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Article

Nebulised Isotonic Hydroxychloroquine Aerosols for Potential Treatment of COVID-19

1
Advanced Drug Delivery Group, Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, Camperdown, NSW 2006, Australia
2
Pulmoquine Therapeutics, Inc., 1155 Camino Del Mar Suite 481, Del Mar, CA 92014, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Jason T. McConville
Pharmaceutics 2021, 13(8), 1260; https://doi.org/10.3390/pharmaceutics13081260
Received: 24 May 2021 / Revised: 7 August 2021 / Accepted: 12 August 2021 / Published: 14 August 2021
(This article belongs to the Special Issue Inhaled Treatment of Respiratory Infections)
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. View Full-Text
Keywords: hydroxychloroquine; coronavirus disease 2019 (COVID-19); vibrating mesh nebuliser; inhalation; aerosol; droplet hydroxychloroquine; coronavirus disease 2019 (COVID-19); vibrating mesh nebuliser; inhalation; aerosol; droplet
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MDPI and ACS Style

Tai, W.; Chow, M.Y.T.; Chang, R.Y.K.; Tang, P.; Gonda, I.; MacArthur, R.B.; Chan, H.-K.; Kwok, P.C.L. Nebulised Isotonic Hydroxychloroquine Aerosols for Potential Treatment of COVID-19. Pharmaceutics 2021, 13, 1260. https://doi.org/10.3390/pharmaceutics13081260

AMA Style

Tai W, Chow MYT, Chang RYK, Tang P, Gonda I, MacArthur RB, Chan H-K, Kwok PCL. Nebulised Isotonic Hydroxychloroquine Aerosols for Potential Treatment of COVID-19. Pharmaceutics. 2021; 13(8):1260. https://doi.org/10.3390/pharmaceutics13081260

Chicago/Turabian Style

Tai, Waiting, Michael Yee Tak Chow, Rachel Yoon Kyung Chang, Patricia Tang, Igor Gonda, Robert B. MacArthur, Hak-Kim Chan, and Philip Chi Lip Kwok. 2021. "Nebulised Isotonic Hydroxychloroquine Aerosols for Potential Treatment of COVID-19" Pharmaceutics 13, no. 8: 1260. https://doi.org/10.3390/pharmaceutics13081260

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