In Vivo Pharmacokinetic Study of Remdesivir Dry Powder for Inhalation in Hamsters

This article has been Reviewed by the following groups

Read the full article See related articles

Discuss this preprint

Start a discussion What are Sciety discussions?

Abstract

Remdesivir dry powder for inhalation was previously developed using thin film freezing (TFF). A single-dose 24-hour pharmacokinetic study in hamsters, a small animal model for SARS-CoV-2, demonstrated that pulmonary delivery of TFF remdesivir can achieve plasma remdesivir and GS-441524 levels higher than the reported EC 50 s of both remdesivir and GS-441524 (in human epithelial cells) over 20 hours. The half-life of GS-4412524 following dry powder insufflation was about 7 hours, suggesting the dosing regimen would be twice daily administration. Although the remdesivir-Captisol ® (80/20 w/w) formulation showed faster and greater absorption of remdesivir and GS-4412524 in the lung, remdesivir-leucine (80/20 w/w) exhibited a greater C max with shorter T max and lower AUC of GS-441524, indicating lower total drug exposure is required to achieve a high effective concentration against SAR-CoV-2. In conclusion, remdesivir dry powder for inhalation would be a promising alternative dosage form for the treatment of COVID-19 disease.

Article activity feed

  1. SciScore for 10.1101/2020.12.22.424071: (What is this?)

    Please note, not all rigor criteria are appropriate for all manuscripts.

    Table 1: Rigor

    Institutional Review Board StatementIACUC: Single-dose dry powder insufflation in hamsters: This study was in compliance with the Institutional Animal Care and Use Committee (IACUC; Protocol Number AUP-2019-00254) guidelines at The University of Texas at Austin.
    Randomizationnot detected.
    Blindingnot detected.
    Power Analysisnot detected.
    Sex as a biological variableFemale Syrian hamsters (Charles River, 049LVG) 35-42-days old and weighing between 80 and 130 g (average weight of 102 g) were housed in a 12-hour light/dark cycle with access to food and water ad libitum and were subjected to one week of acclimation to the housing environment.

    Table 2: Resources

    Software and Algorithms
    SentencesResources
    Sulfobutylether-beta-cyclodextrin (SBECD, Captisol®) was kindly provided by Ligand Pharmaceuticals, Inc. (San Diego, CA)
    Ligand Pharmaceuticals
    suggested: None

    Results from OddPub: We did not detect open data. We also did not detect open code. Researchers are encouraged to share open data when possible (see Nature blog).


    Results from LimitationRecognizer: An explicit section about the limitations of the techniques employed in this study was not found. We encourage authors to address study limitations.

    Results from TrialIdentifier: No clinical trial numbers were referenced.


    Results from Barzooka: We did not find any issues relating to the usage of bar graphs.


    Results from JetFighter: We did not find any issues relating to colormaps.


    Results from rtransparent:
    • Thank you for including a conflict of interest statement. Authors are encouraged to include this statement when submitting to a journal.
    • Thank you for including a funding statement. Authors are encouraged to include this statement when submitting to a journal.
    • No protocol registration statement was detected.

    About SciScore

    SciScore is an automated tool that is designed to assist expert reviewers by finding and presenting formulaic information scattered throughout a paper in a standard, easy to digest format. SciScore checks for the presence and correctness of RRIDs (research resource identifiers), and for rigor criteria such as sex and investigator blinding. For details on the theoretical underpinning of rigor criteria and the tools shown here, including references cited, please follow this link.