Aliphatic polyester terpolymers for stent coating and drug elution: Effect of polymer composition on drug solubility and release
Ring-opening terpolymerization of L-lactide (LA), -caprolactone (CL), and glycolide (GA) was performed in the presence of tin (II) 2-ethylhexanoate at 170°C. Random terpolyesters with weight-average molecular weight up to 130,000 g/mol were obtained. These terpolyesters, especially those with LA:CL:...
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Veröffentlicht in: | Drug delivery 2009-08, Vol.16 (6), p.304-311 |
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creator | Chan-Seng, Delphine Ranganathan, T. Zhang, Xiongfei Tang, Yiwen Lin, Qing Kleiner, Lothar Emrick, Todd |
description | Ring-opening terpolymerization of L-lactide (LA), -caprolactone (CL), and glycolide (GA) was performed in the presence of tin (II) 2-ethylhexanoate at 170°C. Random terpolyesters with weight-average molecular weight up to 130,000 g/mol were obtained. These terpolyesters, especially those with LA:CL:GA composition of 3:1:1, provided good coating integrity following spraying onto bare metal stents. The semi-synthetic macrolide immunosuppressant, everolimus, was incorporated into the terpolyester coating, and its release from the stent was evaluated. Unlike PLLA homopolymers, which are immiscible with the drug and non-optimal for controlled release, these terpolymers gave excellent control in a screening study, by tuning terpolymer molecular weight, relative monomer ratio, and drug-to-polymer ratio. Adjusting the polymer properties to improve drug solubility (or miscibility) in the polymer coating was found beneficial to the release profile. |
doi_str_mv | 10.1080/10717540902999653 |
format | Article |
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Random terpolyesters with weight-average molecular weight up to 130,000 g/mol were obtained. These terpolyesters, especially those with LA:CL:GA composition of 3:1:1, provided good coating integrity following spraying onto bare metal stents. The semi-synthetic macrolide immunosuppressant, everolimus, was incorporated into the terpolyester coating, and its release from the stent was evaluated. Unlike PLLA homopolymers, which are immiscible with the drug and non-optimal for controlled release, these terpolymers gave excellent control in a screening study, by tuning terpolymer molecular weight, relative monomer ratio, and drug-to-polymer ratio. Adjusting the polymer properties to improve drug solubility (or miscibility) in the polymer coating was found beneficial to the release profile.</description><identifier>ISSN: 1071-7544</identifier><identifier>EISSN: 1521-0464</identifier><identifier>DOI: 10.1080/10717540902999653</identifier><identifier>PMID: 19606944</identifier><language>eng</language><publisher>England: Informa UK Ltd</publisher><subject>coating ; Drug Delivery Systems - methods ; drug release ; Drug-Eluting Stents ; everolimus ; Polyester ; Polyesters - chemistry ; Polyesters - pharmacokinetics ; Polymers - chemistry ; Polymers - pharmacokinetics ; Solubility ; stent</subject><ispartof>Drug delivery, 2009-08, Vol.16 (6), p.304-311</ispartof><rights>2009 Informa UK Ltd 2009</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-596290f29dc3aed377970b351a3e95dd84af84d808ae479606e6ce5f1a0d1663</citedby><cites>FETCH-LOGICAL-c366t-596290f29dc3aed377970b351a3e95dd84af84d808ae479606e6ce5f1a0d1663</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.1080/10717540902999653$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.1080/10717540902999653$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,59620,60409,61194,61375</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19606944$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chan-Seng, Delphine</creatorcontrib><creatorcontrib>Ranganathan, T.</creatorcontrib><creatorcontrib>Zhang, Xiongfei</creatorcontrib><creatorcontrib>Tang, Yiwen</creatorcontrib><creatorcontrib>Lin, Qing</creatorcontrib><creatorcontrib>Kleiner, Lothar</creatorcontrib><creatorcontrib>Emrick, Todd</creatorcontrib><title>Aliphatic polyester terpolymers for stent coating and drug elution: Effect of polymer composition on drug solubility and release</title><title>Drug delivery</title><addtitle>Drug Deliv</addtitle><description>Ring-opening terpolymerization of L-lactide (LA), -caprolactone (CL), and glycolide (GA) was performed in the presence of tin (II) 2-ethylhexanoate at 170°C. Random terpolyesters with weight-average molecular weight up to 130,000 g/mol were obtained. These terpolyesters, especially those with LA:CL:GA composition of 3:1:1, provided good coating integrity following spraying onto bare metal stents. The semi-synthetic macrolide immunosuppressant, everolimus, was incorporated into the terpolyester coating, and its release from the stent was evaluated. Unlike PLLA homopolymers, which are immiscible with the drug and non-optimal for controlled release, these terpolymers gave excellent control in a screening study, by tuning terpolymer molecular weight, relative monomer ratio, and drug-to-polymer ratio. Adjusting the polymer properties to improve drug solubility (or miscibility) in the polymer coating was found beneficial to the release profile.</description><subject>coating</subject><subject>Drug Delivery Systems - methods</subject><subject>drug release</subject><subject>Drug-Eluting Stents</subject><subject>everolimus</subject><subject>Polyester</subject><subject>Polyesters - chemistry</subject><subject>Polyesters - pharmacokinetics</subject><subject>Polymers - chemistry</subject><subject>Polymers - pharmacokinetics</subject><subject>Solubility</subject><subject>stent</subject><issn>1071-7544</issn><issn>1521-0464</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc9rFDEUx4Motlb_AC-Sk55Gk8mPmaiXUtoqFLz0HrLJSzclMxmTDLI3_3Sz3QURYSEhL3mf75e89xB6S8lHSkbyiZKBDoITRXqllBTsGTqnoqcd4ZI_b3HLdw3gZ-hVKY-EkJH24iU6o0oSqTg_R78vY1i2pgaLlxR3UCpk3Pb-MkEu2KeM2-NcsU0Nmx-wmR12eX3AENca0vwZX3sPtuLk8VHW2GlJJezTuK0nvKS4bkIMdfdkkSGCKfAavfAmFnhzPC_Q_c31_dW37u7H7fery7vOMilrJ5TsFfG9cpYZcGwY1EA2TFDDQAnnRm78yN1IRgN82JcH0oLw1BBHpWQX6MPBdsnp59rK1FMoFmI0M6S16IEx2lPeD418f5LsSeshoaKB9ADanErJ4PWSw2TyTlOi9_PR_82nad4dzdfNBO6v4jiQBnw9AGFunZ_Mr5Sj09XsYso-m9mGotkp_y__yLdgYt1ak0E_pjXPrcMnfvcHeUSyZw</recordid><startdate>200908</startdate><enddate>200908</enddate><creator>Chan-Seng, Delphine</creator><creator>Ranganathan, T.</creator><creator>Zhang, Xiongfei</creator><creator>Tang, Yiwen</creator><creator>Lin, Qing</creator><creator>Kleiner, Lothar</creator><creator>Emrick, Todd</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>200908</creationdate><title>Aliphatic polyester terpolymers for stent coating and drug elution: Effect of polymer composition on drug solubility and release</title><author>Chan-Seng, Delphine ; Ranganathan, T. ; Zhang, Xiongfei ; Tang, Yiwen ; Lin, Qing ; Kleiner, Lothar ; Emrick, Todd</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-596290f29dc3aed377970b351a3e95dd84af84d808ae479606e6ce5f1a0d1663</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>coating</topic><topic>Drug Delivery Systems - methods</topic><topic>drug release</topic><topic>Drug-Eluting Stents</topic><topic>everolimus</topic><topic>Polyester</topic><topic>Polyesters - chemistry</topic><topic>Polyesters - pharmacokinetics</topic><topic>Polymers - chemistry</topic><topic>Polymers - pharmacokinetics</topic><topic>Solubility</topic><topic>stent</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chan-Seng, Delphine</creatorcontrib><creatorcontrib>Ranganathan, T.</creatorcontrib><creatorcontrib>Zhang, Xiongfei</creatorcontrib><creatorcontrib>Tang, Yiwen</creatorcontrib><creatorcontrib>Lin, Qing</creatorcontrib><creatorcontrib>Kleiner, Lothar</creatorcontrib><creatorcontrib>Emrick, Todd</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Drug delivery</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chan-Seng, Delphine</au><au>Ranganathan, T.</au><au>Zhang, Xiongfei</au><au>Tang, Yiwen</au><au>Lin, Qing</au><au>Kleiner, Lothar</au><au>Emrick, Todd</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Aliphatic polyester terpolymers for stent coating and drug elution: Effect of polymer composition on drug solubility and release</atitle><jtitle>Drug delivery</jtitle><addtitle>Drug Deliv</addtitle><date>2009-08</date><risdate>2009</risdate><volume>16</volume><issue>6</issue><spage>304</spage><epage>311</epage><pages>304-311</pages><issn>1071-7544</issn><eissn>1521-0464</eissn><abstract>Ring-opening terpolymerization of L-lactide (LA), -caprolactone (CL), and glycolide (GA) was performed in the presence of tin (II) 2-ethylhexanoate at 170°C. Random terpolyesters with weight-average molecular weight up to 130,000 g/mol were obtained. These terpolyesters, especially those with LA:CL:GA composition of 3:1:1, provided good coating integrity following spraying onto bare metal stents. The semi-synthetic macrolide immunosuppressant, everolimus, was incorporated into the terpolyester coating, and its release from the stent was evaluated. Unlike PLLA homopolymers, which are immiscible with the drug and non-optimal for controlled release, these terpolymers gave excellent control in a screening study, by tuning terpolymer molecular weight, relative monomer ratio, and drug-to-polymer ratio. Adjusting the polymer properties to improve drug solubility (or miscibility) in the polymer coating was found beneficial to the release profile.</abstract><cop>England</cop><pub>Informa UK Ltd</pub><pmid>19606944</pmid><doi>10.1080/10717540902999653</doi><tpages>8</tpages></addata></record> |
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source | MEDLINE; Taylor & Francis Journals Complete; EZB Electronic Journals Library |
subjects | coating Drug Delivery Systems - methods drug release Drug-Eluting Stents everolimus Polyester Polyesters - chemistry Polyesters - pharmacokinetics Polymers - chemistry Polymers - pharmacokinetics Solubility stent |
title | Aliphatic polyester terpolymers for stent coating and drug elution: Effect of polymer composition on drug solubility and release |
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