The ongoing pandemic, COVID-19 (SARS-CoV-2), has afflicted millions of people around the world, necessitating that the scientific community work, diligently and promptly, on suitable medicaments. Although vaccination programs have been run globally, the new variants of COVID-19 make it difficult to restrict the spread of the virus by vaccination alone. The combination of vaccination with anti-viral drug formulation is an ideal strategy for tackling the current pandemic situation. Drugs approved by the United States Food and Drug Administration (FDA), such as Remdesivir, have been found to be of little or no benefit. On the other hand, re-purposing of FDA-approved drugs, such as niclosamide (NIC), has offered promise but its applicability is limited due to its poor aqueous solubility and, therefore, low bioavailability. With advanced nano-pharmaceutical approaches, re-purposing this drug in a suitable drug-carrier for a better outcome may be possible. In the current study, an attempt was made to explore the loading of NIC into exfoliated layered double hydroxide nanoparticles (X-LDH NPs); prepared NIC-X-LDH NPs were further modified with eudragit S100 (ES100), an enteric coating polymer, to make the final product, ES100-NIC-X-LDH NPs, to improve absorption by the gastro/intestinal tract (GIT). Furthermore, Tween 60 was added as a coating on ES100-NIC-X-LDH NPs, not just to enhance its in vitro and in vivo stability, but also to enhance its mucoadhesive property, and to obtain, ultimately, better in vivo pharmacokinetic (PK) parameters upon oral administration. Release of NIC from Tween 60-ES100-NIC-X-LDH NPs was found to be greater under gastro/intestinal solution within a shorter period of time than the uncoated samples. The in vivo analysis revealed that Tween 60-ES100-NIC-X-LDH NPs were able to maintain a therapeutically relevant NIC plasma concentration in terms of PK parameters compared to the commercially available Yomesan®, proving that the new formulation might prove to be an effective oral drug-delivery system to deal with the SARS-CoV-2 viral infections. Further studies are required to ensure their safety and anti-viral efficacy.

持续的流行病 COVID-19 (SARS-CoV-2) 已经折磨了全世界数百万人，因此科学界必须勤奋、迅速地研究合适的药物。尽管疫苗接种计划已在全球范围内开展，但 COVID-19 的新变种使得仅通过疫苗接种来限制病毒的传播变得困难。疫苗接种与抗病毒药物制剂相结合是应对当前大流行情况的理想策略。经美国食品和药物管理局 (FDA) 批准的药物，例如瑞德西韦，已被发现几乎没有益处。另一方面，重新利用 FDA 批准的药物，如氯硝柳胺 (NIC)，已经提供了希望，但由于其水溶性差，因此其生物利用度低，其适用性受到限制。通过先进的纳米药物方法，将这种药物重新用于合适的药物载体以获得更好的结果是可能的。在目前的研究中，试图探索将 NIC 加载到剥离的层状双氢氧化物纳米粒子 (X-LDH NPs) 中；制备的 NIC-X-LDH NPs 用 eudragit S100 (ES100)（一种肠溶包衣聚合物）进一步改性，制成最终产品 ES100-NIC-X-LDH NPs，以改善胃肠道 (GIT) 的吸收。此外，在 ES100-NIC-X-LDH NPs 上添加 Tween 60 作为涂层，不仅可以增强其体外和体内稳定性，还可以增强其粘膜粘附特性​​，并最终获得更好的体内药代动力学。 PK) 口服给药后的参数。发现 NIC 从 Tween 60-ES100-NIC-X-LDH NPs 的释放在胃/肠道溶液下比未涂层样品在更短的时间内更大。体内分析表明，与市售的 Yomesan® 相比，Tween 60-ES100-NIC-X-LDH NPs 在 PK 参数方面能够维持治疗相关的 NIC 血浆浓度，证明新配方可能被证明是一种有效的口服给药系统来应对 SARS-CoV-2 病毒感染。需要进一步研究以确保其安全性和抗病毒功效。体内分析表明，与市售的 Yomesan® 相比，Tween 60-ES100-NIC-X-LDH NPs 在 PK 参数方面能够维持治疗相关的 NIC 血浆浓度，证明新配方可能被证明是一种有效的口服给药系统来应对 SARS-CoV-2 病毒感染。需要进一步研究以确保其安全性和抗病毒功效。体内分析表明，与市售的 Yomesan® 相比，Tween 60-ES100-NIC-X-LDH NPs 在 PK 参数方面能够维持治疗相关的 NIC 血浆浓度，证明新配方可能被证明是一种有效的口服给药系统来应对 SARS-CoV-2 病毒感染。需要进一步研究以确保其安全性和抗病毒功效。