Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism

To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer. The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of o...

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Veröffentlicht in:Yao hsüeh hsüeh pao 2003-05, Vol.38 (5), p.384-387
Hauptverfasser: Cheng, Zhi-yi, Chen, Hao-fan
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description To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer. The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo. The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate. Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. Its transdermal enhancing mechanism may be that oleyl pyroglutamate induced not only disordering of the stratum corneum lipid, but also change o
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The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo. The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate. Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. Its transdermal enhancing mechanism may be that oleyl pyroglutamate induced not only disordering of the stratum corneum lipid, but also change o</description><identifier>ISSN: 0513-4870</identifier><identifier>PMID: 12958846</identifier><language>chi</language><publisher>China</publisher><subject>Administration, Cutaneous ; Adult ; Animals ; Caffeine - administration &amp; dosage ; Caffeine - pharmacokinetics ; Cortisone - administration &amp; dosage ; Cortisone - pharmacokinetics ; Fatty Alcohols - pharmacology ; Humans ; Male ; Mice ; Oleic Acid - pharmacology ; Pyrrolidonecarboxylic Acid - analogs &amp; derivatives ; Pyrrolidonecarboxylic Acid - chemistry ; Pyrrolidonecarboxylic Acid - pharmacology ; Skin Absorption - drug effects ; Tinidazole - administration &amp; dosage ; Tinidazole - pharmacokinetics</subject><ispartof>Yao hsüeh hsüeh pao, 2003-05, Vol.38 (5), p.384-387</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12958846$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cheng, Zhi-yi</creatorcontrib><creatorcontrib>Chen, Hao-fan</creatorcontrib><title>Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism</title><title>Yao hsüeh hsüeh pao</title><addtitle>Yao Xue Xue Bao</addtitle><description>To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer. The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo. The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate. Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. Its transdermal enhancing mechanism may be that oleyl pyroglutamate induced not only disordering of the stratum corneum lipid, but also change o</description><subject>Administration, Cutaneous</subject><subject>Adult</subject><subject>Animals</subject><subject>Caffeine - administration &amp; dosage</subject><subject>Caffeine - pharmacokinetics</subject><subject>Cortisone - administration &amp; dosage</subject><subject>Cortisone - pharmacokinetics</subject><subject>Fatty Alcohols - pharmacology</subject><subject>Humans</subject><subject>Male</subject><subject>Mice</subject><subject>Oleic Acid - pharmacology</subject><subject>Pyrrolidonecarboxylic Acid - analogs &amp; derivatives</subject><subject>Pyrrolidonecarboxylic Acid - chemistry</subject><subject>Pyrrolidonecarboxylic Acid - pharmacology</subject><subject>Skin Absorption - drug effects</subject><subject>Tinidazole - administration &amp; dosage</subject><subject>Tinidazole - pharmacokinetics</subject><issn>0513-4870</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1kLtOxDAURF2A2GXhF5Arukh2nPhRohUvaaU0UEfXzvUSZCfBTor8PSBCNUejoynmguxZzUVRacV25DrnT8YqboS-IjtemlrrSu5J0wRcA53WNJ7DMkOEGakfE10yUsh0TjDkDlOEQHH4gMFhojB0tJ_zVvTDmUZ0P9jneEMuPYSMt1seyPvT49vxpTg1z6_Hh1Mx8bKcC22s9w6lhprVmnMrlGZMGpDMSlsbUXnjnRdGK1t64WoF2ilpKwGiVF6LA7n_253S-LVgntvYZ4chwIDjklslJK-U-BXvNnGxEbt2Sn2EtLb_F4hvwGFXXQ</recordid><startdate>200305</startdate><enddate>200305</enddate><creator>Cheng, Zhi-yi</creator><creator>Chen, Hao-fan</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>200305</creationdate><title>Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism</title><author>Cheng, Zhi-yi ; Chen, Hao-fan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p122t-89bffce68a505811b3780069a60b6b5934f9fcf3987b2f3c57a8c76b43a327f83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>chi</language><creationdate>2003</creationdate><topic>Administration, Cutaneous</topic><topic>Adult</topic><topic>Animals</topic><topic>Caffeine - administration &amp; dosage</topic><topic>Caffeine - pharmacokinetics</topic><topic>Cortisone - administration &amp; dosage</topic><topic>Cortisone - pharmacokinetics</topic><topic>Fatty Alcohols - pharmacology</topic><topic>Humans</topic><topic>Male</topic><topic>Mice</topic><topic>Oleic Acid - pharmacology</topic><topic>Pyrrolidonecarboxylic Acid - analogs &amp; derivatives</topic><topic>Pyrrolidonecarboxylic Acid - chemistry</topic><topic>Pyrrolidonecarboxylic Acid - pharmacology</topic><topic>Skin Absorption - drug effects</topic><topic>Tinidazole - administration &amp; dosage</topic><topic>Tinidazole - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cheng, Zhi-yi</creatorcontrib><creatorcontrib>Chen, Hao-fan</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Yao hsüeh hsüeh pao</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cheng, Zhi-yi</au><au>Chen, Hao-fan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism</atitle><jtitle>Yao hsüeh hsüeh pao</jtitle><addtitle>Yao Xue Xue Bao</addtitle><date>2003-05</date><risdate>2003</risdate><volume>38</volume><issue>5</issue><spage>384</spage><epage>387</epage><pages>384-387</pages><issn>0513-4870</issn><abstract>To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer. The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo. The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate. Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. 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subjects Administration, Cutaneous
Adult
Animals
Caffeine - administration & dosage
Caffeine - pharmacokinetics
Cortisone - administration & dosage
Cortisone - pharmacokinetics
Fatty Alcohols - pharmacology
Humans
Male
Mice
Oleic Acid - pharmacology
Pyrrolidonecarboxylic Acid - analogs & derivatives
Pyrrolidonecarboxylic Acid - chemistry
Pyrrolidonecarboxylic Acid - pharmacology
Skin Absorption - drug effects
Tinidazole - administration & dosage
Tinidazole - pharmacokinetics
title Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism
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