Al-Mashhadani Abdulazeez M, Al-Samydai Ali, Al-Deeb Ibrahim, Carradori Simone, Azzam Hanan, Janabi Hussein S, Al Qudah Dana, Alshaer Walhan, Mozafari M R
Pharmacological and Diagnostic Research Centre, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman, 19328, Jordan.
Faculty of Pharmacy, Zarqa University, Zarqa, 13132, Jordan.
Anticancer Agents Med Chem. 2025 Jul 16. doi: 10.2174/0118715206388843250709121645.
Colorectal cancer is an important cause of cancer-related mortality, necessitating innovative therapies to improve efficacy and reduce side effects. This study explores the potential of Cisplatin and Rutin-loaded nanoliposomes (Cis-NLs and Rut-NLs) for anti-colorectal cancer activity.
Cis-NLs and Rut-NLs were prepared using thin-film hydration, achieving encapsulation efficiencies of 95.5% and 62.5%, respectively. Drug release studies revealed controlled profiles, with Cis-NLs showing a complete release (100%) and Rut-NLs reaching 23.48% over 48 hours. Stability assessments demonstrated minimal changes in size, polydispersity index (PDI), and zeta potential over three months. Encapsulation efficiency decreased slightly for Cis-NLs (92.87%) and significantly for Rut-NLs (26.55%). Several tests were performed to evaluate the biological activity of this combination on colorectal cancer cells and HDF cells to check its selectivity.
In vitro cytotoxicity studies on HT29 colorectal cancer cells revealed IC50 values of 1.72 μg/mL for free Cisplatin, 2.35 μg/mL for Cis-NLs, >100 μg/mL for free Rutin, and 63.33 μg/mL for Rut-NLs. A combination of Cis-NLs and Rut-NLs reduced the IC50 to 2.2 μg/mL. Selective toxicity evaluation using human dermal fibroblasts showed an IC50 of 79.24 μM for cisplatin, reduced to 63.3 μM in Cis-NLs, with Rut-NLs demonstrating negligible toxicity.
Wound healing assays confirmed significant inhibition of cell migration, with wound closure reduced from 62.41% in controls to 34.35% in treated groups. Utilizing nanotechnology, liposomal formulations were synthesized to enhance drug delivery and therapeutic synergy.
These results highlight the potential of Cisplatin and Rutin-loaded nanoliposomes as a combination therapy for colorectal cancer.
结直肠癌是癌症相关死亡的一个重要原因，因此需要创新疗法来提高疗效并减少副作用。本研究探讨了载有顺铂和芦丁的纳米脂质体（顺铂纳米脂质体和芦丁纳米脂质体）在抗结直肠癌活性方面的潜力。
采用薄膜水化法制备顺铂纳米脂质体和芦丁纳米脂质体，包封率分别达到95.5%和62.5%。药物释放研究显示出可控的释放曲线，顺铂纳米脂质体在48小时内显示完全释放（100%），芦丁纳米脂质体在48小时内释放率达到23.48%。稳定性评估表明，在三个月内，纳米脂质体的大小、多分散指数（PDI）和zeta电位变化极小。顺铂纳米脂质体的包封率略有下降（92.87%），而芦丁纳米脂质体的包封率显著下降（26.55%）。进行了多项测试以评估该组合对结直肠癌细胞和人皮肤成纤维细胞的生物学活性，以检查其选择性。
对HT29结直肠癌细胞的体外细胞毒性研究显示，游离顺铂的IC50值为1.72μg/mL，顺铂纳米脂质体为2.35μg/mL，游离芦丁>100μg/mL，芦丁纳米脂质体为63.33μg/mL。顺铂纳米脂质体和芦丁纳米脂质体的组合将IC50降低至2.2μg/mL。使用人皮肤成纤维细胞进行的选择性毒性评估显示，顺铂的IC50为79.24μM，在顺铂纳米脂质体中降至63.3μM，而芦丁纳米脂质体显示出可忽略不计的毒性。
伤口愈合试验证实细胞迁移受到显著抑制，伤口闭合率从对照组的62.41%降至治疗组的34.35%。利用纳米技术合成脂质体制剂以增强药物递送和治疗协同作用。
这些结果突出了载有顺铂和芦丁的纳米脂质体作为结直肠癌联合治疗方法的潜力。
