Design and evaluation of artificial receptors for the reversal of neuromuscular block
[Display omitted] Applying patient friendly and cost-efficient medications in healthcare will be a real challenge in the 21st century. Sugammadex is a selective, yet expensive agent used for the post-surgical reversal of neuromuscular block since 2008. A wide library of cyclodextrin-based follow-ups...
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| Veröffentlicht in: | International journal of pharmaceutics 2017-10, Vol.531 (2), p.512-520 |
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| container_issue | 2 |
| container_start_page | 512 |
| container_title | International journal of pharmaceutics |
| container_volume | 531 |
| creator | Sohajda, Tamás Fábián, Ákos Tuza, Kata Malanga, Milo Benkovics, Gábor Fülesdi, Béla Tassonyi, Edömér Szente, Lajos |
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Applying patient friendly and cost-efficient medications in healthcare will be a real challenge in the 21st century. Sugammadex is a selective, yet expensive agent used for the post-surgical reversal of neuromuscular block since 2008. A wide library of cyclodextrin-based follow-ups, having potentially similar affinity towards target aminosteroid type neuromuscular blocking agents has been established. Almost 20 compounds were assessed with respect to in vitro affinity against three commonly applied drugs. Based on the capillary electrophoretic screening, carboxymethylated and sulfobutylated gamma-cyclodextrin derivatives have the potential to be promising lead molecules for their affinity towards pipecuronium was identical or even superior to Sugammadex. Carboxymethylated gamma-cyclodextrin showed efficient and complete reversal of the pipecuronium induced neuromuscular block in an ex vivo rat diaphragm experiment. |
| doi_str_mv | 10.1016/j.ijpharm.2017.03.060 |
| format | Article |
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Applying patient friendly and cost-efficient medications in healthcare will be a real challenge in the 21st century. Sugammadex is a selective, yet expensive agent used for the post-surgical reversal of neuromuscular block since 2008. A wide library of cyclodextrin-based follow-ups, having potentially similar affinity towards target aminosteroid type neuromuscular blocking agents has been established. Almost 20 compounds were assessed with respect to in vitro affinity against three commonly applied drugs. Based on the capillary electrophoretic screening, carboxymethylated and sulfobutylated gamma-cyclodextrin derivatives have the potential to be promising lead molecules for their affinity towards pipecuronium was identical or even superior to Sugammadex. Carboxymethylated gamma-cyclodextrin showed efficient and complete reversal of the pipecuronium induced neuromuscular block in an ex vivo rat diaphragm experiment.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2017.03.060</identifier><identifier>PMID: 28366806</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Animal study ; Animals ; Artificial receptor ; Capillary electrophoresis ; Cyclodextrins ; Drug Design ; gamma-Cyclodextrins - pharmacology ; Male ; Neurological agents ; Neuromuscular Blockade ; Neuromuscular Nondepolarizing Agents - pharmacology ; Pipecuronium - pharmacology ; Rats ; Rats, Wistar ; Receptors, Artificial - chemistry ; Sugammadex</subject><ispartof>International journal of pharmaceutics, 2017-10, Vol.531 (2), p.512-520</ispartof><rights>2017 Elsevier B.V.</rights><rights>Copyright © 2017 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-22556deab881a17b632077c667484c78d71ea8bd6f6248f5815c183f0c6102773</citedby><cites>FETCH-LOGICAL-c391t-22556deab881a17b632077c667484c78d71ea8bd6f6248f5815c183f0c6102773</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517317302478$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28366806$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sohajda, Tamás</creatorcontrib><creatorcontrib>Fábián, Ákos</creatorcontrib><creatorcontrib>Tuza, Kata</creatorcontrib><creatorcontrib>Malanga, Milo</creatorcontrib><creatorcontrib>Benkovics, Gábor</creatorcontrib><creatorcontrib>Fülesdi, Béla</creatorcontrib><creatorcontrib>Tassonyi, Edömér</creatorcontrib><creatorcontrib>Szente, Lajos</creatorcontrib><title>Design and evaluation of artificial receptors for the reversal of neuromuscular block</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
Applying patient friendly and cost-efficient medications in healthcare will be a real challenge in the 21st century. Sugammadex is a selective, yet expensive agent used for the post-surgical reversal of neuromuscular block since 2008. A wide library of cyclodextrin-based follow-ups, having potentially similar affinity towards target aminosteroid type neuromuscular blocking agents has been established. Almost 20 compounds were assessed with respect to in vitro affinity against three commonly applied drugs. Based on the capillary electrophoretic screening, carboxymethylated and sulfobutylated gamma-cyclodextrin derivatives have the potential to be promising lead molecules for their affinity towards pipecuronium was identical or even superior to Sugammadex. Carboxymethylated gamma-cyclodextrin showed efficient and complete reversal of the pipecuronium induced neuromuscular block in an ex vivo rat diaphragm experiment.</description><subject>Animal study</subject><subject>Animals</subject><subject>Artificial receptor</subject><subject>Capillary electrophoresis</subject><subject>Cyclodextrins</subject><subject>Drug Design</subject><subject>gamma-Cyclodextrins - pharmacology</subject><subject>Male</subject><subject>Neurological agents</subject><subject>Neuromuscular Blockade</subject><subject>Neuromuscular Nondepolarizing Agents - pharmacology</subject><subject>Pipecuronium - pharmacology</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Artificial - chemistry</subject><subject>Sugammadex</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1PwzAMhiMEYuPjJ4B65NLiJG2SnRDiW5rEBc5RmrqQ0TYjaSfx7wna4MrJkv28tvwQckahoEDF5apwq_W7CX3BgMoCeAEC9sicKslzXkqxT-bApcorKvmMHMW4AgDBKD8kM6a4EArEnLzeYnRvQ2aGJsON6SYzOj9kvs1MGF3rrDNdFtDievQhZq0P2fiOqbPBENMogQNOwfdTtFNnQlZ33n6ckIPWdBFPd_WYvN7fvdw85svnh6eb62Vu-YKOOWNVJRo0tVLUUFkLzkBKK4QsVWmlaiRFo-pGtIKVqq0UrSxVvAUrKDAp-TG52O5dB_85YRx176LFrjMD-ilqqhRXfKEYJLTaojb4GAO2eh1cb8KXpqB_jOqV3hnVP0Y1cJ2Mptz57sRU99j8pX4VJuBqC2B6dOMw6GgdDhYbl7yNuvHunxPf8j6J0w</recordid><startdate>20171015</startdate><enddate>20171015</enddate><creator>Sohajda, Tamás</creator><creator>Fábián, Ákos</creator><creator>Tuza, Kata</creator><creator>Malanga, Milo</creator><creator>Benkovics, Gábor</creator><creator>Fülesdi, Béla</creator><creator>Tassonyi, Edömér</creator><creator>Szente, Lajos</creator><general>Elsevier B.V</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></search><sort><creationdate>20171015</creationdate><title>Design and evaluation of artificial receptors for the reversal of neuromuscular block</title><author>Sohajda, Tamás ; Fábián, Ákos ; Tuza, Kata ; Malanga, Milo ; Benkovics, Gábor ; Fülesdi, Béla ; Tassonyi, Edömér ; Szente, Lajos</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-22556deab881a17b632077c667484c78d71ea8bd6f6248f5815c183f0c6102773</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Animal study</topic><topic>Animals</topic><topic>Artificial receptor</topic><topic>Capillary electrophoresis</topic><topic>Cyclodextrins</topic><topic>Drug Design</topic><topic>gamma-Cyclodextrins - pharmacology</topic><topic>Male</topic><topic>Neurological agents</topic><topic>Neuromuscular Blockade</topic><topic>Neuromuscular Nondepolarizing Agents - pharmacology</topic><topic>Pipecuronium - pharmacology</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Artificial - chemistry</topic><topic>Sugammadex</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sohajda, Tamás</creatorcontrib><creatorcontrib>Fábián, Ákos</creatorcontrib><creatorcontrib>Tuza, Kata</creatorcontrib><creatorcontrib>Malanga, Milo</creatorcontrib><creatorcontrib>Benkovics, Gábor</creatorcontrib><creatorcontrib>Fülesdi, Béla</creatorcontrib><creatorcontrib>Tassonyi, Edömér</creatorcontrib><creatorcontrib>Szente, Lajos</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><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sohajda, Tamás</au><au>Fábián, Ákos</au><au>Tuza, Kata</au><au>Malanga, Milo</au><au>Benkovics, Gábor</au><au>Fülesdi, Béla</au><au>Tassonyi, Edömér</au><au>Szente, Lajos</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and evaluation of artificial receptors for the reversal of neuromuscular block</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2017-10-15</date><risdate>2017</risdate><volume>531</volume><issue>2</issue><spage>512</spage><epage>520</epage><pages>512-520</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
Applying patient friendly and cost-efficient medications in healthcare will be a real challenge in the 21st century. Sugammadex is a selective, yet expensive agent used for the post-surgical reversal of neuromuscular block since 2008. A wide library of cyclodextrin-based follow-ups, having potentially similar affinity towards target aminosteroid type neuromuscular blocking agents has been established. Almost 20 compounds were assessed with respect to in vitro affinity against three commonly applied drugs. Based on the capillary electrophoretic screening, carboxymethylated and sulfobutylated gamma-cyclodextrin derivatives have the potential to be promising lead molecules for their affinity towards pipecuronium was identical or even superior to Sugammadex. Carboxymethylated gamma-cyclodextrin showed efficient and complete reversal of the pipecuronium induced neuromuscular block in an ex vivo rat diaphragm experiment.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>28366806</pmid><doi>10.1016/j.ijpharm.2017.03.060</doi><tpages>9</tpages></addata></record> |
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| ispartof | International journal of pharmaceutics, 2017-10, Vol.531 (2), p.512-520 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animal study Animals Artificial receptor Capillary electrophoresis Cyclodextrins Drug Design gamma-Cyclodextrins - pharmacology Male Neurological agents Neuromuscular Blockade Neuromuscular Nondepolarizing Agents - pharmacology Pipecuronium - pharmacology Rats Rats, Wistar Receptors, Artificial - chemistry Sugammadex |
| title | Design and evaluation of artificial receptors for the reversal of neuromuscular block |
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