Characterization and optimization of co-delivery Farnesol-Gingerol Niosomal formulation to enhance anticancer activities against breast cancer cells

Abstract

The current investigation is designed to formulate and characterize an optimized Farnesol-Gingerol-loaded (N-Far/Gin) niosomal drug delivery system as a therapeutic approach for breast cancer. The formulation was optimized by altering the surfactant:cholesterol ratio, Span 60:Tween 60 ratio and lipid content, resulting in niosomes with acceptable encapsulation and a controlled release profile. The optimized niosomal formulation demonstrated excellent stability for up to two months with only slight alterations in size and drug encapsulation quality during the storage period. Furthermore, the results demonstrated a pH-dependent release pattern, with delayed drug release under physiological conditions (pH 7.4) and substantial drug release under acidic conditions (pH 5.4), meaning these niosomes display a potent therapeutic potential for breast cancer. Cytotoxicity assays showed a biocompatibility of N-Far/Gin with normal cells while exhibiting inhibitory activity on MCF7 and SKBR3 breast cancer cell lines. The N-Far/Gin down-regulated gene expression levels of BCL2, HER2, CDK4, CCND1, and CCNE while up-regulating gene expression levels of P21, BAX, CASP3, and CASP9 in breast cancer cell lines. Apoptosis assays indicated that N-Far/Gin induces apoptosis in both MCF7 and SKBR3 cell lines, which can be attributed to the synergic efficacy of the two agents. The ROS assay revealed high antioxidant activity of the N-Far/Gin formulation. The experimental findings from this study highlight the importance of highly biocompatible niosomal formulations to the future of nanomedicine; the co-delivery of two phytochemical compounds into cancer cells could enhance therapy effectiveness due to the synergistic impact.