Tuning the rheological properties of an ammonium methacrylate copolymer for the design of adhesives suitable for transdermal patches
Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with t...
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Veröffentlicht in: | European journal of pharmaceutical sciences 2018-01, Vol.111, p.238-246 |
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description | Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with tributyl citrate (TBC) or triacetin (TRI) in order to design a pressure sensitive adhesive suitable for transdermal patch preparation. The patch adhesive properties (i.e. tack, peel adhesion and shear adhesion) as well as its in vitro biopharmaceutical performances were determined after loading ibuprofen, ketoprofen or flurbiprofen. The addition of 40–60% w/w TBC or 40–50% w/w TRI to EuRL permitted to obtain matrices with the desired adhesive properties. Moreover, the increase of plasticizer content and loading of the drug reduced the relaxation time (τR). Consequently, the shear adhesion values decreased and the in vitro drug release constants (k) increased. Indeed, the k values from patches containing TBC were lower than the corresponding with TRI because of the lower fluidity of such matrices. In conclusion, the 60/40 EuRL/TBC binary blend is suitable for the design of transdermal patches since the in vitro permeability of the three selected drugs appeared comparable to those described in literature for marketed products.
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doi_str_mv | 10.1016/j.ejps.2017.10.006 |
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[Display omitted]</description><identifier>ISSN: 0928-0987</identifier><identifier>EISSN: 1879-0720</identifier><identifier>DOI: 10.1016/j.ejps.2017.10.006</identifier><identifier>PMID: 28987537</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Adhesives - chemistry ; Ammonium Compounds - chemistry ; Condensed Matter ; Drug release ; Eudragit RL ; Methacrylates - chemistry ; Models, Chemical ; Physics ; Polyurethanes ; Pressure-sensitive adhesives ; Rheology ; Skin permeation ; Soft Condensed Matter ; Transdermal Patch ; Transdermal patches</subject><ispartof>European journal of pharmaceutical sciences, 2018-01, Vol.111, p.238-246</ispartof><rights>2017 Elsevier B.V.</rights><rights>Copyright © 2017 Elsevier B.V. All rights reserved.</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-6936a7eb084f3d15848411fb45794b2811681abe73f965cbc8c4c6a2564fd6fc3</citedby><cites>FETCH-LOGICAL-c390t-6936a7eb084f3d15848411fb45794b2811681abe73f965cbc8c4c6a2564fd6fc3</cites><orcidid>0000-0003-3560-291X ; 0000-0002-0177-9680</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ejps.2017.10.006$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,780,784,885,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28987537$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.science/hal-02076931$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Quaroni, Gaia M.G.</creatorcontrib><creatorcontrib>Gennari, Chiara G.M.</creatorcontrib><creatorcontrib>Cilurzo, Francesco</creatorcontrib><creatorcontrib>Ducouret, Guylaine</creatorcontrib><creatorcontrib>Creton, Costantino</creatorcontrib><creatorcontrib>Minghetti, Paola</creatorcontrib><title>Tuning the rheological properties of an ammonium methacrylate copolymer for the design of adhesives suitable for transdermal patches</title><title>European journal of pharmaceutical sciences</title><addtitle>Eur J Pharm Sci</addtitle><description>Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with tributyl citrate (TBC) or triacetin (TRI) in order to design a pressure sensitive adhesive suitable for transdermal patch preparation. The patch adhesive properties (i.e. tack, peel adhesion and shear adhesion) as well as its in vitro biopharmaceutical performances were determined after loading ibuprofen, ketoprofen or flurbiprofen. The addition of 40–60% w/w TBC or 40–50% w/w TRI to EuRL permitted to obtain matrices with the desired adhesive properties. Moreover, the increase of plasticizer content and loading of the drug reduced the relaxation time (τR). Consequently, the shear adhesion values decreased and the in vitro drug release constants (k) increased. Indeed, the k values from patches containing TBC were lower than the corresponding with TRI because of the lower fluidity of such matrices. In conclusion, the 60/40 EuRL/TBC binary blend is suitable for the design of transdermal patches since the in vitro permeability of the three selected drugs appeared comparable to those described in literature for marketed products.
[Display omitted]</description><subject>Adhesives - chemistry</subject><subject>Ammonium Compounds - chemistry</subject><subject>Condensed Matter</subject><subject>Drug release</subject><subject>Eudragit RL</subject><subject>Methacrylates - chemistry</subject><subject>Models, Chemical</subject><subject>Physics</subject><subject>Polyurethanes</subject><subject>Pressure-sensitive adhesives</subject><subject>Rheology</subject><subject>Skin permeation</subject><subject>Soft Condensed Matter</subject><subject>Transdermal Patch</subject><subject>Transdermal patches</subject><issn>0928-0987</issn><issn>1879-0720</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc1u1DAURi0EotPCC7BAXsIig50f25HYVBW0SCOxKWvLca4nHtlxsJORZs-D4zSlS1a2Pp17rnQ_hD5QsqeEsi-nPZymtC8J5TnYE8JeoR0VvC0IL8lrtCNtKQrSCn6FrlM6kUwITt6iq1LksKn4Dv15XEY7HvE8AI4DBBeOViuHpxgmiLOFhIPBasTK-zDaxWMP86B0vDg1A9ZhCu7iIWIT4pOkh2SP49NQP-T_ORvSYmfVOdigqMbUQ_TrFjXrDL1Db4xyCd4_vzfo1_dvj3cPxeHn_Y-720Ohq5bMBWsrpjh0RNSm6mkjalFTarq64W3dlYJSJqjqgFemZY3utNC1ZqpsWG16ZnR1gz5v3kE5OUXrVbzIoKx8uD3INSMl4XkLPdPMftrYfInfC6RZeps0OKdGCEuStK1bIhrOWUbLDdUxpBTBvLgpkWtT8iTXpuTa1JrlHvLQx2f_0nnoX0b-VZOBrxsA-SJnC1EmbWHU0NsIepZ9sP_z_wXwQabI</recordid><startdate>20180101</startdate><enddate>20180101</enddate><creator>Quaroni, Gaia M.G.</creator><creator>Gennari, Chiara G.M.</creator><creator>Cilurzo, Francesco</creator><creator>Ducouret, Guylaine</creator><creator>Creton, Costantino</creator><creator>Minghetti, Paola</creator><general>Elsevier B.V</general><general>Elsevier</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>7X8</scope><scope>1XC</scope><orcidid>https://orcid.org/0000-0003-3560-291X</orcidid><orcidid>https://orcid.org/0000-0002-0177-9680</orcidid></search><sort><creationdate>20180101</creationdate><title>Tuning the rheological properties of an ammonium methacrylate copolymer for the design of adhesives suitable for transdermal patches</title><author>Quaroni, Gaia M.G. ; Gennari, Chiara G.M. ; Cilurzo, Francesco ; Ducouret, Guylaine ; Creton, Costantino ; Minghetti, Paola</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-6936a7eb084f3d15848411fb45794b2811681abe73f965cbc8c4c6a2564fd6fc3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Adhesives - chemistry</topic><topic>Ammonium Compounds - chemistry</topic><topic>Condensed Matter</topic><topic>Drug release</topic><topic>Eudragit RL</topic><topic>Methacrylates - chemistry</topic><topic>Models, Chemical</topic><topic>Physics</topic><topic>Polyurethanes</topic><topic>Pressure-sensitive adhesives</topic><topic>Rheology</topic><topic>Skin permeation</topic><topic>Soft Condensed Matter</topic><topic>Transdermal Patch</topic><topic>Transdermal patches</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Quaroni, Gaia M.G.</creatorcontrib><creatorcontrib>Gennari, Chiara G.M.</creatorcontrib><creatorcontrib>Cilurzo, Francesco</creatorcontrib><creatorcontrib>Ducouret, Guylaine</creatorcontrib><creatorcontrib>Creton, Costantino</creatorcontrib><creatorcontrib>Minghetti, Paola</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>European journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Quaroni, Gaia M.G.</au><au>Gennari, Chiara G.M.</au><au>Cilurzo, Francesco</au><au>Ducouret, Guylaine</au><au>Creton, Costantino</au><au>Minghetti, Paola</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Tuning the rheological properties of an ammonium methacrylate copolymer for the design of adhesives suitable for transdermal patches</atitle><jtitle>European journal of pharmaceutical sciences</jtitle><addtitle>Eur J Pharm Sci</addtitle><date>2018-01-01</date><risdate>2018</risdate><volume>111</volume><spage>238</spage><epage>246</epage><pages>238-246</pages><issn>0928-0987</issn><eissn>1879-0720</eissn><abstract>Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with tributyl citrate (TBC) or triacetin (TRI) in order to design a pressure sensitive adhesive suitable for transdermal patch preparation. The patch adhesive properties (i.e. tack, peel adhesion and shear adhesion) as well as its in vitro biopharmaceutical performances were determined after loading ibuprofen, ketoprofen or flurbiprofen. The addition of 40–60% w/w TBC or 40–50% w/w TRI to EuRL permitted to obtain matrices with the desired adhesive properties. Moreover, the increase of plasticizer content and loading of the drug reduced the relaxation time (τR). Consequently, the shear adhesion values decreased and the in vitro drug release constants (k) increased. Indeed, the k values from patches containing TBC were lower than the corresponding with TRI because of the lower fluidity of such matrices. In conclusion, the 60/40 EuRL/TBC binary blend is suitable for the design of transdermal patches since the in vitro permeability of the three selected drugs appeared comparable to those described in literature for marketed products.
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subjects | Adhesives - chemistry Ammonium Compounds - chemistry Condensed Matter Drug release Eudragit RL Methacrylates - chemistry Models, Chemical Physics Polyurethanes Pressure-sensitive adhesives Rheology Skin permeation Soft Condensed Matter Transdermal Patch Transdermal patches |
title | Tuning the rheological properties of an ammonium methacrylate copolymer for the design of adhesives suitable for transdermal patches |
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