ArticleInternational journal of nanomedicine2015
Oral lipid-based nanoformulation of tafenoquine enhanced bioavailability and blood stage antimalarial efficacy and led to a reduction in human red blood cell loss in mice.
Article in International journal of nanomedicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- Using chanarin-dorfman syndrome patient fibroblasts to explore disease mechanisms and new treatment avenues.Orphanet journal of rare diseases · 2025Article
- Pharmacokinetic Models of Tafenoquine: Insights for Optimal Malaria Treatment Strategies.Pharmaceutics · 2024Review
- Liver-targeted polymeric prodrugs delivered subcutaneously improve tafenoquine therapeutic window for malaria radical cure.Science advances · 2024Article
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- Heparin-Coated Dendronized Hyperbranched Polymers for Antimalarial Targeted Delivery.ACS applied polymer materials · 2023Article
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- The zebrafish embryo as an in vivo model for screening nanoparticle-formulated lipophilic anti-tuberculosis compounds.Disease models & mechanisms · 2022Article
- A Perspective on Nanotechnology and COVID-19 Vaccine Research and Production in South Africa.Viruses · 2021Article
- Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether.Antimicrobial agents and chemotherapy · 2021Article
- Preclinical Assessment Addressing Intravenous Administration of a [Molecules (Basel, Switzerland) · 2021Article
- Nanotechnology approaches for global infectious diseases.Nature nanotechnology · 2021Review
- Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy againstBioactive materials · 2021Article
- Could the Drug Tafenoquine Revolutionize Treatment of Babesia microti Infection?The Journal of infectious diseases · 2019Article
- Nanomedicines for Malaria Chemotherapy: Encapsulation vs. Polymer Therapeutics.Pharmaceutical research · 2018Review
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tafenoquine (TQ), a new synthetic analog of primaquine, has relatively poor bioavailability and associated toxicity in glucose-6-phosphate dehydrogenase (G6PD)-deficient individuals. A microemulsion formulation of TQ (MTQ) with sizes <20 nm improved the solubility of TQ and enhanced the oral bioavailability from 55% to 99% in healthy mice (area under the curve 0 to infinity: 11,368±1,232 and 23,842±872 min·μmol/L) for reference TQ and MTQ, respectively. Average parasitemia in Plasmodium berghei-infected mice was four- to tenfold lower in the MTQ-treated group. In vitro antiplasmodial activities against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum indicated no change in half maximal inhibitory concentration, suggesting that the microemulsion did not affect the inherent activity of TQ. In a humanized mouse model of G6PD deficiency, we observed reduction in toxicity of TQ as delivered by MTQ at low but efficacious concentrations of TQ. We hereby report an enhancement in the solubility, bioavailibility, and efficacy of TQ against blood stages of Plasmodium parasites without a corresponding increase in toxicity.
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