Terbinafine for prostate cancer: development of coated zein nanospheres for ameliorated pro-apoptosis in PC3 cells.

Aim: The purpose of this study was to investigate comparatively the anticancer potential of Terbinafine loaded Dextran Sulphate coated Zein nanospheres against human prostate cancer PC3 cells to enhance the repurposing profile of terbinafine utilizing optimized nano-sized delivery systems.

Materials & methods: The formula was fabricated using the thin film hydration technique. Particle size analysis, drug diffusion, and encapsulation efficiency were considered when evaluating the fabricated formula, which were developed using a Box-Behnken statistical design.

Results: Due to the formula optimization, the mean particle size was 273.2 ± 1.98 nm, the zeta potential was -38.4 ± 2.77 mV, and the amount released after 36 h was 97.4 ± 5.7%. The formula exhibited significantly reduced IC₅₀ in PC3 cells by around 14-fold. A higher cellular uptake was observed. The cell cycle assay results obtained suppression of the proliferation, especially in the G₀/G₁ and S phases. This pro-apoptotic pattern of the optimized formula was confirmed by the increased mRNA expression of CASP3 and P53 and reduced expression of CDK1, CDK7, and CDK9. Furthermore, a higher production of reactive oxygen species was achieved.

Conclusion: The optimized formula revealed enhanced pro-apoptosis in PC3 cells which support the repurposing profile of terbinafine toward prostate cancer.