Silibinin-loaded cubosomes: a gateway to enhanced hepatoprotective activity

IF 3 Q2 PHARMACOLOGY & PHARMACY
Khaled Y. Mahmoud, Yasmeen N. Ezzeldeen, Arwa A. Nasr, Mai O. Ghonim, Menna W. Ibrahim, Mohamed G. Ali, Mona A. Helmi, Nada A. Mostafa, Nada T. Abdelaziz, Naira N. Elmohandes, Yara H. Mahmoud, Shady A. Swidan
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引用次数: 0

Abstract

Background

The liver is a vital organ that detoxifies drugs and xenobiotics. However, breaking down toxins creates byproducts that can damage the liver. Silibinin possesses a proven hepatoprotective and antioxidant effect as it inhibits the free radicals produced from the metabolism of toxic substances, such as paracetamol and ethanol. Unfortunately, the poor bioavailability of silibinin hinders its use, which could be overcome by loading it into lipid nanocarriers, such as cubosomes. This study aims to formulate silibinin-loaded cubosomes and evaluate their hepatoprotective effect in vivo.

Results

A full factorial design was conducted to evaluate the percentage of poloxamer 407 and the sonication time. The prepared cubosomes were characterized by multiple characterization techniques. The in vitro release of silibinin from the chosen formulation was also evaluated. An induced acute paracetamol hepatotoxicity model in mice was utilized for in vivo evaluation. The particle size of the formulated cubosomes ranged from 123.2 to 210.9 nm, and the polydispersity index range was 0.226–0.560. The zeta potential of the formulations ranged between − 14.2 and − 25.6 mV. The chosen formulation displayed a controlled release pattern. The chosen formulation showed a significant hepatoprotective action by reducing the liver marker enzymes. The histopathological study also confirmed the hepatoprotective activity of the chosen cubosomes. The hepatoprotective effects of the chosen formulation can be attributed to positive impacts on oxidative stress, as demonstrated in oxidative stress markers.

Conclusion

The obtained results suggest that silibinin-loaded cubosomal formulation offers apotentially improved hepatoprotection effect against induced acute paracetamol hepatotoxicity.

Graphical abstract

装载水飞蓟宾的立方体体:增强肝保护活性的途径
肝脏是一个重要的器官,可以为药物和外来药物排毒。然而,分解毒素会产生损害肝脏的副产品。水飞蓟宾具有肝脏保护和抗氧化作用,因为它能抑制有毒物质代谢产生的自由基,如扑热息痛和乙醇。不幸的是,水飞蓟宾的低生物利用度阻碍了它的使用,这可以通过将其装载到脂质纳米载体(如立方体)中来克服。本研究旨在制备装载水飞蓟宾的体质体,并在体内评价其肝保护作用。结果采用全因子设计评价波洛沙姆407的含量和超声时间。用多种表征技术对制备的立方体体进行了表征。并对所选制剂水飞蓟宾的体外释放度进行了评价。采用小鼠急性对乙酰氨基酚肝毒性模型进行体内评价。配制的立方体体粒径范围为123.2 ~ 210.9 nm,多分散性指数范围为0.226 ~ 0.560。zeta电位在−14.2 ~−25.6 mV之间。所选择的制剂显示出控释模式。所选择的配方通过降低肝脏标记酶显示出显著的肝保护作用。组织病理学研究也证实了所选立方体体的肝保护活性。正如氧化应激标志物所证明的那样,所选配方的肝保护作用可归因于对氧化应激的积极影响。结论水飞蓟宾立方体制剂对急性扑热息痛肝毒性有一定的保护作用。图形抽象
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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来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
期刊介绍: Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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