publication . Article . Other literature type . 2018

The Curious Case of the OZ439 Mesylate Salt: An Amphiphilic Antimalarial Drug with Diverse Solution and Solid State Structures

Clulow, Andrew J.; Salim, Malinda; Hawley, Adrian; Gilbert, Elliot P.; Boyd, Ben J.;
Open Access
  • Published: 20 Mar 2018 Journal: Molecular Pharmaceutics, volume 15, pages 2,027-2,035 (issn: 1543-8384, eissn: 1543-8392, Copyright policy)
  • Publisher: American Chemical Society (ACS)
Abstract
Efforts to develop orally administered drugs tend to place an exceptional focus on aqueous solubility as this is an essential criterion for their absorption in the gastrointestinal tract. In this work we examine the solid state behavior and solubility of OZ439, a promising single-dose cure for malaria being developed as the highly water-soluble mesylate salt. The aqueous phase behavior of the OZ439 mesylate salt was determined using a combination of small angle neutron and X-ray scattering (SANS and SAXS, respectively). It was found that this salt has low solubility at low concentrations with the drug largely precipitated in free base aggregates. However, with i...
Subjects
free text keywords: Molecular Medicine, Drug Discovery, Pharmaceutical Science, Solubility, Free base, Lamellar structure, Small-angle X-ray scattering, Amphiphile, Mesylate, chemistry.chemical_compound, chemistry, Inorganic chemistry, Micelle, Aqueous two-phase system, Biochemistry, Article, polymorph, self-assembly, micelles, scattering
Funded by
ARC| Discovery Projects - Grant ID: DP160102906
Project
  • Funder: Australian Research Council (ARC) (ARC)
  • Project Code: DP160102906
  • Funding stream: Discovery Projects

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publication . Article . Other literature type . 2018

The Curious Case of the OZ439 Mesylate Salt: An Amphiphilic Antimalarial Drug with Diverse Solution and Solid State Structures

Clulow, Andrew J.; Salim, Malinda; Hawley, Adrian; Gilbert, Elliot P.; Boyd, Ben J.;