PMID- 20524194 OWN - NLM STAT- MEDLINE DCOM- 20100909 LR - 20200930 IS - 1552-4981 (Electronic) IS - 1552-4973 (Linking) VI - 94 IP - 1 DP - 2010 Jul TI - Synthesis and anticoagulant activity of heparin immobilized "end-on" to polystyrene microspheres coated with end-group activated polyethylene oxide. PG - 187-95 LID - 10.1002/jbm.b.31640 [doi] AB - Thiol groups were introduced to unfractionated heparin (UFH) and end-aminated heparin (HepNH(2)) by reaction with 2-iminothiolane under conditions favoring selective modification of terminal over primary amines. End-thiolated heparin retained anticoagulant activity as shown by the activated partial thromboplastin time (aPTT) and anti-Factor Xa (anti-FXa) assays. Thiolated heparins were linked to pyridyl-disulfide activated poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymers adsorbed to 1.15-mum polystyrene microspheres. Surface loadings were similarly low for each type of thiolated heparin. No anticoagulant activity was observed with aPTT assays of heparinized microspheres, due either to the presence of an insufficient amount of immobilized heparin, or to steric constraints inhibiting the formation of a functional heparin-antihrombin complex. However, immobilized heparin retained substantial anti-FXa activity, with significantly greater activity exhibited by the end-thiolated HepNH(2) than the internally (randomly) thiolated UFH. CI - (c) 2010 Wiley Periodicals, Inc. FAU - Fry, Allyson K AU - Fry AK AD - School of Chemical, Biological and Environmental Engineering, Oregon State University, Corvallis, Oregon 97331, USA. FAU - Schilke, Karl F AU - Schilke KF FAU - McGuire, Joseph AU - McGuire J FAU - Bird, Karyn E AU - Bird KE LA - eng PT - Evaluation Study PT - Journal Article PT - Research Support, U.S. Gov't, Non-P.H.S. PL - United States TA - J Biomed Mater Res B Appl Biomater JT - Journal of biomedical materials research. Part B, Applied biomaterials JID - 101234238 RN - 0 (Amines) RN - 0 (Anticoagulants) RN - 0 (Biocompatible Materials) RN - 0 (Factor Xa Inhibitors) RN - 0 (PEO-PPO-PEO) RN - 0 (Polystyrenes) RN - 0 (Propylene Glycols) RN - 0 (Sulfhydryl Compounds) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 9005-49-6 (Heparin) SB - IM MH - Adsorption MH - Amines/chemistry MH - *Anticoagulants/chemistry/pharmacology MH - Biocompatible Materials/chemistry/pharmacology MH - Blood Coagulation/*drug effects MH - Factor Xa Inhibitors MH - *Heparin/chemistry/pharmacology MH - Humans MH - Materials Testing MH - *Microspheres MH - Molecular Structure MH - Partial Thromboplastin Time MH - Polyethylene Glycols/*chemistry MH - Polystyrenes/*chemistry MH - Propylene Glycols/chemistry MH - Sulfhydryl Compounds/chemistry EDAT- 2010/06/05 06:00 MHDA- 2010/09/10 06:00 CRDT- 2010/06/05 06:00 PHST- 2010/06/05 06:00 [entrez] PHST- 2010/06/05 06:00 [pubmed] PHST- 2010/09/10 06:00 [medline] AID - 10.1002/jbm.b.31640 [doi] PST - ppublish SO - J Biomed Mater Res B Appl Biomater. 2010 Jul;94(1):187-95. doi: 10.1002/jbm.b.31640.