NLCs were developed by ultrasonic irradiation using a mixture of plant derived lipids and block copolymers. The NLCs showed physicochemical characteristics similar to those described in the literature, with DHm of 230.7 nm ± 30.6, PZ of -36.5 ± 2.1 mV, IP of 0.247 ± 0.07 and EE of 91.29 ± 2.09%. During three months, the formulation showed satisfactory preliminary stability under all storage conditions. In the assay with the fibroblast lineage, it was observed that nanostructuring may contribute to a greater tolerability of cells in relation to free QCT. On the other hand, for keratinocytes, there was no significant difference between the cell viability values for QCT and CLN QCT. Furthermore, for both cell lines, the formulation containing 50 µg/mL of QCT showed no significant difference in cell viability when compared to the negative control. In the comet assay, it was possible to observe that NLCs containing QCT (50 µg/mL) were effective in preventing damage to the DNA of fibroblast cells, which was caused by UVA radiation. This effect was more pronounced when compared to free QCT and control groups. In view of this, it is possible to suggest that the developed nanocarrier may be promising for the prevention of DNA-damaging effects resulting from UVA radiation.