3 years ago

Calcium Coordination Solids for pH-Triggered Release of Olsalazine

Miguel I. Gonzalez, Tomče Runčevski, Julia Oktawiec, Jeffrey R. Long, Kristen A. Colwell, Dana Jaya Levine, Christina M. Legendre
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)·4H₂O chains, two-dimensional Ca(H₂olz)·2H₂O 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)·xH₂O (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 compared 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.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700540

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