Department of Earth and Planetary Sciences, Weizmann Institute of Science, Rehovot 76100, Israel.
Department of Biomolecular Sciences, Weizmann Institute of Science, Rehovot 76100, Israel.
ACS Biomater Sci Eng. 2022 Jun 13;8(6):2553-2563. doi: 10.1021/acsbiomaterials.2c00419. Epub 2022 May 24.
Delivering medication to the lungs via nebulization of pharmaceuticals is a noninvasive and efficient therapy route, particularly for respiratory diseases. The recent worldwide severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) pandemic urges the development of such therapies as an effective alternative to vaccines. The main difficulties in using inhalation therapy are the development of effective medicine and methods to stabilize the biological molecules and transfer them to the lungs efficiently following nebulization. We have developed a high-affinity angiotensin-converting enzyme 2 (ACE2) receptor-binding domain (RBD-62) that can be used as a medication to inhibit infection with SARS-CoV-2 and its variants. In this study, we established a nebulization protocol for drug delivery by inhalation using two commercial vibrating mesh (VM) nebulizers (Aerogen Solo and PARI eFlow) that generate similar mist size distribution in a size range that allows efficient deposition in the small respiratory airway. In a series of experiments, we show the high activity of RBD-62, interferon-α2 (IFN-α2), and other proteins following nebulization. The addition of gelatin significantly stabilizes the proteins and enhances the fractions of active proteins after nebulization, minimizing the medication dosage. Furthermore, hamster inhalation experiments verified the feasibility of the protocol in pulmonary drug delivery. In short, the gelatin-modified RBD-62 formulation in coordination with VM nebulizer can be used as a therapy to cure SARS-CoV-2.
通过将药物雾化输送到肺部是一种非侵入性且高效的治疗途径,尤其适用于呼吸系统疾病。最近全球严重急性呼吸系统综合征冠状病毒 2 型(SARS-CoV-2)大流行促使人们开发出这种治疗方法,作为疫苗的有效替代品。使用吸入疗法的主要困难在于开发有效的药物以及稳定生物分子的方法,并在雾化后有效地将其递送到肺部。我们已经开发出一种高亲和力的血管紧张素转换酶 2(ACE2)受体结合域(RBD-62),可作为一种药物来抑制 SARS-CoV-2 及其变体的感染。在这项研究中,我们建立了一种通过吸入使用两种商业振动网(VM)雾化器(Aerogen Solo 和 PARI eFlow)进行药物输送的雾化协议,这两种雾化器产生的雾滴大小分布相似,在允许有效沉积在小呼吸道的范围内。在一系列实验中,我们展示了 RBD-62、干扰素-α2(IFN-α2)和其他蛋白质在雾化后的高活性。明胶的添加显著稳定了蛋白质,并增强了雾化后活性蛋白质的分数,从而最小化了药物剂量。此外,仓鼠吸入实验验证了该方案在肺部药物输送中的可行性。简而言之,与 VM 雾化器配合使用的明胶修饰的 RBD-62 制剂可作为治疗 SARS-CoV-2 的方法。