Remdesivir powders manufactured by jet milling for potential pulmonary treatment of COVID-19

Abstract

Remdesivir is one of the effective drugs proposed for the treatment of coronavirus disease 2019 (COVID-19). However, the study on inhalable regimen is currently limited though COVID-19 is respiratory diseases and infects lung area. This work aims to prepare inhalable remdesivir formulations and verify their effectiveness through in vitro evaluations. Formulations containing different ratios of jet-milled inhalable remdesivir (5, 10, 20,40, and 70%) with excipients were produced and characterized in terms of the particle size distribution, particle morphology, flowability, water content, crystallinity, the water sorption and desorption capabilities, and the aerodynamic performance. Results indicating that drug loading are a vital factor in facilitating the dispersion of remdesivir dry powder, and the ternary excipient plays a negligible role in improving aerosol performance. Besides, the 70% remdesivir with lactose carrier (70% RD-Lac) was physically stable and retain high aerosol performance after conditioned at 40 °C and 75% RH for a month. Therefore, formulation 70% RD-Lac might be recommended as a candidate product for the potential treatment of COVID-19.

Graphical Abstract

Keywords:

• Remdesivir
• dry powder inhalation
• drug loading
• jet milling
• pulmonary delivery

Acknowledgments

The author acknowledge the Zhejiang Xianju Pharmaceutical company (Hangzhou) for the technical and instrument support during the project.

Disclosure statement

The authors report there are no competing interests to declare.

Additional information

Funding

This work was supported by the (National Key R&D Project of China) funding scheme under Grant [2021YFB1715500] and Ministry of Sciences and Technology of the People's Republic of China.