Atovaquone: A Comprehensive Review of Its Antimicrobial Efficacy and Mechanism of Action

The emergence of parasite resistance and the low oral bioavailability of antimalarial drugs are the two main problems that hinder the clinical success of antimalarial chemotherapy. The prophylactic efficacy of 17C91, a carbamate prodrug of atovaquone (ATQ), was studied in a severe combined immunodeficient mouse model of Pneumocystis carinii pneumonia (PCP) at an oral dose equivalent to 100 mg ATQ per kg body weight per day. The activity of atovaquone in combination with another antimalarial agent should be studied. The aim of this study was to improve the solubility and bioavailability of the Atovaquone tablet, using an internal biosynthesizer in a ternary solid dispersion system containing hydrophilic polymers with different concentrations of biosurfactant. Atovaquone is an antimalarial agent and belongs to the class IV biopharmaceutical classification system. The developed method is simple, sensitive and reproducible and can be used for routine analysis of atovaquone in bulk and tablet dosage forms. Solid nanoparticles of atovaquone were successfully produced by electrospray and characterized for their particle size and flow properties. Atovaquone is measured at 251 nm in methanol. The Beer’s law was observed in the drug concentration range of 1–10 μg/mL. Food likely increasing its absorption of Atovaquone by increasing its solubility in the gut lumen. These results suggest that liposome loaded ATV is more efficacious than the free drug against Leishmania infantum in this murine model.

Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2024-12-13
DOI
https://doi.org/10.5281/zenodo.14451885
Primary Topic
Pneumocystis jirovecii pneumonia detection and treatment
Type
article
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article

Atovaquone: A Comprehensive Review of Its Antimicrobial Efficacy and Mechanism of Action

Zenodo (CERN European Organization for Nuclear Research)
Pneumocystis jirovecii pneumonia detection and treatment
article

Atovaquone: A Comprehensive Review of Its Antimicrobial Efficacy and Mechanism of Action

article en

Abstract

The emergence of parasite resistance and the low oral bioavailability of antimalarial drugs are the two main problems that hinder the clinical success of antimalarial chemotherapy. The prophylactic efficacy of 17C91, a carbamate prodrug of atovaquone (ATQ), was studied in a severe combined immunodeficient mouse model of Pneumocystis carinii pneumonia (PCP) at an oral dose equivalent to 100 mg ATQ per kg body weight per day. The activity of atovaquone in combination with another antimalarial agent should be studied. The aim of this study was to improve the solubility and bioavailability of the Atovaquone tablet, using an internal biosynthesizer in a ternary solid dispersion system containing hydrophilic polymers with different concentrations of biosurfactant. Atovaquone is an antimalarial agent and belongs to the class IV biopharmaceutical classification system. The developed method is simple, sensitive and reproducible and can be used for routine analysis of atovaquone in bulk and tablet dosage forms. Solid nanoparticles of atovaquone were successfully produced by electrospray and characterized for their particle size and flow properties. Atovaquone is measured at 251 nm in methanol. The Beer’s law was observed in the drug concentration range of 1–10 μg/mL. Food likely increasing its absorption of Atovaquone by increasing its solubility in the gut lumen. These results suggest that liposome loaded ATV is more efficacious than the free drug against Leishmania infantum in this murine model.

Zenodo (CERN European Organization for Nuclear Research)
Openalex Percentile: Top 56%
Pneumocystis jirovecii pneumonia detection and treatment
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