A study of microemulsion systems for transdermal delivery of triptolide
Triptolide possesses immunosuppressive, anti-fertility and anti-cancer activities. Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was...
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Veröffentlicht in: | Journal of controlled release 2004-08, Vol.98 (3), p.427-436 |
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creator | Chen, Huabing Chang, Xueling Weng, Ting Zhao, Xiaozhi Gao, Zhonghong Yang, Yajiang Xu, Huibi Yang, Xiangliang |
description | Triptolide possesses immunosuppressive, anti-fertility and anti-cancer activities. Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was to investigate the microemulsions for transdermal delivery of triptolide. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using oleic acid as an oil, Tween 80 as a surfactant and propylene glycol as a cosurfactant. The droplet size of microemulsions was characterized by photocorrelation spectroscopy. The transdermal ability of triptolide from microemulsions was evaluated in vitro using Franz diffusion cells fitted with mouse skins and triptolide was analyzed by high-performance liquid chromatography. The effect of menthol as a permeation enhancer, and the loading dose of triptolide in microemulsions on the permeation rate were also evaluated. The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. The results indicate that the studied microemulsion systems, especially ME6, may be promising vehicles for the transdermal delivery of triptolide. |
doi_str_mv | 10.1016/j.jconrel.2004.06.001 |
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Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was to investigate the microemulsions for transdermal delivery of triptolide. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using oleic acid as an oil, Tween 80 as a surfactant and propylene glycol as a cosurfactant. The droplet size of microemulsions was characterized by photocorrelation spectroscopy. The transdermal ability of triptolide from microemulsions was evaluated in vitro using Franz diffusion cells fitted with mouse skins and triptolide was analyzed by high-performance liquid chromatography. The effect of menthol as a permeation enhancer, and the loading dose of triptolide in microemulsions on the permeation rate were also evaluated. The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. The results indicate that the studied microemulsion systems, especially ME6, may be promising vehicles for the transdermal delivery of triptolide.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/j.jconrel.2004.06.001</identifier><identifier>PMID: 15312998</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Administration, Cutaneous ; Animals ; Antineoplastic Agents, Phytogenic - administration & dosage ; Antineoplastic Agents, Phytogenic - adverse effects ; Antispermatogenic Agents - administration & dosage ; Antispermatogenic Agents - adverse effects ; Biological and medical sciences ; Chromatography, High Pressure Liquid ; Diterpenes - administration & dosage ; Diterpenes - adverse effects ; Emulsions ; Epoxy Compounds ; General pharmacology ; Immunosuppressive Agents - administration & dosage ; Immunosuppressive Agents - adverse effects ; In Vitro Techniques ; Irritants - pharmacology ; Male ; Medical sciences ; Menthol ; Mice ; Microemulsion ; Oleic Acid ; Permeability ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Phenanthrenes - administration & dosage ; Phenanthrenes - adverse effects ; Propylene Glycol ; Skin Absorption ; Transdermal delivery ; Triptolide ; Tween 80</subject><ispartof>Journal of controlled release, 2004-08, Vol.98 (3), p.427-436</ispartof><rights>2004 Elsevier B.V.</rights><rights>2004 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c422t-634a97d93f4a07e9942c02bc4401bd888f7a178e540c17f2474d34c81068016c3</citedby><cites>FETCH-LOGICAL-c422t-634a97d93f4a07e9942c02bc4401bd888f7a178e540c17f2474d34c81068016c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S016836590400269X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16083156$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15312998$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chen, Huabing</creatorcontrib><creatorcontrib>Chang, Xueling</creatorcontrib><creatorcontrib>Weng, Ting</creatorcontrib><creatorcontrib>Zhao, Xiaozhi</creatorcontrib><creatorcontrib>Gao, Zhonghong</creatorcontrib><creatorcontrib>Yang, Yajiang</creatorcontrib><creatorcontrib>Xu, Huibi</creatorcontrib><creatorcontrib>Yang, Xiangliang</creatorcontrib><title>A study of microemulsion systems for transdermal delivery of triptolide</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>Triptolide possesses immunosuppressive, anti-fertility and anti-cancer activities. Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was to investigate the microemulsions for transdermal delivery of triptolide. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using oleic acid as an oil, Tween 80 as a surfactant and propylene glycol as a cosurfactant. The droplet size of microemulsions was characterized by photocorrelation spectroscopy. The transdermal ability of triptolide from microemulsions was evaluated in vitro using Franz diffusion cells fitted with mouse skins and triptolide was analyzed by high-performance liquid chromatography. The effect of menthol as a permeation enhancer, and the loading dose of triptolide in microemulsions on the permeation rate were also evaluated. The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. The results indicate that the studied microemulsion systems, especially ME6, may be promising vehicles for the transdermal delivery of triptolide.</description><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Antineoplastic Agents, Phytogenic - administration & dosage</subject><subject>Antineoplastic Agents, Phytogenic - adverse effects</subject><subject>Antispermatogenic Agents - administration & dosage</subject><subject>Antispermatogenic Agents - adverse effects</subject><subject>Biological and medical sciences</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Diterpenes - administration & dosage</subject><subject>Diterpenes - adverse effects</subject><subject>Emulsions</subject><subject>Epoxy Compounds</subject><subject>General pharmacology</subject><subject>Immunosuppressive Agents - administration & dosage</subject><subject>Immunosuppressive Agents - adverse effects</subject><subject>In Vitro Techniques</subject><subject>Irritants - pharmacology</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Menthol</subject><subject>Mice</subject><subject>Microemulsion</subject><subject>Oleic Acid</subject><subject>Permeability</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Phenanthrenes - administration & dosage</subject><subject>Phenanthrenes - adverse effects</subject><subject>Propylene Glycol</subject><subject>Skin Absorption</subject><subject>Transdermal delivery</subject><subject>Triptolide</subject><subject>Tween 80</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1r3DAQhkVpaDZpf0KLL83NzsiSLelUwpIvCOSSnIVWGoMW2dpKdmD_fZWuIcec5vK8M_M-hPyk0FCg_fW-2ds4JQxNC8Ab6BsA-oVsqBSs5kp1X8mmcLJmfafOyUXOewDoGBffyDntGG2Vkhtyf1PleXHHKg7V6G2KOC4h-zhV-ZhnHHM1xFTNyUzZYRpNqBwG_4bpf2JO_jDH4B1-J2eDCRl_rPOSvN7dvmwf6qfn-8ftzVNtedvOdc-4UcIpNnADApXirYV2ZzkHunNSykEYKiR2HCwVQ8sFd4xbSaGXpY1ll-TqtPeQ4t8F86xHny2GYCaMS9ZUdJJJpgrYncDSKeeEgz4kP5p01BT0u0G916tB_W5QQ6-LwZL7tR5YdiO6j9SqrAC_V8Bka8JQ1FifP7geJKNdX7g_Jw6LjjePSWfrcbLofEI7axf9J6_8A2iVkSY</recordid><startdate>20040827</startdate><enddate>20040827</enddate><creator>Chen, Huabing</creator><creator>Chang, Xueling</creator><creator>Weng, Ting</creator><creator>Zhao, Xiaozhi</creator><creator>Gao, Zhonghong</creator><creator>Yang, Yajiang</creator><creator>Xu, Huibi</creator><creator>Yang, Xiangliang</creator><general>Elsevier B.V</general><general>Elsevier</general><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></search><sort><creationdate>20040827</creationdate><title>A study of microemulsion systems for transdermal delivery of triptolide</title><author>Chen, Huabing ; Chang, Xueling ; Weng, Ting ; Zhao, Xiaozhi ; Gao, Zhonghong ; Yang, Yajiang ; Xu, Huibi ; Yang, Xiangliang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c422t-634a97d93f4a07e9942c02bc4401bd888f7a178e540c17f2474d34c81068016c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Antineoplastic Agents, Phytogenic - administration & dosage</topic><topic>Antineoplastic Agents, Phytogenic - adverse effects</topic><topic>Antispermatogenic Agents - administration & dosage</topic><topic>Antispermatogenic Agents - adverse effects</topic><topic>Biological and medical sciences</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Diterpenes - administration & dosage</topic><topic>Diterpenes - adverse effects</topic><topic>Emulsions</topic><topic>Epoxy Compounds</topic><topic>General pharmacology</topic><topic>Immunosuppressive Agents - administration & dosage</topic><topic>Immunosuppressive Agents - adverse effects</topic><topic>In Vitro Techniques</topic><topic>Irritants - pharmacology</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Menthol</topic><topic>Mice</topic><topic>Microemulsion</topic><topic>Oleic Acid</topic><topic>Permeability</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Phenanthrenes - administration & dosage</topic><topic>Phenanthrenes - adverse effects</topic><topic>Propylene Glycol</topic><topic>Skin Absorption</topic><topic>Transdermal delivery</topic><topic>Triptolide</topic><topic>Tween 80</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chen, Huabing</creatorcontrib><creatorcontrib>Chang, Xueling</creatorcontrib><creatorcontrib>Weng, Ting</creatorcontrib><creatorcontrib>Zhao, Xiaozhi</creatorcontrib><creatorcontrib>Gao, Zhonghong</creatorcontrib><creatorcontrib>Yang, Yajiang</creatorcontrib><creatorcontrib>Xu, Huibi</creatorcontrib><creatorcontrib>Yang, Xiangliang</creatorcontrib><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><jtitle>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chen, Huabing</au><au>Chang, Xueling</au><au>Weng, Ting</au><au>Zhao, Xiaozhi</au><au>Gao, Zhonghong</au><au>Yang, Yajiang</au><au>Xu, Huibi</au><au>Yang, Xiangliang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A study of microemulsion systems for transdermal delivery of triptolide</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2004-08-27</date><risdate>2004</risdate><volume>98</volume><issue>3</issue><spage>427</spage><epage>436</epage><pages>427-436</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>Triptolide possesses immunosuppressive, anti-fertility and anti-cancer activities. Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was to investigate the microemulsions for transdermal delivery of triptolide. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using oleic acid as an oil, Tween 80 as a surfactant and propylene glycol as a cosurfactant. The droplet size of microemulsions was characterized by photocorrelation spectroscopy. The transdermal ability of triptolide from microemulsions was evaluated in vitro using Franz diffusion cells fitted with mouse skins and triptolide was analyzed by high-performance liquid chromatography. The effect of menthol as a permeation enhancer, and the loading dose of triptolide in microemulsions on the permeation rate were also evaluated. The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. The results indicate that the studied microemulsion systems, especially ME6, may be promising vehicles for the transdermal delivery of triptolide.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>15312998</pmid><doi>10.1016/j.jconrel.2004.06.001</doi><tpages>10</tpages></addata></record> |
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subjects | Administration, Cutaneous Animals Antineoplastic Agents, Phytogenic - administration & dosage Antineoplastic Agents, Phytogenic - adverse effects Antispermatogenic Agents - administration & dosage Antispermatogenic Agents - adverse effects Biological and medical sciences Chromatography, High Pressure Liquid Diterpenes - administration & dosage Diterpenes - adverse effects Emulsions Epoxy Compounds General pharmacology Immunosuppressive Agents - administration & dosage Immunosuppressive Agents - adverse effects In Vitro Techniques Irritants - pharmacology Male Medical sciences Menthol Mice Microemulsion Oleic Acid Permeability Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Phenanthrenes - administration & dosage Phenanthrenes - adverse effects Propylene Glycol Skin Absorption Transdermal delivery Triptolide Tween 80 |
title | A study of microemulsion systems for transdermal delivery of triptolide |
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