- Research Article
- 10.1128/mbio.03696-25
Development and evaluation of novel zein-based artemisinin sustained-release formulation for treating drug-resistant malaria.
- Jan 12, 2026
- mBio
- Yijie Wang + 9 more +9
Half of the world's population is at risk of malaria infection, and artemisinin (ART) turns out to be a powerful medicine for malaria control. The rapid emergence and global spread of resistance to ART have led to a significantly increasing clinical treatment failure rate worldwide. A critical limitation of ART is its extremely short blood half-life (~1 h), which results in rapid declines in plasma drug concentrations below therapeutic thresholds. Some parasites may switch into a "dormant" form, which is less sensitive to ART, resulting in recrudescence following treatment. Thus, developing a sustained-release formulation provides a promising solution to prolong the in vivo half-life of ART. Additionally, its relatively low solubility restricts its in vivo bioavailability, primarily due to the limited dissolution and absorption of the compound in aqueous biological environments. In this study, we prepared a zein-based sustained-release formulation of ART for oral and intraperitoneal administration. Our results indicate that this zein-based sustained release nanoformulation not only significantly improves ART's water solubility (a key barrier to its bioavailability) but also extends its in vivo half-life via controlled drug release. Importantly, the prolonged half-life ensures sustained therapeutic ART concentrations, directly enhancing the formulation's ability against ART-resistant P. falciparum strains. Collectively, these results highlight the formulation's substantial potential for clinical application in improving ART-based antimalarial therapy.
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