Journal
JOURNAL OF CONTROLLED RELEASE
Volume 96, Issue 2, Pages 301-307Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2004.02.013
Keywords
polyrotaxanes; calcium binding; trypsin inhibition
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Carboxyethylester-polyrotaxanes (CEE-polyrotaxanes) with the various number of CEE-modified alpha-cyclodextrins (CEE-alpha-CDs) were synthesized, and the effects of the number of CEE-alpha-CDs on calcium binding and trypsin inhibition were investigated. Calcium binding affinity was dependent on the density of the CEE groups accompanied with the number of alpha-CD threading in the CEE-polyrotaxanes. The high number of CEE-alpha-CDs leads to greater inhibition of trypsin activity than poly(acrylic acid), which is mainly due to the good calcium binding affinity. The CEE-polyrotaxane with the smallest number of CEE-alpha-CDs temporally interacted with trypsin, which was well correlated with the inhibition and recovery of trypsin activity. Therefore, the number of CEE-alpha-CDs in the CEE-polyrotaxanes can control the inhibition mechanism of trypsin activity. (C) 2004 Elsevier B.V. All rights reserved.
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