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

Abstract

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:
Research Org.:
Lawrence Berkeley National Lab. (LBNL), Berkeley, CA (United States); Energy Frontier Research Centers (EFRC) (United States). Center for Gas Separations Relevant to Clean Energy Technologies (CGS)
Sponsoring Org.:
USDOE Office of Science (SC), Basic Energy Sciences (BES) (SC-22)
OSTI Identifier:
1420116
Alternate Identifier(s):
OSTI ID: 1407822
Grant/Contract Number:  
AC02-05CH11231; SC0001015; AC02-06CH11357
Resource Type:
Journal Article: 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
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

Citation Formats

Levine, Dana J., Gonzalez, Miguel I., Legendre, Christina M., Runcevski, Tomce, Oktawiec, Julia, Colwell, Kristen A., and Long, Jeffrey R. Calcium Coordination Solids for pH-Triggered Release of Olsalazine. United States: N. p., 2017. Web. doi:10.1002/cmdc.201700540.
Levine, Dana J., Gonzalez, Miguel I., Legendre, Christina M., Runcevski, Tomce, Oktawiec, Julia, Colwell, Kristen A., & Long, Jeffrey R. Calcium Coordination Solids for pH-Triggered Release of Olsalazine. United States. doi:10.1002/cmdc.201700540.
Levine, Dana J., Gonzalez, Miguel I., Legendre, Christina M., Runcevski, Tomce, Oktawiec, Julia, Colwell, Kristen A., and Long, Jeffrey R. Tue . "Calcium Coordination Solids for pH-Triggered Release of Olsalazine". United States. doi:10.1002/cmdc.201700540. https://www.osti.gov/servlets/purl/1420116.
@article{osti_1420116,
title = {Calcium Coordination Solids for pH-Triggered Release of Olsalazine},
author = {Levine, Dana J. and Gonzalez, Miguel I. and Legendre, Christina M. and Runcevski, Tomce and Oktawiec, Julia and Colwell, Kristen A. and Long, Jeffrey R.},
abstractNote = {Here, 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 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.},
doi = {10.1002/cmdc.201700540},
journal = {ChemMedChem(Print)},
number = 21,
volume = 12,
place = {United States},
year = {Tue Sep 12 00:00:00 EDT 2017},
month = {Tue Sep 12 00:00:00 EDT 2017}
}

Journal Article:
Free Publicly Available Full Text
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