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This content will become publicly available on September 12, 2018

Title: Calcium Coordination Solids for pH-Triggered Release of Olsalazine

Here, calcium coordination solids were synthesized and evaluated for delivery of olsalazine (H 4olz), an anti-inflammatory compound used for treatment of ulcerative colitis. The materials include one-dimensional Ca(H 2olz)•4H 2O chains, two-dimensional Ca(H 2olz)•2H 2O sheets, and a three-dimensional metal-organic framework Ca(H 2olz)•2DMF (DMF= N,N-dimethylformamide). The framework undergoes structural changes in response to solvent, forming a dense Ca(H 2olz) phase when exposed to aqueous HCl. The compounds Ca(H 2olz)•xH 2O (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 Na 2(H 2olz), the commercial formulation, illustrating how formulation of a drug within an extended coordination solid can serve to tune its solubility and performance.
Authors:
ORCiD logo [1] ; ORCiD logo [2] ;  [2] ;  [3] ; ORCiD logo [2] ; ORCiD logo [2] ; ORCiD logo [3]
  1. Univ. of California, Berkeley, CA (United States); California Inst. of Technology (CalTech), Pasadena, CA (United States)
  2. Univ. of California, Berkeley, CA (United States)
  3. Univ. of California, Berkeley, CA (United States); Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States)
Publication Date:
Grant/Contract Number:
AC02-05CH11231; SC0001015; AC02-06CH11357
Type:
Accepted Manuscript
Journal Name:
ChemMedChem(Print)
Additional Journal Information:
Journal Name: ChemMedChem(Print); Journal Volume: 12; Journal Issue: 21; Journal ID: ISSN 1860-7179
Publisher:
ChemPubSoc Europe
Research Org:
Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States)
Sponsoring Org:
USDOE Office of Science (SC), Basic Energy Sciences (BES) (SC-22)
Country of Publication:
United States
Language:
English
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY; calcium; coordination polymers; crystal engineering; drug delivery; metal-organic frameworks
OSTI Identifier:
1420116
Alternate Identifier(s):
OSTI ID: 1407822