Folate Receptor-Targeted Nanodelivery of Apigenin in Breast Cancer: Formulation Development, Characterization and In Vitro Evaluation

Abstract

Cancer is a dreadful disease with a high mortality rate and breast cancer is the most common cancer among females in the world. Different strategies have been used for the treatment of breast cancer, including chemotherapy but it has a wide range of side effects. This problem can be overcome by delivering anticancer agents with nano-formulations. Apigenin (4′,5,7-trihydroxyflavone), present in many different medicinal plants, shows potential anticancer properties in various cancers. However, its use in clinical practice is limited due to its low water solubility and bioavailability. In this study, we examined folate receptor-targeted and PEGylated poly(lactide-co-glycolide) nanoparticles (PLGA-PEG-FA NPs) containing apigenin for targeted delivery to MCF-7 breast cancer cells. Apigenin-loaded PLGA-PEG and PLGA-PEG-FA NPs were small in size, had a negative zeta potential, showed sustained release of apigenin and showed significantly higher anticancer activity than the free drug in breast cancer cells. The half maximal inhibitory concentration (IC50) values of apigenin, apigenin-loaded PLGA, PLGA-PEG and PLGA-PEG-FA NPs were 50.2, 49.4, 18.1 and 13.3 μM, respectively. Apigenin-loaded PLGA-PEG and PLGA-PEG-FA NPs showed 2.79- and 3.77-fold higher cytotoxicity than the pristine drug. Folate-conjugated PLGA nanoparticles could be developed for potential target-specific delivery of apigenin in the treatment of breast cancer.