Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge

Objectives To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α‐tocopherol and lipoic acid into viable skin layers. Methods α‐Tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside‐based microemulsions conta...

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Veröffentlicht in:Journal of pharmacy and pharmacology 2013-06, Vol.65 (6), p.817-826
Hauptverfasser: Cichewicz, Allie, Pacleb, Chelsea, Connors, Ashley, Hass, Martha A., Lopes, Luciana B.
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container_issue 6
container_start_page 817
container_title Journal of pharmacy and pharmacology
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creator Cichewicz, Allie
Pacleb, Chelsea
Connors, Ashley
Hass, Martha A.
Lopes, Luciana B.
description Objectives To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α‐tocopherol and lipoic acid into viable skin layers. Methods α‐Tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside‐based microemulsions containing mono‐dicaprylin. Microemulsions containing surfactant : oil : water (w/w/w) at 60 : 30 : 10 (ME‐O) and 46 : 23 : 31 (ME‐W), as well as a cationic form of ME‐W containing 1% phytosphingosine (ME‐Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME‐Wphy‐treated skin was assessed using the thiobarbituric acid‐reactive substances (TBARS) assay. Key findings The internal phase diameters of microemulsions ranged between 42 and 55 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME‐O displayed w/o structure, whereas ME‐W and ME‐Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α‐Tocopherol delivery increased following the order ME‐O < ME‐W < ME‐Wphy. ME‐Wphy presented suitable short‐term stability. The antioxidants delivered by ME‐Wphy decreased TBARS cutaneous levels. Conclusions Even though microemulsion structure only affected tocopherol penetration, delivered levels of both antioxidants were sufficient for a decrease in TBARS, supporting their use for enhanced protection.
doi_str_mv 10.1111/jphp.12045
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Methods α‐Tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside‐based microemulsions containing mono‐dicaprylin. Microemulsions containing surfactant : oil : water (w/w/w) at 60 : 30 : 10 (ME‐O) and 46 : 23 : 31 (ME‐W), as well as a cationic form of ME‐W containing 1% phytosphingosine (ME‐Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME‐Wphy‐treated skin was assessed using the thiobarbituric acid‐reactive substances (TBARS) assay. Key findings The internal phase diameters of microemulsions ranged between 42 and 55 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME‐O displayed w/o structure, whereas ME‐W and ME‐Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α‐Tocopherol delivery increased following the order ME‐O &lt; ME‐W &lt; ME‐Wphy. ME‐Wphy presented suitable short‐term stability. The antioxidants delivered by ME‐Wphy decreased TBARS cutaneous levels. Conclusions Even though microemulsion structure only affected tocopherol penetration, delivered levels of both antioxidants were sufficient for a decrease in TBARS, supporting their use for enhanced protection.</description><identifier>ISSN: 0022-3573</identifier><identifier>EISSN: 2042-7158</identifier><identifier>DOI: 10.1111/jphp.12045</identifier><identifier>PMID: 23647675</identifier><language>eng</language><publisher>England: Blackwell Publishing Ltd</publisher><subject><![CDATA[Administration, Cutaneous ; alpha-Tocopherol - administration & dosage ; alpha-Tocopherol - chemistry ; Animals ; Antioxidants - administration & dosage ; Antioxidants - chemistry ; Chemistry, Pharmaceutical - methods ; cutaneous delivery ; Emulsions - administration & dosage ; Emulsions - chemistry ; Glucosides - administration & dosage ; Glucosides - chemistry ; Hydrogen-Ion Concentration ; lipoic acid ; medium chain monoglycerides ; microemulsions ; Oils - chemistry ; Permeability ; phytosphingosine ; Research Paper ; Skin - metabolism ; Skin Absorption ; Sphingosine - analogs & derivatives ; Sphingosine - chemistry ; Surface-Active Agents - chemistry ; Swine ; Thioctic Acid - administration & dosage ; Thioctic Acid - chemistry ; Water - chemistry ; α-tocopherol]]></subject><ispartof>Journal of pharmacy and pharmacology, 2013-06, Vol.65 (6), p.817-826</ispartof><rights>2013 Royal Pharmaceutical Society</rights><rights>2013 Royal Pharmaceutical Society.</rights><rights>2013 Royal Pharmaceutical Society 2013</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4585-76c1e1d7c07d8343afb31fc4fd4ce1ed611b99285589061d0ef6575079fe7c093</citedby><cites>FETCH-LOGICAL-c4585-76c1e1d7c07d8343afb31fc4fd4ce1ed611b99285589061d0ef6575079fe7c093</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fjphp.12045$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fjphp.12045$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>230,314,780,784,885,1417,27923,27924,45573,45574</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23647675$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cichewicz, Allie</creatorcontrib><creatorcontrib>Pacleb, Chelsea</creatorcontrib><creatorcontrib>Connors, Ashley</creatorcontrib><creatorcontrib>Hass, Martha A.</creatorcontrib><creatorcontrib>Lopes, Luciana B.</creatorcontrib><title>Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge</title><title>Journal of pharmacy and pharmacology</title><addtitle>J Pharm Pharmacol</addtitle><description>Objectives To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α‐tocopherol and lipoic acid into viable skin layers. Methods α‐Tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside‐based microemulsions containing mono‐dicaprylin. Microemulsions containing surfactant : oil : water (w/w/w) at 60 : 30 : 10 (ME‐O) and 46 : 23 : 31 (ME‐W), as well as a cationic form of ME‐W containing 1% phytosphingosine (ME‐Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME‐Wphy‐treated skin was assessed using the thiobarbituric acid‐reactive substances (TBARS) assay. Key findings The internal phase diameters of microemulsions ranged between 42 and 55 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME‐O displayed w/o structure, whereas ME‐W and ME‐Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α‐Tocopherol delivery increased following the order ME‐O &lt; ME‐W &lt; ME‐Wphy. ME‐Wphy presented suitable short‐term stability. The antioxidants delivered by ME‐Wphy decreased TBARS cutaneous levels. Conclusions Even though microemulsion structure only affected tocopherol penetration, delivered levels of both antioxidants were sufficient for a decrease in TBARS, supporting their use for enhanced protection.</description><subject>Administration, Cutaneous</subject><subject>alpha-Tocopherol - administration &amp; dosage</subject><subject>alpha-Tocopherol - chemistry</subject><subject>Animals</subject><subject>Antioxidants - administration &amp; dosage</subject><subject>Antioxidants - chemistry</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>cutaneous delivery</subject><subject>Emulsions - administration &amp; dosage</subject><subject>Emulsions - chemistry</subject><subject>Glucosides - administration &amp; dosage</subject><subject>Glucosides - chemistry</subject><subject>Hydrogen-Ion Concentration</subject><subject>lipoic acid</subject><subject>medium chain monoglycerides</subject><subject>microemulsions</subject><subject>Oils - chemistry</subject><subject>Permeability</subject><subject>phytosphingosine</subject><subject>Research Paper</subject><subject>Skin - metabolism</subject><subject>Skin Absorption</subject><subject>Sphingosine - analogs &amp; derivatives</subject><subject>Sphingosine - chemistry</subject><subject>Surface-Active Agents - chemistry</subject><subject>Swine</subject><subject>Thioctic Acid - administration &amp; dosage</subject><subject>Thioctic Acid - chemistry</subject><subject>Water - chemistry</subject><subject>α-tocopherol</subject><issn>0022-3573</issn><issn>2042-7158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFu1DAURS0EokNhwwcgr5FS7Di2ExZIaASdolK6aFV2lsd-nnFJ4shO2s5n8SP9JjwdOoJNvXmLd--x3kHoLSVHNL8P18N6OKIlqfgzNMujLCTl9XM0I6QsC8YlO0CvUromhEghxEt0UDJRSSH5DHXzadQ9hClhC62_gbjBweH738UYTBjWEEOLdW9x64fgDdbGWzwl369w500M0E1t8qFPH7HvXTtBb2ALMKEbQvJjXj3UzVrHFbxGL5xuE7z5Ow_R5dcvF_NFcfrj-GT--bQwFa95IYWhQK00RNqaVUy7JaPOVM5WBihYQemyacqa87ohgloCTnDJiWwc5FLDDtGnHXeYlh1YA_0YdauG6DsdNypor_7f9H6tVuFGZS91XcsMeL8D5BNTiuD2XUrUVrraSlcP0nP43b-_7aOPlnOA7gK3voXNEyj17Xxx_ggtdh2fRrjbd3T8pYRkkqurs2N1JRj9vvhJ1Jz9AfPZoBA</recordid><startdate>201306</startdate><enddate>201306</enddate><creator>Cichewicz, Allie</creator><creator>Pacleb, Chelsea</creator><creator>Connors, Ashley</creator><creator>Hass, Martha A.</creator><creator>Lopes, Luciana B.</creator><general>Blackwell Publishing Ltd</general><general>Oxford University Press</general><scope>BSCLL</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>5PM</scope></search><sort><creationdate>201306</creationdate><title>Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge</title><author>Cichewicz, Allie ; Pacleb, Chelsea ; Connors, Ashley ; Hass, Martha A. ; Lopes, Luciana B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4585-76c1e1d7c07d8343afb31fc4fd4ce1ed611b99285589061d0ef6575079fe7c093</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Administration, Cutaneous</topic><topic>alpha-Tocopherol - administration &amp; dosage</topic><topic>alpha-Tocopherol - chemistry</topic><topic>Animals</topic><topic>Antioxidants - administration &amp; dosage</topic><topic>Antioxidants - chemistry</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>cutaneous delivery</topic><topic>Emulsions - administration &amp; dosage</topic><topic>Emulsions - chemistry</topic><topic>Glucosides - administration &amp; dosage</topic><topic>Glucosides - chemistry</topic><topic>Hydrogen-Ion Concentration</topic><topic>lipoic acid</topic><topic>medium chain monoglycerides</topic><topic>microemulsions</topic><topic>Oils - chemistry</topic><topic>Permeability</topic><topic>phytosphingosine</topic><topic>Research Paper</topic><topic>Skin - metabolism</topic><topic>Skin Absorption</topic><topic>Sphingosine - analogs &amp; derivatives</topic><topic>Sphingosine - chemistry</topic><topic>Surface-Active Agents - chemistry</topic><topic>Swine</topic><topic>Thioctic Acid - administration &amp; dosage</topic><topic>Thioctic Acid - chemistry</topic><topic>Water - chemistry</topic><topic>α-tocopherol</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cichewicz, Allie</creatorcontrib><creatorcontrib>Pacleb, Chelsea</creatorcontrib><creatorcontrib>Connors, Ashley</creatorcontrib><creatorcontrib>Hass, Martha A.</creatorcontrib><creatorcontrib>Lopes, Luciana B.</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Journal of pharmacy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cichewicz, Allie</au><au>Pacleb, Chelsea</au><au>Connors, Ashley</au><au>Hass, Martha A.</au><au>Lopes, Luciana B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge</atitle><jtitle>Journal of pharmacy and pharmacology</jtitle><addtitle>J Pharm Pharmacol</addtitle><date>2013-06</date><risdate>2013</risdate><volume>65</volume><issue>6</issue><spage>817</spage><epage>826</epage><pages>817-826</pages><issn>0022-3573</issn><eissn>2042-7158</eissn><abstract>Objectives To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α‐tocopherol and lipoic acid into viable skin layers. Methods α‐Tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside‐based microemulsions containing mono‐dicaprylin. Microemulsions containing surfactant : oil : water (w/w/w) at 60 : 30 : 10 (ME‐O) and 46 : 23 : 31 (ME‐W), as well as a cationic form of ME‐W containing 1% phytosphingosine (ME‐Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME‐Wphy‐treated skin was assessed using the thiobarbituric acid‐reactive substances (TBARS) assay. Key findings The internal phase diameters of microemulsions ranged between 42 and 55 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME‐O displayed w/o structure, whereas ME‐W and ME‐Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α‐Tocopherol delivery increased following the order ME‐O &lt; ME‐W &lt; ME‐Wphy. ME‐Wphy presented suitable short‐term stability. The antioxidants delivered by ME‐Wphy decreased TBARS cutaneous levels. Conclusions Even though microemulsion structure only affected tocopherol penetration, delivered levels of both antioxidants were sufficient for a decrease in TBARS, supporting their use for enhanced protection.</abstract><cop>England</cop><pub>Blackwell Publishing Ltd</pub><pmid>23647675</pmid><doi>10.1111/jphp.12045</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record>
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source MEDLINE; Oxford University Press Journals All Titles (1996-Current); Wiley Online Library All Journals
subjects Administration, Cutaneous
alpha-Tocopherol - administration & dosage
alpha-Tocopherol - chemistry
Animals
Antioxidants - administration & dosage
Antioxidants - chemistry
Chemistry, Pharmaceutical - methods
cutaneous delivery
Emulsions - administration & dosage
Emulsions - chemistry
Glucosides - administration & dosage
Glucosides - chemistry
Hydrogen-Ion Concentration
lipoic acid
medium chain monoglycerides
microemulsions
Oils - chemistry
Permeability
phytosphingosine
Research Paper
Skin - metabolism
Skin Absorption
Sphingosine - analogs & derivatives
Sphingosine - chemistry
Surface-Active Agents - chemistry
Swine
Thioctic Acid - administration & dosage
Thioctic Acid - chemistry
Water - chemistry
α-tocopherol
title Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge
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