Enhanced In Vitro Antiviral Activity of Hydroxychloroquine Ionic Liquids against SARS-CoV-2

The development of effective antiviral drugs against SARS-CoV-2 is urgently needed and a global health priority. In light of the initial data regarding the repurposing of hydroxychloroquine (HCQ) to tackle this coronavirus, herein we present a quantitative synthesis and spectroscopic and thermal cha...

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Published inPharmaceutics Vol. 14; no. 4; p. 877
Main Authors Faísca, Francisco, Correia, Vanessa, Petrovski, Željko, Branco, Luís C, Rebelo-de-Andrade, Helena, Santos, Miguel M
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 17.04.2022
MDPI
Subjects
API-ILs
Bioavailability
Biological activity
Coronaviruses
COVID-19
Drugs
hydroxychloroquine
Infections
Malaria
Pandemics
Pharmaceutical industry
pharmaceutical ionic liquids
Respiratory diseases
SARS-CoV-2
Severe acute respiratory syndrome coronavirus 2
Viral infections
COVID-19
pharmaceutical ionic liquids
SARS-CoV-2
hydroxychloroquine
API-ILs
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Summary:The development of effective antiviral drugs against SARS-CoV-2 is urgently needed and a global health priority. In light of the initial data regarding the repurposing of hydroxychloroquine (HCQ) to tackle this coronavirus, herein we present a quantitative synthesis and spectroscopic and thermal characterization of seven HCQ room temperature ionic liquids (HCQ-ILs) obtained by direct protonation of the base with two equivalents of organic sulfonic, sulfuric and carboxylic acids of different polarities. Two non-toxic and hydrophilic HCQ-ILs, in particular, [HCQH2][C1SO3]2 and [HCQH2][GlcCOO]2, decreased the virus-induced cytopathic effect by two-fold in comparison with the original drug, [HCQH2][SO4]. Despite there being no significant differences in viral RNA production between the three compounds, progeny virus production was significantly affected (p < 0.05) by [HCQH2][GlcCOO]2. Overall, the data suggest that the in vitro antiviral activities of the HCQ-ILs are most likely the result of specific intra- and intermolecular interactions and not so much related with their hydrophilic or lipophilic character. This work paves the way for the development of future novel ionic formulations of hydroxychloroquine with enhanced physicochemical properties.
Bibliography:These authors contributed equally to this work.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics14040877