Predictive relationships for the effects of triglyceride ester concentration and water uptake on solubility and partitioning of small molecules into lipid vehicles

Journal of Pharmaceutical Sciences
Yichen CaoBradley D Anderson

Abstract

The ability to predict drug solubility and partitioning in triglyceride solvents from the chemical structures of the solute and the triglyceride would be highly useful in drug formulation development and in screening drug candidates for lipid solubility and possibly drug bioavailability. This study explores the role of triglyceride ester concentration on small molecule partitioning between lipid vehicles and water, including the effect of ester concentration on water uptake. The influence of solvated water is further examined in studies of small molecule solubility in dry and water saturated lipid vehicles varying in triglyceride ester concentration. A series of model solutes with varying hydrogen bond donating/accepting abilities was chosen for this study while triglyceride ester concentrations were varied by using squalane/tricaprylin solvent mixtures. General linear free energy solvation relationships having the form utilized previously by Abraham were obtained at each solvent composition. An examination of the solvent descriptors indicated that those descriptors representing the sensitivity of the solvent to the solute dipolarity/polarizability, s, and to the hydrogen bond acidity of the solute, a, vary systematically with ...Continue Reading

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Citations

May 21, 2005·Pharmaceutical Research·Laura M LandPaul Michael Bummer
Jun 19, 2013·Pharmaceutical Research·Linda C PerssonChristel A S Bergström
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Apr 4, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nadine Monika FranckeHeike Bunjes
Jun 15, 2018·Langmuir : the ACS Journal of Surfaces and Colloids·Mona S MinkaraJ Ilja Siepmann

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