Encapsulating Apigenin in Chitosan-PLGA Nanoparticles for Enhanced Breast Cancer Cytotoxicity

Abstract

Breast cancer is a significant global health concern, with limitations in current therapies highlighting the need for novel approaches. Apigenin (APG), a flavonoid derived from natural sources, displays promising anti-cancer effects, but its effectiveness is limited by its low solubility and bioavailability. This study aimed to develop and evaluate chitosan-coated PLGA nanoparticles (CS-PLGA NPs) for enhanced delivery and efficacy of APG against breast cancer cells. CS-PLGA NPs loaded with APG were synthesized and characterized by size, surface charge, drug loading, and release profile. Subsequently, their cytotoxicity against SKBR3 breast cancer cells was compared to free APG. APG-CS-PLGA NPs exhibited the desired characteristics (size ~ 170 nm, positive zeta potential, high encapsulation efficiency 98.7%) and displayed a sustained APG release profile. Release results in gastrointestinal conditions suggest that PLGA-CS nanoparticles are promising for oral apigenin (APG) administration, as they retain most of the drug content. Notably, these nanoparticles significantly enhanced APG cytotoxicity toward SKBR3 cells compared to free APG (IC50: 67.1 vs. 151.5 µg/mL), indicating improved cellular uptake and efficacy. This study demonstrates the successful development of CS-PLGA NPs as a promising platform for targeted APG delivery with enhanced anticancer activity against breast cancer cells. Further investigations are warranted to explore in vivo efficacy and optimize the system for clinical applications.