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

Nanomedicine (London, England) Pub Date : 2025-04-01 Epub Date: 2025-04-02 DOI:10.1080/17435889.2025.2481823
Majid M Al-Sawahli, Yasmin A El-Feky, Ahmed J Mohammed, Nada M Mohamed, Rania El-Telbany, Zaenah Zuhair Alamri, Sahar Jameel Melebary, Mohammad Y Alfaifi, Serag Eldin I Elbehairi, Ayman M Noreddin, Ashraf B Abdel-Naim, Ebtesam M Alolayan, Dalia F El-Telbany
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Abstract

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.

特比萘芬治疗前列腺癌:用于改善PC3细胞凋亡的包被玉米蛋白纳米球的开发。
目的:比较特比萘芬负载的葡聚糖硫酸盐包被玉米蛋白纳米微球对人前列腺癌PC3细胞的抗癌潜力,以优化特比萘芬的纳米递送系统。材料与方法:采用薄膜水化技术制备该配方。采用Box-Behnken统计设计对配方进行评价,考虑粒径分析、药物扩散和包封效率。结果:经配方优化后,平均粒径为273.2±1.98 nm, zeta电位为-38.4±2.77 mV, 36 h后释放量为97.4±5.7%。该配方显著降低PC3细胞的IC50约14倍。观察到较高的细胞摄取。细胞周期实验结果显示,细胞增殖受到抑制,特别是在G0/G1期和S期。CASP3和P53 mRNA表达增加,CDK1、CDK7和CDK9 mRNA表达降低,证实了优化配方的这种促凋亡模式。此外,还获得了较高的活性氧产量。结论:优化后的配方可增强PC3细胞的促凋亡作用,支持特比萘芬治疗前列腺癌的新用途。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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