ArticleMolecular pharmaceutics2019
Impact of Ferroquine on the Solubilization of Artefenomel (OZ439) during in Vitro Lipolysis in Milk and Implications for Oral Combination Therapy for Malaria.
Article in Molecular pharmaceutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 40 citations in OpenAlex.
- Pharmacokinetics of a Novel Piperaquine Dispersible Granules Formulation Under Fasting and Various Fed Conditions Versus Piperaquine Tablets When Fasted in Healthy Tanzanian Adults: A Randomized, Phase I Study.Clinical and translational science · 2025Trial
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- Unexpected Effect of Digestion Products of Infant Formula in Enhancing the Solubilisation of Tolfenamic Acid During Digestion.Pharmaceutics · 2026Article
- Recent Advancement in Drug Development for Treating Malaria using Herbal Medicine and Nanotechnological Approach.Current pharmaceutical design · 2025Review
- Implications of the Digestion of Milk-Based Formulations for the Solubilization of Lopinavir/Ritonavir in a Combination Therapy.Molecular pharmaceutics · 2023Article
- Small-volumeInternational journal of pharmaceutics: X · 2022Article
- Fighting Plasmodium chloroquine resistance with acetylenic chloroquine analogues.International journal for parasitology. Drugs and drug resistance · 2022Article
- Impact of pasteurization on the self-assembly of human milk lipids during digestion.Journal of lipid research · 2022Article
- Potential of nanoformulations in malaria treatment.Frontiers in pharmacology · 2022Review
- The influence of lipid digestion on the fate of orally administered drug delivery vehicles.Biochemical Society transactions · 2021Review
- Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.ACS medicinal chemistry letters · 2021Article
- Article
- Lipid Compositions in Infant Formulas Affect the Solubilization of Antimalarial Drugs Artefenomel (OZ439) and Ferroquine during Digestion.Molecular pharmaceutics · 2020Article
- Correlating Digestion-Driven Self-Assembly in Milk and Infant Formulas with Changes in Lipid Composition.ACS applied bio materials · 2020Article
- Low-Frequency Raman Scattering Spectroscopy as an Accessible Approach to Understand Drug Solubilization in Milk-Based Formulations during Digestion.Molecular pharmaceutics · 2020Article
- Application of Low-Frequency Raman Scattering Spectroscopy to Probe in Situ Drug Solubilization in Milk during Digestion.The journal of physical chemistry letters · 2019Article
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Milk is an attractive lipid-based formulation for the delivery of poorly water-soluble drugs to pediatric populations. We recently observed that solubilization of artefenomel (OZ439) during in vitro intestinal lipolysis was driven by digestion of triglycerides in full-cream bovine milk, reflecting the ability of milk to act as an enabling formulation in the clinic. However, when OZ439 was co-administered with a second antimalarial drug, ferroquine (FQ) the exposure of OZ439 was reduced. The current study therefore aimed to understand the impact of the presence of FQ on the solubilization of OZ439 in milk during in vitro intestinal digestion. Synchrotron small-angle X-ray scattering was used for in situ monitoring of drug solubilization (inferred via decreases in the intensity of drug diffraction peaks) and polymorphic transformations that occurred during the course of digestion. Quantification of the amount of each drug solubilized over time and analysis of their distributions across the separated phases of digested milk were determined using high-performance liquid chromatography. The results show that FQ reduced the solubilization of OZ439 during milk digestion, which may be due to competitive binding of FQ to the digested milk products. Interactions between the protonated FQ-H
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