喷雾干燥的可吸入微粒组合雷姆迪西维尔和埃布塞伦,用于对抗SARS-CoV-2感染
Tushar Saha1, Shubhra Sinha2, Rhodri Harfoot2
1School of Pharmacy, University of Otago, Dunedin 9054, New Zealand.
Pharmaceutics
|September 28, 2023
概括
研究人员开发了一种可吸入的干粉,结合了remdesivir和ebselen,用于COVID-19治疗. 这种组合疗法显示出增强的疗效和低细胞毒性,为呼吸道病毒性疾病提供了一个有前途的新策略.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 病毒学 病毒学
背景情况:
- 开发针对2019年新冠病毒病 (COVID-19) 和其他病毒性呼吸道感染的有效治疗方法仍然是优先事项.
- 吸入疗法对于像SARS-CoV-2这样的呼吸道病毒是合乎逻辑的,向主要感染部位.
- 虽然单一治疗一直是标准,但药物组合在其他病毒性疾病中表现出更高的疗效.
研究的目的:
- 开发和描述一种可吸入的干粉配方,将雷梅西维尔和埃布塞伦结合起来,用于潜在的COVID-19治疗.
- 评估联合药物配方的气溶化特性,细胞毒性和抗病毒活性.
主要方法:
- 使用喷雾干燥技术,制造了雷梅西维尔和埃布塞伦的干粉配方.
- 添加L-氨酸作为一种气溶增强剂.
- 评估了颗粒大小,发射剂量 (ED),细颗粒分数 (FPF),细胞毒性 (CC50) 和抗SARS-CoV-2活性 (EC50).
主要成果:
- 成功制备了具有适合吸入颗粒大小 (1-3μm) 的球形晶体干粉.
- 氨酸显著改善了气溶化,使ED增加到>86%和FPF增加到>67%.
- 组合配方表现出最小的细胞毒性 (CC50 > 100μM),并保留了强大的抗SARS-CoV-2活性 (EC50 2.77至18.64μM).
结论:
- 通过喷雾干燥成功开发了一种可吸入的remdesivir和ebselen干粉配方.
- 该配方表现出有利的物理化学特性,用L-氨酸增强了气溶化,并保持了低细胞毒性的抗病毒疗效.
- 需要进一步的体内研究来验证这种组合疗法的治疗潜力,以防止SARS-CoV-2在呼吸道中的复制.
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