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Calcium Coordination Solids for pH-Triggered Release of Olsalazine

  • Author(s): Levine, DJ
  • Gonzalez, MI
  • Legendre, CM
  • Runčevski, T
  • Oktawiec, J
  • Colwell, KA
  • Long, JR
  • et al.
Abstract

© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H4olz), an anti-inflammatory compound used for treatment of ulcerative colitis. The materials include one-dimensional Ca(H2olz)⋅4 H2O chains, two-dimensional Ca(H2olz)⋅2 H2O sheets, and a three-dimensional metal-organic framework Ca(H2olz)⋅2DMF (DMF=N,N-dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H2olz) phase when exposed to aqueous HCl. The compounds Ca(H2olz)⋅x H2O (x=0, 2, 4) were each pressed into pellets and exposed to simulated gastrointestinal fluids to mimic the passage of a pill from the acidic stomach to the pH-neutral intestines. All three calcium materials exhibited a delayed release of olsalazine relative to Na2(H2olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.

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