Enhanced Anticancer Activity Of Taxifolin Via Niosomal Encapsulation In MCF-7 Breast Cancer Cells

Abstract

Background: Though taxifolin is a naturally occurring flavonoid with autoantioxidant capabilities and some reported anticancer effects, its real-world applications are still limited due to its instability and poor bioavailability. Niosomes, as a nanodelivery system, are expected to enhance delivery effectiveness. This investigation aimed to evaluate the potential chemoprotective and pro-apoptotic effects of taxifolin-loaded niosomes (Tax-NIO) in MCF-7 breast cancer cells.

Methods: The thin-film method was used to prepare the niosomes, which were characterized for morphology, size, and polydispersity index (PDI). The drugs loaded niosomes were subjected to entrapment efficiency (EE) and stability, and drug release studies. We further evaluated the impact of Taxifolin on the viability of breast cancer cells, RT-qPCR assays, malondialdehyde (MDA) activity, and cell cycle progression.

Results: Tax-NIO has a small size of approximately 51 ± 0.40 nm, a low PDI of 0.132 ± 0.14, and a zeta potential of -21 ± 0.23 mV, indicating stability. There was a continuous release of drugs in comparison to unencapsulated taxifolin. In a dose-dependent manner, Tax-NIO caused a drop in MCF-7 cell viability, and its IC₅₀ was 48.9 µM, which was higher than the 23.4 µM IC₅₀ for olaparib. Upregulation of pro-apoptotic genes such as p53, Bax, Caspase-9, and Caspase-3 was observed, whereas anti-apoptotic genes Bcl-2 and PARP-1 were downregulated. Tax-NIO resulted in a significantly lower level of lipid peroxidation. Cell cycle analysis also showed there was significant G2/M phase arrest in the Tax-NIO-treated cells.

Conclusions: Incorporation of taxifolin into niosomes exhibits even greater anticancer effects against MCF-7 breast cancer cells, including increased apoptosis, greater inhibition of oxidative stress, and greater disruption of cell-cycle progression. Thus, these findings indicate that Tax-NIO could serve as an effective nanotherapeutic strategy for breast cancer and warrant further preclinical and translational studies.