Nebulised Isotonic Hydroxychloroquine Aerosols for Potential Treatment of COVID-19
| Autor: | Philip Chi Lip Kwok, Michael Yee Tak Chow, Rachel Yoon Kyung Chang, Patricia Tang, Hak-Kim Chan, Igor Gonda, Waiting Tai, Robert MacArthur |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
hydroxychloroquine
Coronavirus disease 2019 (COVID-19) Hydroxychloroquine sulphate aerosol Pharmaceutical Science vibrating mesh nebuliser Pharmacology Article Pharmacy and materia medica In vivo Isotonic medicine 11 Medical and Health Sciences inhalation Inhalation Chemistry Aerosol droplet COVID-19 Hydroxychloroquine Aerosol RS1-441 Coronavirus coronavirus disease 2019 (COVID-19) droplet 1115 Pharmacology and Pharmaceutical Sciences medicine.drug |
| Zdroj: | Pharmaceutics Volume 13 Issue 8 Pharmaceutics, Vol 13, Iss 1260, p 1260 (2021) |
| ISSN: | 1999-4923 |
| DOI: | 10.3390/pharmaceutics13081260 |
| Popis: | The coronavirus disease 2019 (COVID-19) is an unprecedented pandemic that has severely impacted global public health and the economy. Hydroxychloroquine administered orally to COVID-19 patients was ineffective, but its antiviral and anti-inflammatory actions were observed in vitro. The lack of efficacy in vivo could be due to the inefficiency of the oral route in attaining high drug concentration in the lungs. Delivering hydroxychloroquine by inhalation may be a promising alternative for direct targeting with minimal systemic exposure. This paper reports on the characterisation of isotonic, pH-neutral hydroxychloroquine sulphate (HCQS) solutions for nebulisation for COVID-19. They can be prepared, sterilised, and nebulised for testing as an investigational new drug for treating this infection. The 20, 50, and 100 mg/mL HCQS solutions were stable for at least 15 days without refrigeration when stored in darkness. They were atomised from Aerogen Solo Ultra vibrating mesh nebulisers (1 mL of each of the three concentrations and, in addition, 1.5 mL of 100 mg/mL) to form droplets having a median volumetric diameter of 4.3–5.2 µm, with about 50–60% of the aerosol by volume < 5 µm. The aerosol droplet size decreased (from 4.95 to 4.34 µm) with increasing drug concentration (from 20 to 100 mg/mL). As the drug concentration and liquid volume increased, the nebulisation duration increased from 3 to 11 min. The emitted doses ranged from 9.1 to 75.9 mg, depending on the concentration and volume nebulised. The HCQS solutions appear suitable for preclinical and clinical studies for potential COVID-19 treatment. |
| Databáze: | OpenAIRE |
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