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
Hauptverfasser: Chen, Huabing, Chang, Xueling, Weng, Ting, Zhao, Xiaozhi, Gao, Zhonghong, Yang, Yajiang, Xu, Huibi, Yang, Xiangliang
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container_end_page 436
container_issue 3
container_start_page 427
container_title Journal of controlled release
container_volume 98
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. 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Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Phenanthrenes - administration &amp; 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 &amp; dosage</topic><topic>Antineoplastic Agents, Phytogenic - adverse effects</topic><topic>Antispermatogenic Agents - administration &amp; dosage</topic><topic>Antispermatogenic Agents - adverse effects</topic><topic>Biological and medical sciences</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Diterpenes - administration &amp; dosage</topic><topic>Diterpenes - adverse effects</topic><topic>Emulsions</topic><topic>Epoxy Compounds</topic><topic>General pharmacology</topic><topic>Immunosuppressive Agents - administration &amp; 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. 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Drug treatments</topic><topic>Phenanthrenes - administration &amp; 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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