ArticlePharmaceutics2019
Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure.
Article in 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, 44 citations in OpenAlex.
- The expanding role of formulations to enable oral delivery of poorly water-soluble drugs.Nature reviews. Drug discovery · 2026Review
- Oral peptide drug delivery: design of SEDDS providing a protective effect against intestinal membrane-bound enzymes.Drug delivery and translational research · 2026Article
- Review
- Vitamin D-loaded lipid nanoparticles: antioxidant properties, preparation, optimization, and in vitro characterization.Drug delivery and translational research · 2025Article
- Rilpivirine Ionic Liquid Nanoemulsion Augments the Oral Bioavailability of Rilpivirine and Its Delivery to the HIV Sanctuary Sites.ACS applied materials & interfaces · 2025Article
- Sweetening the Deal: Sweetener-Based Ionic Liquid of Albendazole Significantly Enhances Its Solubility and Oral Bioavailability.Molecular pharmaceutics · 2025Article
- An Overview on the Role of Ionic Liquids and Deep Eutectic Solvents in Oral Pharmaceuticals.Pharmaceutics · 2025Review
- Rationalizing Counterion Selection for the Development of Lipophilic Salts: A Case Study with Venetoclax.Molecular pharmaceutics · 2024Article
- Oral Self-Nanoemulsifying System Containing Ionic Liquid of BX795 Is Effective against Genital HSV-2 Infection in Mice.ACS infectious diseases · 2024Article
- A Comprehensive Review on Imperative Role of Ionic Liquids in Pharmaceutical Sciences.Current drug delivery · 2024Review
- Recent Advances in Biocompatible Ionic Liquids in Drug Formulation and Delivery.Pharmaceutics · 2023Review
- Application of Design of Experiments in the Development of Self-Microemulsifying Drug Delivery Systems.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Solidification of Self-Emulsifying Drug Delivery Systems as a Novel Approach to the Management of Uncomplicated Malaria.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Docusate-Based Ionic Liquids of Anthelmintic Benzimidazoles Show Improved Pharmaceutical Processability, Lipid Solubility, andACS infectious diseases · 2021Article
- Ionic Liquids and Deep Eutectic Solvents for Application in Pharmaceutics.Pharmaceutics · 2020Article
- Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine.International journal of molecular sciences · 2020Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as low melting, lipophilic salts or ionic liquids (ILs) provides one means to enhance drug solubility in LBFs. However, whether different ILs benefit from formulation in different LBFs is largely unknown. In the current studies, lumefantrine was isolated as a number of different lipophilic salt/ionic liquid forms and performance was assessed after formulation in a range of LBFs. The solubility of lumefantrine in LBF was enhanced 2- to 80-fold by isolation as the lumefantrine docusate IL when compared to lumefantrine free base. The increase in drug loading subsequently enhanced concentrations in the aqueous phase of model intestinal fluids during in vitro dispersion and digestion testing of the LBF. To assess in vivo performance, the systemic exposure of lumefantrine docusate after administration in Type II-MCF, IIIB-MCF, IIIB-LCF, and IV formulations was evaluated after oral administration to rats. In vivo exposure was compared to control lipid and aqueous suspension formulations of lumefantrine free base. Lumefantrine docusate in the Type IIIB-LCF showed significantly higher plasma exposure compared to all other formulations (up to 35-fold higher). The data suggest that isolation of a lipid-soluble IL, coupled with an appropriate formulation, is a viable means to increase drug dose in an oral formulation and to enhance exposure of lumefantrine
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.