UC Berkeley

Calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H₄ olz), an anti-inflammatory compound used for treatment of ulcerative colitis. The materials include one-dimensional Ca(H₂ olz)⋅4 H₂ O chains, two-dimensional Ca(H₂ olz)⋅2 H₂ O sheets, and a three-dimensional metal-organic framework Ca(H₂ olz)⋅2DMF (DMF=N,N-dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H₂ olz) phase when exposed to aqueous HCl. The compounds Ca(H₂ olz)⋅x H₂ O (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 (H₂ olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.