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Contribution to the Improvement of an Oral Formulation of Niclosamide, an Antihelmintic Drug Candidate for Repurposing in SARS-CoV-2 and Other Viruses

preprint
submitted on 01.04.2020 and posted on 06.04.2020 by Eduardo José Barbosa, Mariana Ribeiro Gubitoso, Nádia Araci Bou-Chacra, Stephen R. Byrn, Flavio M. S. Carvalho, Gabriel Lima Barros de Araujo

Niclosamide (NCL) is an effective anthelmintic agent that has been shown to possess broad-spectrum antiviral activity, including against SARS-CoV-2. Due to its poor solubility in aqueous medium, however, the commercially available NCL formulations can act only locally in gastrointestinal worms and are not suitable to achieve plasmatic levels to treat systemic diseases. Consequently, the repurposing of this drug represents a challenge for formulation development with serious risks to the biological availability and can compromise preclinical and clinical outcomes. Herein, we report possible formulation, through the research and development, of stable amorphous solid dispersions to improve its solubility. The results of exploratory screening of NCL-polymer dispersions (performed through X-ray powder diffraction and kinetic solubility studies) indicate that soluplus-niclosamide dispersions can increase its aqueous solubility and, consequently, have the potential to enhance NCL bioavailability. This outcome can be used for the development of oral dosage forms for clinical trials in SARS-CoV-2 and other viruses.

Funding

grant #2018/00273-0, São Paulo Research Foundation (FAPESP);Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil (CAPES) - Finance Code 001.

History

Email Address of Submitting Author

gabriel.araujo@usp.br

Institution

School of Pharmaceutical Sciences, University of Sao Paulo

Country

Brazil

ORCID For Submitting Author

0000-0001-7590-3587

Declaration of Conflict of Interest

we have no conflict of interest to disclose.

Version Notes

Draft Version 1

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