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Injectable niclosamide nanohybrid as an anti-SARS-CoV-2 strategy
Colloids and Surfaces B: Biointerfaces ( IF 5.4 ) Pub Date : 2021-08-24 , DOI: 10.1016/j.colsurfb.2021.112063
N Sanoj Rejinold 1 , Huiyan Piao 1 , Geun-Woo Jin 2 , Goeun Choi 3 , Jin-Ho Choy 4
Affiliation  

COVID-19 is a rapidly evolving emergency, which necessitates scientific community to come up with novel formulations that could find quick relief to the millions affected around the globe. Remdesivir being the only injectable drug by FDA for COVID-19, it initially showed promising results, however, later on failed to retain its claims, hence rejected by the WHO. Therefore, it is important to develop injectable formulation that are effective and affordable. Here in this work, we formulated poly ethylene glycol (PEG) coated bovine serum albumin (BSA) stabilized Niclosamide (NIC) nanoparticles (NPs) (∼BSA-NIC-PEG NPs) as an effective injectable formulation. Here, serum albumin mediated strategy was proposed as an effective strategy to specifically target SARS-CoV-2, the virus that causes COVID-19. The in-vitro results showed that the developed readily water dispersible formulation with a particle size <120 nm size were well stable even after 3 weeks. Even though the in-vitro studies showed promising results, the in-vivo pharmaco-kinetic (PK) study in rats demands the need of conducting further experiments to specifically target the SARS-CoV-2 in the virus infected model. We expect that this present formulation would be highly preferred for targeting hypoalbuminemia conditions, which was often reported in elderly COVID-19 patients. Such studies are on the way to summarize its potential applications in the near future.



中文翻译:

可注射的氯硝柳胺纳米杂化物作为抗 SARS-CoV-2 策略

COVID-19 是一种迅速发展的紧急情况,这就要求科学界想出新的配方,以迅速缓解全球数百万受影响的人。Remdesivir 是 FDA 唯一针对 COVID-19 的可注射药物,它最初显示出可喜的结果,但后来未能保留其声明,因此被 WHO 拒绝。因此,开发有效且负担得起的可注射制剂非常重要。在这项工作中,我们配制了聚乙二醇 (PEG) 包被的牛血清白蛋白 (BSA) 稳定的氯硝柳胺 (NIC) 纳米颗粒 (NPs) (∼BSA-NIC-PEG NPs) 作为一种有效的可注射制剂。在这里,血清白蛋白介导的策略被提出作为一种有效的策略来专门针对 SARS-CoV-2,即导致 COVID-19 的病毒。体外_结果表明,即使在 3 周后,所开发的粒径 <120 nm 的易水分散制剂也非常稳定。尽管体外研究显示出有希望的结果,但大鼠体内药代动力学 (PK) 研究需要进行进一步的实验,以专门针对病毒感染模型中的 SARS-CoV-2。我们预计目前的配方将非常适合针对低白蛋白血症的情况,这在老年 COVID-19 患者中经常被报道。这些研究正在总结其在不久的将来的潜在应用。

更新日期:2021-09-03
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