Evaluation of chemical enhancers in the transdermal delivery of lidocaine
The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl...
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| Veröffentlicht in: | International journal of pharmaceutics 2006-02, Vol.308 (1), p.33-39 |
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| creator | Lee, Philip J. Ahmad, Naina Langer, Robert Mitragotri, Samir Prasad Shastri, V. |
| description | The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl myristate (IPM) showed no significant flux enhancement. However, the binary system of IPM/
n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6
±
8.4
μg
cm
−2
h
−1 through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (
p
<
0.001). NMP was also found to co-transport through human skin with lidocaine free base and improve enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs. |
| doi_str_mv | 10.1016/j.ijpharm.2005.10.027 |
| format | Article |
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n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6
±
8.4
μg
cm
−2
h
−1 through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (
p
<
0.001). NMP was also found to co-transport through human skin with lidocaine free base and improve enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2005.10.027</identifier><identifier>PMID: 16321488</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Administration, Cutaneous ; Anesthetics, Local - administration & dosage ; Anesthetics, Local - chemistry ; Anesthetics, Local - metabolism ; Animals ; Biological and medical sciences ; Chemical enhancers ; Drug Combinations ; Drug Delivery Systems ; General pharmacology ; Humans ; Hydrophobic and Hydrophilic Interactions ; In Vitro Techniques ; Lidocaine ; Lidocaine - administration & dosage ; Lidocaine - chemistry ; Lidocaine - metabolism ; Medical sciences ; Myristates - administration & dosage ; Myristates - pharmacology ; n-Methyl pyrrolidone ; Pharmaceutic Aids - administration & dosage ; Pharmaceutic Aids - pharmacology ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Pyrrolidinones - administration & dosage ; Pyrrolidinones - pharmacology ; Skin Absorption - drug effects ; Solubility ; Swine ; Transdermal drug delivery</subject><ispartof>International journal of pharmaceutics, 2006-02, Vol.308 (1), p.33-39</ispartof><rights>2005 Elsevier B.V.</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c484t-78bf7d348b89020914caeb4d836b36dade0ad7dca90fff398d85b903065fafad3</citedby><cites>FETCH-LOGICAL-c484t-78bf7d348b89020914caeb4d836b36dade0ad7dca90fff398d85b903065fafad3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2005.10.027$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17439603$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16321488$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lee, Philip J.</creatorcontrib><creatorcontrib>Ahmad, Naina</creatorcontrib><creatorcontrib>Langer, Robert</creatorcontrib><creatorcontrib>Mitragotri, Samir</creatorcontrib><creatorcontrib>Prasad Shastri, V.</creatorcontrib><title>Evaluation of chemical enhancers in the transdermal delivery of lidocaine</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl myristate (IPM) showed no significant flux enhancement. However, the binary system of IPM/
n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6
±
8.4
μg
cm
−2
h
−1 through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (
p
<
0.001). NMP was also found to co-transport through human skin with lidocaine free base and improve enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs.</description><subject>Administration, Cutaneous</subject><subject>Anesthetics, Local - administration & dosage</subject><subject>Anesthetics, Local - chemistry</subject><subject>Anesthetics, Local - metabolism</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Chemical enhancers</subject><subject>Drug Combinations</subject><subject>Drug Delivery Systems</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Hydrophobic and Hydrophilic Interactions</subject><subject>In Vitro Techniques</subject><subject>Lidocaine</subject><subject>Lidocaine - administration & dosage</subject><subject>Lidocaine - chemistry</subject><subject>Lidocaine - metabolism</subject><subject>Medical sciences</subject><subject>Myristates - administration & dosage</subject><subject>Myristates - pharmacology</subject><subject>n-Methyl pyrrolidone</subject><subject>Pharmaceutic Aids - administration & dosage</subject><subject>Pharmaceutic Aids - pharmacology</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrrolidinones - administration & dosage</subject><subject>Pyrrolidinones - pharmacology</subject><subject>Skin Absorption - drug effects</subject><subject>Solubility</subject><subject>Swine</subject><subject>Transdermal drug delivery</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1rHDEMhk1paLZJf0LLXNrbbOWxx_acSglpGwj0kpyNxpZZL_OxtWcX8u_jZQdy7EkgPa8kHsY-c9hy4Or7fhv3hx2mcdsAtKW3hUa_YxtutKiF1Oo924DQpm65FtfsY857AFANFx_YNVei4dKYDXu4P-FwxCXOUzWHyu1ojA6HiqYdTo5SruJULTuqloRT9pTGMvQ0xBOll3NiiH52GCe6ZVcBh0yf1nrDnn_dP939qR___n64-_lYO2nkUmvTB-2FNL3poIGOS4fUS2-E6oXy6AnQa--wgxCC6Iw3bd-BANUGDOjFDft22XtI878j5cWOMTsaBpxoPmarQRktdVfA9gK6NOecKNhDiiOmF8vBnh3avV0d2rPDc7s4LLkv64FjP5J_S63SCvB1BTAXV6GYcTG_cVqKToEo3I8LR0XHKVKy2UUqVn1M5Bbr5_ifV14B6peTXA</recordid><startdate>20060203</startdate><enddate>20060203</enddate><creator>Lee, Philip J.</creator><creator>Ahmad, Naina</creator><creator>Langer, Robert</creator><creator>Mitragotri, Samir</creator><creator>Prasad Shastri, V.</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>7X8</scope></search><sort><creationdate>20060203</creationdate><title>Evaluation of chemical enhancers in the transdermal delivery of lidocaine</title><author>Lee, Philip J. ; Ahmad, Naina ; Langer, Robert ; Mitragotri, Samir ; Prasad Shastri, V.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c484t-78bf7d348b89020914caeb4d836b36dade0ad7dca90fff398d85b903065fafad3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Administration, Cutaneous</topic><topic>Anesthetics, Local - administration & dosage</topic><topic>Anesthetics, Local - chemistry</topic><topic>Anesthetics, Local - metabolism</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Chemical enhancers</topic><topic>Drug Combinations</topic><topic>Drug Delivery Systems</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Hydrophobic and Hydrophilic Interactions</topic><topic>In Vitro Techniques</topic><topic>Lidocaine</topic><topic>Lidocaine - administration & dosage</topic><topic>Lidocaine - chemistry</topic><topic>Lidocaine - metabolism</topic><topic>Medical sciences</topic><topic>Myristates - administration & dosage</topic><topic>Myristates - pharmacology</topic><topic>n-Methyl pyrrolidone</topic><topic>Pharmaceutic Aids - administration & dosage</topic><topic>Pharmaceutic Aids - pharmacology</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrrolidinones - administration & dosage</topic><topic>Pyrrolidinones - pharmacology</topic><topic>Skin Absorption - drug effects</topic><topic>Solubility</topic><topic>Swine</topic><topic>Transdermal drug delivery</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lee, Philip J.</creatorcontrib><creatorcontrib>Ahmad, Naina</creatorcontrib><creatorcontrib>Langer, Robert</creatorcontrib><creatorcontrib>Mitragotri, Samir</creatorcontrib><creatorcontrib>Prasad Shastri, V.</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>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lee, Philip J.</au><au>Ahmad, Naina</au><au>Langer, Robert</au><au>Mitragotri, Samir</au><au>Prasad Shastri, V.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of chemical enhancers in the transdermal delivery of lidocaine</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2006-02-03</date><risdate>2006</risdate><volume>308</volume><issue>1</issue><spage>33</spage><epage>39</epage><pages>33-39</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The effect of various classes of chemical enhancers was investigated for the transdermal delivery of the anesthetic lidocaine across pig and human skin in vitro. The lipid disrupting agents (LDA) oleic acid, oleyl alcohol, butenediol, and decanoic acid by themselves or in combination with isopropyl myristate (IPM) showed no significant flux enhancement. However, the binary system of IPM/
n-methyl pyrrolidone (IPM/NMP) improved drug transport. At 2% lidocaine dose, this synergistic enhancement peaked at 25:75 (v/v) IPM:NMP with a steady state flux of 57.6
±
8.4
μg
cm
−2
h
−1 through human skin. This observed flux corresponds to a four-fold enhancement over a 100% NMP solution and over 25-fold increase over 100% IPM at the same drug concentration (
p
<
0.001). NMP was also found to co-transport through human skin with lidocaine free base and improve enhancement due to LDA. These findings allow a more rational approach for designing oil-based formulations for the transdermal delivery of lidocaine free base and similar drugs.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>16321488</pmid><doi>10.1016/j.ijpharm.2005.10.027</doi><tpages>7</tpages></addata></record> |
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| subjects | Administration, Cutaneous Anesthetics, Local - administration & dosage Anesthetics, Local - chemistry Anesthetics, Local - metabolism Animals Biological and medical sciences Chemical enhancers Drug Combinations Drug Delivery Systems General pharmacology Humans Hydrophobic and Hydrophilic Interactions In Vitro Techniques Lidocaine Lidocaine - administration & dosage Lidocaine - chemistry Lidocaine - metabolism Medical sciences Myristates - administration & dosage Myristates - pharmacology n-Methyl pyrrolidone Pharmaceutic Aids - administration & dosage Pharmaceutic Aids - pharmacology Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Pyrrolidinones - administration & dosage Pyrrolidinones - pharmacology Skin Absorption - drug effects Solubility Swine Transdermal drug delivery |
| title | Evaluation of chemical enhancers in the transdermal delivery of lidocaine |
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