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Vesicular Formation of Trans -Ferulic Acid: an Efficient Approach to Improve the Radical Scavenging and Antimicrobial Properties
Journal of Pharmaceutical Innovation ( IF 2.6 ) Pub Date : 2021-03-01 , DOI: 10.1007/s12247-021-09543-8
Anahita Rezaeiroshan , Majid Saeedi , Katayoun Morteza-Semnani , Jafar Akbari , Akbar Hedayatizadeh-Omran , Hamidreza Goli , Ali Nokhodchi

Purposes

Reactive oxygen species production is harmful to human’s health. The presence of antioxidants in the body may help to diminish reactive oxygen species. Trans-ferulic acid is a good antioxidant, but its low water solubility excludes its utilization. The study aims to explore whether a vesicular drug delivery could be a way to overcome the poor absorption of trans-ferulic acid hence improving its antimicrobial efficiency and antioxidant effect.

Methods

Niosomal vesicles containing the drug were prepared by film hydration method. The obtained vesicles were investigated in terms of morphology, size, entrapment efficiency, release behavior, cellular cytotoxicity, antioxidant, cellular protection study, and antimicrobial evaluations.

Results

The optimized niosomal formulation had a particle size of 158.7 nm and entrapment efficiency of 21.64%. The results showed that the optimized formulation containing 25 μM of trans-ferulic acid could enhance the viability of human foreskin fibroblast HFF cell line against reactive oxygen species production. The minimum effective dose of the plain drug and the niosomal formulation against Staphylococcus aurous (ATCC 29213) was 750 µg/mL and 375 µg/mL, respectively, and for Escherichia coli (ATCC 25922), it was 750 µg/mL and 187/5 µg/mL, respectively. The formulation could also improve the minimum bactericidal concentration of the drug in Staphylococcus aurous, Escherichia coli, and Acinobacter baumannii (ATCC 19606).

Conclusion

These results revealed an improvement in both antibacterial and antioxidant effects of the drug in the niosomal formulation.



中文翻译:

反式果酸的囊泡形成:改善自由基清除和抗菌性能的有效方法。

目的

活性氧的产生对人体健康有害。体内抗氧化剂的存在可能有助于减少活性氧。反式阿魏酸是一种良好的抗氧化剂,但其水溶性低,无法利用。该研究旨在探讨水泡药物的输送是否可以克服反式阿魏酸吸收差,从而提高其抗菌效率和抗氧化作用的方法。

方法

通过膜水合作用制备含药物的脂质体囊泡。从形态,大小,包封率,释放行为,细胞毒性,抗氧化剂,细胞保护研究和抗菌评估等方面对获得的囊泡进行了研究。

结果

优化的纳米脂质体制剂的粒径为158.7 nm,包封率为21.64%。结果表明,含有25μM反式阿魏酸的优化配方可以增强人包皮成纤维细胞HFF细胞系对活性氧产生的活力。普通药物和尼古斯丁制剂对金黄色葡萄球菌的最低有效剂量(ATCC 29213)分别为750 µg / mL和375 µg / mL,而对于大肠杆菌(ATCC 25922)的最低有效剂量分别为750 µg / mL和187 / g分别为5 µg / mL。该制剂还可以提高金黄色葡萄球菌大肠杆菌大肠杆菌中药物的最低杀菌浓度。鲍曼不动杆菌(ATCC 19606)。

结论

这些结果揭示了该药物在鼻内制剂中的抗菌和抗氧化作用均得到改善。

更新日期:2021-03-01
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