研究负载顺铂和芦丁的纳米脂质体对结直肠癌细胞的治疗潜力。

IF 3 4区 医学 Q3 CHEMISTRY, MEDICINAL
Abdulazeez M Al-Mashhadani, Ali Al-Samydai, Ibrahim Al-Deeb, Simone Carradori, Hanan Azzam, Hussein S Janabi, Dana Al Qudah, Walhan Alshaer, M R Mozafari
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引用次数: 0

摘要

导语:结直肠癌是癌症相关死亡的重要原因,需要创新的治疗方法来提高疗效和减少副作用。本研究探讨了顺铂和负载芦丁的纳米脂质体(Cis-NLs和Rut-NLs)抗结直肠癌活性的潜力。方法:采用薄膜水合法制备顺式nls和Rut-NLs,包封率分别为95.5%和62.5%。药物释放研究显示,顺式nls在48小时内完全释放(100%),而鲁特nls达到23.48%。稳定性评估表明,在三个月内,尺寸、多分散性指数(PDI)和zeta电位的变化很小。顺式nls的包封率略有下降(92.87%),而鲁特- nls的包封率显著下降(26.55%)。我们进行了几项试验来评估该组合对结直肠癌细胞和HDF细胞的生物活性,以检查其选择性。结果:体外对HT29结直肠癌细胞的细胞毒性研究显示,游离顺铂的IC50值为1.72 μg/mL,顺- nls的IC50值为2.35 μg/mL,游离芦丁的IC50值为100 μg/mL,游离芦丁的IC50值为63.33 μg/mL。Cis-NLs和Rut-NLs联合使用可使IC50降至2.2 μg/mL。使用人真皮成纤维细胞进行的选择性毒性评估显示,顺铂的IC50为79.24 μM,顺- nls的IC50降至63.3 μM,而Rut-NLs的毒性可以忽略。讨论:伤口愈合实验证实了细胞迁移的显著抑制,伤口愈合从对照组的62.41%降低到治疗组的34.35%。利用纳米技术,合成了脂质体制剂,以增强药物传递和治疗协同作用。结论:这些结果突出了顺铂和负载芦丁的纳米脂质体作为结直肠癌联合治疗的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Investigating the Therapeutic Potential of Cisplatin- and Rutin-Loaded Nanoliposomes against Colorectal Cancer Cells.

Introduction: 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.

Methods: 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.

Results: 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.

Discussion: 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.

Conclusion: These results highlight the potential of Cisplatin and Rutin-loaded nanoliposomes as a combination therapy for colorectal cancer.

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来源期刊
Anti-cancer agents in medicinal chemistry
Anti-cancer agents in medicinal chemistry ONCOLOGY-CHEMISTRY, MEDICINAL
CiteScore
5.10
自引率
3.60%
发文量
323
审稿时长
4-8 weeks
期刊介绍: Formerly: Current Medicinal Chemistry - Anti-Cancer Agents. Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents. Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication. Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
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