Development and Characterization of Polylactic Acid-Resveratrol-Based Polymeric Nanoparticles and Their Cytotoxic Effect on Two Breast Cancer Cell Lines in Combination with Doxorubicin.

Background/

Objectives

Resveratrol (RSV) is a phenolic compound that possesses antioxidant properties and whose biological application has been limited by its physicochemical properties, including its low solubility and stability.

Methods

In this study, polymeric nanoparticles (NPs) were developed using polylactic acid (PLA) to encapsulate resveratrol and improve its bioavailability, using a factorial design to optimize the formulation and evaluate its cytotoxicity against breast cancer cells.

Results

The optimized system presented an average size of 389.2 nm, a PDI of 0.127, a negative z-potential, and an encapsulation efficiency of 76.02%. The statistical analysis indicated that the PLA: RSV ratio was the main determinant of encapsulation percentage and particle size (p < 0.05). On the other hand, with the hemolysis test, blood compatibility was evidenced at all concentrations evaluated, while in the cell assays, the PLA-RSV nanoparticles significantly decreased the cellular viability of MCF-7 and MDA-MB 231 cells compared to untreated cells, and in combination with NP PLA-RSV and doxorubicin, greater cytotoxicity was produced in MCF-7 cells compared to nanoparticle-only treatments (p < 0.05, ANOVA, via followed by a Fisher test).

Conclusions

In addition, distinct cytotoxic effects are observed, associated with their tumor phenotype. Taken together, these results suggest that PLA-RSV NPs are a useful system for future studies on redox status and other biological processes important in cancer.