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Improving antimalarial drug absorption through eutectic mixtures with tailored excipients

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Summary:The limited water solubility of many antimalarial drugs significantly restricts their therapeutic efficacy by reducing dissolution rates, bioavailability, and even clinical outcomes. To address this challenge, tailored solvents are used to improve the solubility and bioavailability of antimalarial active pharmaceutical ingredients (APIs) by developing eutectic mixtures. The present study aims to enhance the aqueous solubility of two antimalarial drugs (dapsone and quinine) by formulating eutectic mixtures with selected pharmaceutical excipients (menthol, benzophenone, or glycolic acid). Eutectic systems offer a promising strategy for lowering the melting points of crystalline drugs, thereby improving their dissolution behavior. The solid–liquid equilibria of binary mixtures of dapsone or quinine with each excipient were experimentally measured using the capillary melting point method. The data revealed a significant decrease in the melting points of the APIs. Additionally, most systems exhibited negative deviations from ideal behavior at least in some composition ranges, indicating strong interactions between the drugs and excipients. In general, the COSMO-RS model provided a fair qualitative description of the phase diagrams of the systems, though it predicted positive deviations from ideality in systems that presented experimental negative deviations (dapsone and menthol; dapsone and benzophenone). The methodologies investigated in this work are consistent with the principles of green chemistry, supporting the development of more sustainable and effective solutions for the pharmaceutical industry.
Main Authors:Yahmadi, Rihab
Subject:Antimalarial drugs Eutectic mixtures Tailored excipients Solubility COSMO-RS Solid-liquid equilibria
Year:2026
Country:Portugal
Document type:master thesis
Access type:restricted access
Associated institution:Universidade Politécnica de Bragança
Language:English
Origin:Biblioteca Digital da UPB

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