In vitro evaluation of thio-poly acrylic acid for intraoral delivery
Context: Intraoral drug delivery as mucosal delivery pathway provides a huge platform in the pharmaceutical field. Objective: Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery. Materials and methods: Mediated by carbodiimide, c...
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Veröffentlicht in: | Drug delivery 2016-07, Vol.23 (6), p.2065-2073 |
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creator | Laffleur, Flavia Leder, Nina Barthelmes, Jan |
description | Context: Intraoral drug delivery as mucosal delivery pathway provides a huge platform in the pharmaceutical field.
Objective: Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery.
Materials and methods: Mediated by carbodiimide, cysteine was covalently attached to poly acrylic acid. This thiomer was assessed with regard to cytotoxicity, stability, mucoadhesion, and rheology as well as release behavior of Lidocaine.
Results: Stability assays of thio-poly acrylic acid were complying with United States Pharmacopeia requirements. Mucoadhesion assay such as tensile (total work of adhesion), bioadhesion, rotating cylinder revealed as this thiomer was superior in comparison to non-thiolated poly acrylic acid with 7.61-fold, 2.8-fold, 5.61-fold improvement, respectively without any toxic effect. The cell viability exhibited over 90% after incubation time of 3 h and 24 h respectively. Lidocaine release showed 1.98-fold more controlled release over 3 h in comparison to unmodified poly acrylic acid.
Conclusion: Taken the findings in consideration, thio-poly acrylic acid provides excellent stability, controlled release, and superior mucoadhesive features. The prolonged residence time of thio-poly acrylic acid represents a pillar in the buccal drug delivery. |
doi_str_mv | 10.3109/10717544.2015.1122673 |
format | Article |
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Objective: Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery.
Materials and methods: Mediated by carbodiimide, cysteine was covalently attached to poly acrylic acid. This thiomer was assessed with regard to cytotoxicity, stability, mucoadhesion, and rheology as well as release behavior of Lidocaine.
Results: Stability assays of thio-poly acrylic acid were complying with United States Pharmacopeia requirements. Mucoadhesion assay such as tensile (total work of adhesion), bioadhesion, rotating cylinder revealed as this thiomer was superior in comparison to non-thiolated poly acrylic acid with 7.61-fold, 2.8-fold, 5.61-fold improvement, respectively without any toxic effect. The cell viability exhibited over 90% after incubation time of 3 h and 24 h respectively. Lidocaine release showed 1.98-fold more controlled release over 3 h in comparison to unmodified poly acrylic acid.
Conclusion: Taken the findings in consideration, thio-poly acrylic acid provides excellent stability, controlled release, and superior mucoadhesive features. The prolonged residence time of thio-poly acrylic acid represents a pillar in the buccal drug delivery.</description><identifier>ISSN: 1071-7544</identifier><identifier>EISSN: 1521-0464</identifier><identifier>DOI: 10.3109/10717544.2015.1122673</identifier><identifier>PMID: 26666520</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Acrylates - chemistry ; Acrylates - metabolism ; Cystine - analogs & derivatives ; Cystine - chemistry ; Cystine - metabolism ; Delayed-Action Preparations - chemistry ; Delayed-Action Preparations - metabolism ; Delayed-Action Preparations - pharmacokinetics ; Drug Delivery Systems ; Drug Stability ; Humans ; Intraoral drug delivery ; Lidocaine ; Lidocaine - chemistry ; Lidocaine - metabolism ; Lidocaine - pharmacokinetics ; mucoadhesion ; Rheology ; thio-poly acrylic acid ; thiomer</subject><ispartof>Drug delivery, 2016-07, Vol.23 (6), p.2065-2073</ispartof><rights>2015 Informa UK Limited, trading as Taylor & Francis Group. 2015</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-26ae4b801d8aae00a9872506a7871565b475498af6b9c025e64f68e7d438ba933</citedby><cites>FETCH-LOGICAL-c366t-26ae4b801d8aae00a9872506a7871565b475498af6b9c025e64f68e7d438ba933</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26666520$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Laffleur, Flavia</creatorcontrib><creatorcontrib>Leder, Nina</creatorcontrib><creatorcontrib>Barthelmes, Jan</creatorcontrib><title>In vitro evaluation of thio-poly acrylic acid for intraoral delivery</title><title>Drug delivery</title><addtitle>Drug Deliv</addtitle><description>Context: Intraoral drug delivery as mucosal delivery pathway provides a huge platform in the pharmaceutical field.
Objective: Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery.
Materials and methods: Mediated by carbodiimide, cysteine was covalently attached to poly acrylic acid. This thiomer was assessed with regard to cytotoxicity, stability, mucoadhesion, and rheology as well as release behavior of Lidocaine.
Results: Stability assays of thio-poly acrylic acid were complying with United States Pharmacopeia requirements. Mucoadhesion assay such as tensile (total work of adhesion), bioadhesion, rotating cylinder revealed as this thiomer was superior in comparison to non-thiolated poly acrylic acid with 7.61-fold, 2.8-fold, 5.61-fold improvement, respectively without any toxic effect. The cell viability exhibited over 90% after incubation time of 3 h and 24 h respectively. Lidocaine release showed 1.98-fold more controlled release over 3 h in comparison to unmodified poly acrylic acid.
Conclusion: Taken the findings in consideration, thio-poly acrylic acid provides excellent stability, controlled release, and superior mucoadhesive features. The prolonged residence time of thio-poly acrylic acid represents a pillar in the buccal drug delivery.</description><subject>Acrylates - chemistry</subject><subject>Acrylates - metabolism</subject><subject>Cystine - analogs & derivatives</subject><subject>Cystine - chemistry</subject><subject>Cystine - metabolism</subject><subject>Delayed-Action Preparations - chemistry</subject><subject>Delayed-Action Preparations - metabolism</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Drug Delivery Systems</subject><subject>Drug Stability</subject><subject>Humans</subject><subject>Intraoral drug delivery</subject><subject>Lidocaine</subject><subject>Lidocaine - chemistry</subject><subject>Lidocaine - metabolism</subject><subject>Lidocaine - pharmacokinetics</subject><subject>mucoadhesion</subject><subject>Rheology</subject><subject>thio-poly acrylic acid</subject><subject>thiomer</subject><issn>1071-7544</issn><issn>1521-0464</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtOwzAQRS0EoqXwCSD_QMrYsR1nByqvSpXYwDqaJI4wcuPKSYPy9zhqy5LZ3FncO49DyC2DZcogv2eQsUwKseTA5JIxzlWWnpE5k5wlIJQ4j330JJNpRq667hsANOPyksy4iiU5zMnTuqWD7YOnZkC3x976lvqG9l_WJzvvRopVGJ2totqaNj5Q2_YBfUBHa-PsYMJ4TS4adJ25OeqCfL48f6zeks3763r1uEmqVKk-4QqNKDWwWiMaAMx1xiUozHTGpJKliLfmGhtV5hVwaZRolDZZLVJdYp6mCyIPc6vguy6YptgFu8UwFgyKiUpxolJMVIojlZi7O-R2-3Jr6r_UCUM0PBwMto0fbvHHB1cXPY7OhyZgW9lumv_fjl8SSHBy</recordid><startdate>20160723</startdate><enddate>20160723</enddate><creator>Laffleur, Flavia</creator><creator>Leder, Nina</creator><creator>Barthelmes, Jan</creator><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></search><sort><creationdate>20160723</creationdate><title>In vitro evaluation of thio-poly acrylic acid for intraoral delivery</title><author>Laffleur, Flavia ; Leder, Nina ; Barthelmes, Jan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-26ae4b801d8aae00a9872506a7871565b475498af6b9c025e64f68e7d438ba933</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Acrylates - chemistry</topic><topic>Acrylates - metabolism</topic><topic>Cystine - analogs & derivatives</topic><topic>Cystine - chemistry</topic><topic>Cystine - metabolism</topic><topic>Delayed-Action Preparations - chemistry</topic><topic>Delayed-Action Preparations - metabolism</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Drug Delivery Systems</topic><topic>Drug Stability</topic><topic>Humans</topic><topic>Intraoral drug delivery</topic><topic>Lidocaine</topic><topic>Lidocaine - chemistry</topic><topic>Lidocaine - metabolism</topic><topic>Lidocaine - pharmacokinetics</topic><topic>mucoadhesion</topic><topic>Rheology</topic><topic>thio-poly acrylic acid</topic><topic>thiomer</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Laffleur, Flavia</creatorcontrib><creatorcontrib>Leder, Nina</creatorcontrib><creatorcontrib>Barthelmes, Jan</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Drug delivery</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Laffleur, Flavia</au><au>Leder, Nina</au><au>Barthelmes, Jan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In vitro evaluation of thio-poly acrylic acid for intraoral delivery</atitle><jtitle>Drug delivery</jtitle><addtitle>Drug Deliv</addtitle><date>2016-07-23</date><risdate>2016</risdate><volume>23</volume><issue>6</issue><spage>2065</spage><epage>2073</epage><pages>2065-2073</pages><issn>1071-7544</issn><eissn>1521-0464</eissn><abstract>Context: Intraoral drug delivery as mucosal delivery pathway provides a huge platform in the pharmaceutical field.
Objective: Combining mucoadhesiveness and controlled release of thio-poly acrylic acid as advanced excipient for buccal drug delivery.
Materials and methods: Mediated by carbodiimide, cysteine was covalently attached to poly acrylic acid. This thiomer was assessed with regard to cytotoxicity, stability, mucoadhesion, and rheology as well as release behavior of Lidocaine.
Results: Stability assays of thio-poly acrylic acid were complying with United States Pharmacopeia requirements. Mucoadhesion assay such as tensile (total work of adhesion), bioadhesion, rotating cylinder revealed as this thiomer was superior in comparison to non-thiolated poly acrylic acid with 7.61-fold, 2.8-fold, 5.61-fold improvement, respectively without any toxic effect. The cell viability exhibited over 90% after incubation time of 3 h and 24 h respectively. Lidocaine release showed 1.98-fold more controlled release over 3 h in comparison to unmodified poly acrylic acid.
Conclusion: Taken the findings in consideration, thio-poly acrylic acid provides excellent stability, controlled release, and superior mucoadhesive features. The prolonged residence time of thio-poly acrylic acid represents a pillar in the buccal drug delivery.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>26666520</pmid><doi>10.3109/10717544.2015.1122673</doi><tpages>9</tpages></addata></record> |
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subjects | Acrylates - chemistry Acrylates - metabolism Cystine - analogs & derivatives Cystine - chemistry Cystine - metabolism Delayed-Action Preparations - chemistry Delayed-Action Preparations - metabolism Delayed-Action Preparations - pharmacokinetics Drug Delivery Systems Drug Stability Humans Intraoral drug delivery Lidocaine Lidocaine - chemistry Lidocaine - metabolism Lidocaine - pharmacokinetics mucoadhesion Rheology thio-poly acrylic acid thiomer |
title | In vitro evaluation of thio-poly acrylic acid for intraoral delivery |
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