Novel approach to improve permeation of ondansetron across shed snake skin as a model membrane
The purpose of this study was to investigate the feasibility of transdermal drug delivery of ondansetron, an antagonist of the 5‐HT3 receptor, used for the treatment of chemotherapy‐induced emesis. The permeability of ondansetron from an aqueous suspension through shed snake skin as a model membrane...
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Veröffentlicht in: | Journal of pharmacy and pharmacology 2001-06, Vol.53 (6), p.789-794 |
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description | The purpose of this study was to investigate the feasibility of transdermal drug delivery of ondansetron, an antagonist of the 5‐HT3 receptor, used for the treatment of chemotherapy‐induced emesis. The permeability of ondansetron from an aqueous suspension through shed snake skin as a model membrane was very low and in order to improve it, several enhancers were tested. Ethanol increased the flux at a concentration of 40% or more. The solubility of ondansetron also increased as the ethanol concentration increased. The permeability coefficient increased after pretreatment of the shed snake skin with Azone, oleic acid or lauryl alcohol. Further improvement of the permeability was observed when ethanol was combined with other enhancers and was maximum for the combination of ethanol and oleic acid. Oleic acid dramatically increased the partition of ondansetron to n‐hexane and shed snake skin. Oleic acid may enhance the permeation of ondansetron in two ways: by a direct effect on the stratum corneum or via counterion formation of an ion‐pair. The maximum flux obtained from the combination of ethanol and other enhancers seems to be high enough to obtain a therapeutic effect. |
doi_str_mv | 10.1211/0022357011776135 |
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Oleic acid dramatically increased the partition of ondansetron to n‐hexane and shed snake skin. Oleic acid may enhance the permeation of ondansetron in two ways: by a direct effect on the stratum corneum or via counterion formation of an ion‐pair. The maximum flux obtained from the combination of ethanol and other enhancers seems to be high enough to obtain a therapeutic effect.</description><identifier>ISSN: 0022-3573</identifier><identifier>EISSN: 2042-7158</identifier><identifier>DOI: 10.1211/0022357011776135</identifier><identifier>PMID: 11428654</identifier><identifier>CODEN: JPPMAB</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Administration, Cutaneous ; Animals ; Biological and medical sciences ; Ethanol - pharmacology ; Humans ; Medical sciences ; Models, Animal ; Molting ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Oleic Acid - pharmacology ; Ondansetron - pharmacokinetics ; Permeability ; Pharmacology. Drug treatments ; Serotonin Antagonists - pharmacokinetics ; Serotoninergic system ; Skin - drug effects ; Skin Physiological Phenomena ; Snakes ; Solubility ; Solvents - pharmacology ; Vomiting - chemically induced ; Vomiting - drug therapy</subject><ispartof>Journal of pharmacy and pharmacology, 2001-06, Vol.53 (6), p.789-794</ispartof><rights>2001 Royal Pharmaceutical Society of Great Britain</rights><rights>2001 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5476-c7f63602a6c5d6b21e7aed7c869dd5f402b120add0a32ee05c832b74263bca0a3</citedby><cites>FETCH-LOGICAL-c5476-c7f63602a6c5d6b21e7aed7c869dd5f402b120add0a32ee05c832b74263bca0a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1211%2F0022357011776135$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1211%2F0022357011776135$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1416,27923,27924,45573,45574</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=987970$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11428654$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Takahashi, Koichi</creatorcontrib><creatorcontrib>Rytting, J. Howard</creatorcontrib><title>Novel approach to improve permeation of ondansetron across shed snake skin as a model membrane</title><title>Journal of pharmacy and pharmacology</title><addtitle>J Pharm Pharmacol</addtitle><description>The purpose of this study was to investigate the feasibility of transdermal drug delivery of ondansetron, an antagonist of the 5‐HT3 receptor, used for the treatment of chemotherapy‐induced emesis. The permeability of ondansetron from an aqueous suspension through shed snake skin as a model membrane was very low and in order to improve it, several enhancers were tested. Ethanol increased the flux at a concentration of 40% or more. The solubility of ondansetron also increased as the ethanol concentration increased. The permeability coefficient increased after pretreatment of the shed snake skin with Azone, oleic acid or lauryl alcohol. Further improvement of the permeability was observed when ethanol was combined with other enhancers and was maximum for the combination of ethanol and oleic acid. Oleic acid dramatically increased the partition of ondansetron to n‐hexane and shed snake skin. Oleic acid may enhance the permeation of ondansetron in two ways: by a direct effect on the stratum corneum or via counterion formation of an ion‐pair. The maximum flux obtained from the combination of ethanol and other enhancers seems to be high enough to obtain a therapeutic effect.</description><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Ethanol - pharmacology</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Models, Animal</subject><subject>Molting</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Oleic Acid - pharmacology</subject><subject>Ondansetron - pharmacokinetics</subject><subject>Permeability</subject><subject>Pharmacology. Drug treatments</subject><subject>Serotonin Antagonists - pharmacokinetics</subject><subject>Serotoninergic system</subject><subject>Skin - drug effects</subject><subject>Skin Physiological Phenomena</subject><subject>Snakes</subject><subject>Solubility</subject><subject>Solvents - pharmacology</subject><subject>Vomiting - chemically induced</subject><subject>Vomiting - drug therapy</subject><issn>0022-3573</issn><issn>2042-7158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM1v1DAQxS0EokvhzglZQuIWGNuxnRyhgm1RVcqXyglrYk_UsPnY2tmW_vd42VWRuPRke-b33owfY88FvBZSiDcAUiptQQhrjVD6AVtIKGVhha4essW2XeS-OmBPUvoFANYY85gdCFHKyuhywX6eTdfUc1yv44T-ks8T74Z8vya-pjgQzt008qnl0xhwTDTH_EQfp5R4uqTA04gr4mnV5XLiyIcpZL-BhibiSE_Zoxb7RM_25yH7_uH9t6Pj4vTT8uTo7WnhdWlN4W1rlAGJxutgGinIIgXrK1OHoNsSZCMkYAiAShKB9pWSjS2lUY3HXDxkr3a-efWrDaXZDV3y1Pd5h2mTnIW61kLqe0EJJk_SWxB24N-_RmrdOnYDxlsnwG3Dd_-HnyUv9t6bZqDwT7BPOwMv9wAmj32bE_JduuPqytYWMmV21E3X0-29Y93H8-NzIWqThcVO2KWZft8JMa6cscpqd3G2dF_Mj-WF-vrOfVZ_AJRaqhg</recordid><startdate>200106</startdate><enddate>200106</enddate><creator>Takahashi, Koichi</creator><creator>Rytting, J. Howard</creator><general>Blackwell Publishing Ltd</general><general>Pharmaceutical Press</general><scope>BSCLL</scope><scope>IQODW</scope><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>200106</creationdate><title>Novel approach to improve permeation of ondansetron across shed snake skin as a model membrane</title><author>Takahashi, Koichi ; Rytting, J. Howard</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5476-c7f63602a6c5d6b21e7aed7c869dd5f402b120add0a32ee05c832b74263bca0a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Ethanol - pharmacology</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Models, Animal</topic><topic>Molting</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Oleic Acid - pharmacology</topic><topic>Ondansetron - pharmacokinetics</topic><topic>Permeability</topic><topic>Pharmacology. Drug treatments</topic><topic>Serotonin Antagonists - pharmacokinetics</topic><topic>Serotoninergic system</topic><topic>Skin - drug effects</topic><topic>Skin Physiological Phenomena</topic><topic>Snakes</topic><topic>Solubility</topic><topic>Solvents - pharmacology</topic><topic>Vomiting - chemically induced</topic><topic>Vomiting - drug therapy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Takahashi, Koichi</creatorcontrib><creatorcontrib>Rytting, J. Howard</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><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>Journal of pharmacy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Takahashi, Koichi</au><au>Rytting, J. Howard</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel approach to improve permeation of ondansetron across shed snake skin as a model membrane</atitle><jtitle>Journal of pharmacy and pharmacology</jtitle><addtitle>J Pharm Pharmacol</addtitle><date>2001-06</date><risdate>2001</risdate><volume>53</volume><issue>6</issue><spage>789</spage><epage>794</epage><pages>789-794</pages><issn>0022-3573</issn><eissn>2042-7158</eissn><coden>JPPMAB</coden><abstract>The purpose of this study was to investigate the feasibility of transdermal drug delivery of ondansetron, an antagonist of the 5‐HT3 receptor, used for the treatment of chemotherapy‐induced emesis. The permeability of ondansetron from an aqueous suspension through shed snake skin as a model membrane was very low and in order to improve it, several enhancers were tested. Ethanol increased the flux at a concentration of 40% or more. The solubility of ondansetron also increased as the ethanol concentration increased. The permeability coefficient increased after pretreatment of the shed snake skin with Azone, oleic acid or lauryl alcohol. Further improvement of the permeability was observed when ethanol was combined with other enhancers and was maximum for the combination of ethanol and oleic acid. Oleic acid dramatically increased the partition of ondansetron to n‐hexane and shed snake skin. Oleic acid may enhance the permeation of ondansetron in two ways: by a direct effect on the stratum corneum or via counterion formation of an ion‐pair. The maximum flux obtained from the combination of ethanol and other enhancers seems to be high enough to obtain a therapeutic effect.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>11428654</pmid><doi>10.1211/0022357011776135</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Administration, Cutaneous Animals Biological and medical sciences Ethanol - pharmacology Humans Medical sciences Models, Animal Molting Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oleic Acid - pharmacology Ondansetron - pharmacokinetics Permeability Pharmacology. Drug treatments Serotonin Antagonists - pharmacokinetics Serotoninergic system Skin - drug effects Skin Physiological Phenomena Snakes Solubility Solvents - pharmacology Vomiting - chemically induced Vomiting - drug therapy |
title | Novel approach to improve permeation of ondansetron across shed snake skin as a model membrane |
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