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Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery
To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery. ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro. While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontop...
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| Published in: | Pharmaceutical research 2006-08, Vol.23 (8), p.1842-1849 |
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| creator | ABLA, Nada NAIK, Aarti GUY, Richard H KALIA, Yogeshvar N |
| description | To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery.
ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro.
While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontophoresed into the skin than the parent molecule, ACV, only the latter was detectable in the receptor chamber, suggesting that VCV was enzymatically cleaved into the active metabolite during skin transit. Iontophoresis of VCV was significantly more efficient than that of ACV; the cumulative permeation of ACV after 1, 2 and 3 h of VCV iontophoresis at 0.5 mA cm(-2) and using an aqueous 2 mM (approximately 0.06%) formulation was 20+/-10, 104+/-47 and 194+/- 82 microg cm( -2), respectively (cf. non-quantifiable levels, 0.1 and 1.0+/-0.7 microg cm(-2) after ACV iontophoresis).
These delivery rates provide ample room to reduce either current density or the duration of current application. Preliminary in vitro data serve to emphasize the potential of VCV iontophoresis to improve the topical therapy of cutaneous herpes simplex infections and merit further investigation to demonstrate clinical efficacy. |
| doi_str_mv | 10.1007/s11095-006-9017-2 |
| format | article |
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ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro.
While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontophoresed into the skin than the parent molecule, ACV, only the latter was detectable in the receptor chamber, suggesting that VCV was enzymatically cleaved into the active metabolite during skin transit. Iontophoresis of VCV was significantly more efficient than that of ACV; the cumulative permeation of ACV after 1, 2 and 3 h of VCV iontophoresis at 0.5 mA cm(-2) and using an aqueous 2 mM (approximately 0.06%) formulation was 20+/-10, 104+/-47 and 194+/- 82 microg cm( -2), respectively (cf. non-quantifiable levels, 0.1 and 1.0+/-0.7 microg cm(-2) after ACV iontophoresis).
These delivery rates provide ample room to reduce either current density or the duration of current application. Preliminary in vitro data serve to emphasize the potential of VCV iontophoresis to improve the topical therapy of cutaneous herpes simplex infections and merit further investigation to demonstrate clinical efficacy.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1007/s11095-006-9017-2</identifier><identifier>PMID: 16850271</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>Acyclovir - administration & dosage ; Acyclovir - analogs & derivatives ; Acyclovir - pharmacokinetics ; Administration, Topical ; Algorithms ; Animals ; Antiviral Agents - administration & dosage ; Antiviral Agents - pharmacokinetics ; Biological and medical sciences ; Chromatography, High Pressure Liquid ; Drug Delivery Systems ; Drug dosages ; Epidermis - metabolism ; General pharmacology ; Herpes viruses ; Humans ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Iontophoresis ; Medical sciences ; Mice ; Mice, Hairless ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology ; Pharmacology. Drug treatments ; Prodrugs ; Rabbits ; Rodents ; Skin ; Skin Absorption - physiology ; Spectrophotometry, Ultraviolet ; Swine ; Transdermal medication ; Valine - administration & dosage ; Valine - analogs & derivatives ; Valine - pharmacokinetics</subject><ispartof>Pharmaceutical research, 2006-08, Vol.23 (8), p.1842-1849</ispartof><rights>2006 INIST-CNRS</rights><rights>Springer Science+Business Media, Inc. 2006</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-83723f55d2a47ef9b261ab7665d38f40e0dcdbf5b3dbf260308ab789ed333fe13</citedby><cites>FETCH-LOGICAL-c430t-83723f55d2a47ef9b261ab7665d38f40e0dcdbf5b3dbf260308ab789ed333fe13</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18082726$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16850271$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>ABLA, Nada</creatorcontrib><creatorcontrib>NAIK, Aarti</creatorcontrib><creatorcontrib>GUY, Richard H</creatorcontrib><creatorcontrib>KALIA, Yogeshvar N</creatorcontrib><title>Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery.
ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro.
While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontophoresed into the skin than the parent molecule, ACV, only the latter was detectable in the receptor chamber, suggesting that VCV was enzymatically cleaved into the active metabolite during skin transit. Iontophoresis of VCV was significantly more efficient than that of ACV; the cumulative permeation of ACV after 1, 2 and 3 h of VCV iontophoresis at 0.5 mA cm(-2) and using an aqueous 2 mM (approximately 0.06%) formulation was 20+/-10, 104+/-47 and 194+/- 82 microg cm( -2), respectively (cf. non-quantifiable levels, 0.1 and 1.0+/-0.7 microg cm(-2) after ACV iontophoresis).
These delivery rates provide ample room to reduce either current density or the duration of current application. Preliminary in vitro data serve to emphasize the potential of VCV iontophoresis to improve the topical therapy of cutaneous herpes simplex infections and merit further investigation to demonstrate clinical efficacy.</description><subject>Acyclovir - administration & dosage</subject><subject>Acyclovir - analogs & derivatives</subject><subject>Acyclovir - pharmacokinetics</subject><subject>Administration, Topical</subject><subject>Algorithms</subject><subject>Animals</subject><subject>Antiviral Agents - administration & dosage</subject><subject>Antiviral Agents - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Drug Delivery Systems</subject><subject>Drug dosages</subject><subject>Epidermis - metabolism</subject><subject>General pharmacology</subject><subject>Herpes viruses</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>In Vitro Techniques</subject><subject>Iontophoresis</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Hairless</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Prodrugs</subject><subject>Rabbits</subject><subject>Rodents</subject><subject>Skin</subject><subject>Skin Absorption - physiology</subject><subject>Spectrophotometry, Ultraviolet</subject><subject>Swine</subject><subject>Transdermal medication</subject><subject>Valine - administration & dosage</subject><subject>Valine - analogs & derivatives</subject><subject>Valine - pharmacokinetics</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><recordid>eNqFkU1rGzEQhkVIiV0nPyCXsATS27aj0a6kPQaTfoChlxSSk9DqA8usLUfyGvzvq2CDIZdcNAg98zKah5BbCt8pgPiRKYWurQF43QEVNV6QKW0FK7fm5ZJMQWBTS9HQCfma8woAJO2aKzKhXLaAgk7J63PcBqOHKsTNLm6XMbkcchV9tdeDNsEMcR9StTzYFM1yiClYV4X1NsW9y5UZd3rj4pirM2rdEPYuHa7JF6-H7G5OdUb-_Xx6nv-uF39__Zk_LmrTMNjVkglkvm0t6kY43_XIqe4F561l0jfgwBrb-7Zn5UQODGR5lp2zjDHvKJuRb8fcMtPb6PJOrUM2bhiOkykuETqE5lMQKTIUJXVG7j-AqzimTfmEQkTetWWLBaJHyKSYc3JebVNY63RQFNS7HXW0o4od9W5HYem5OwWP_drZc8dJRwEeToDORYpPemNCPnMSJArk7D_JpZjf</recordid><startdate>20060801</startdate><enddate>20060801</enddate><creator>ABLA, Nada</creator><creator>NAIK, Aarti</creator><creator>GUY, Richard H</creator><creator>KALIA, Yogeshvar N</creator><general>Springer</general><general>Springer Nature B.V</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>3V.</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>20060801</creationdate><title>Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery</title><author>ABLA, Nada ; NAIK, Aarti ; GUY, Richard H ; KALIA, Yogeshvar N</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-83723f55d2a47ef9b261ab7665d38f40e0dcdbf5b3dbf260308ab789ed333fe13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Acyclovir - administration & dosage</topic><topic>Acyclovir - analogs & derivatives</topic><topic>Acyclovir - pharmacokinetics</topic><topic>Administration, Topical</topic><topic>Algorithms</topic><topic>Animals</topic><topic>Antiviral Agents - administration & dosage</topic><topic>Antiviral Agents - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Drug Delivery Systems</topic><topic>Drug dosages</topic><topic>Epidermis - metabolism</topic><topic>General pharmacology</topic><topic>Herpes viruses</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>In Vitro Techniques</topic><topic>Iontophoresis</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Hairless</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Prodrugs</topic><topic>Rabbits</topic><topic>Rodents</topic><topic>Skin</topic><topic>Skin Absorption - physiology</topic><topic>Spectrophotometry, Ultraviolet</topic><topic>Swine</topic><topic>Transdermal medication</topic><topic>Valine - administration & dosage</topic><topic>Valine - analogs & derivatives</topic><topic>Valine - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>ABLA, Nada</creatorcontrib><creatorcontrib>NAIK, Aarti</creatorcontrib><creatorcontrib>GUY, Richard H</creatorcontrib><creatorcontrib>KALIA, Yogeshvar N</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>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni)</collection><collection>ProQuest Central</collection><collection>AUTh Library subscriptions: ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>ABLA, Nada</au><au>NAIK, Aarti</au><au>GUY, Richard H</au><au>KALIA, Yogeshvar N</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>2006-08-01</date><risdate>2006</risdate><volume>23</volume><issue>8</issue><spage>1842</spage><epage>1849</epage><pages>1842-1849</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery.
ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro.
While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontophoresed into the skin than the parent molecule, ACV, only the latter was detectable in the receptor chamber, suggesting that VCV was enzymatically cleaved into the active metabolite during skin transit. Iontophoresis of VCV was significantly more efficient than that of ACV; the cumulative permeation of ACV after 1, 2 and 3 h of VCV iontophoresis at 0.5 mA cm(-2) and using an aqueous 2 mM (approximately 0.06%) formulation was 20+/-10, 104+/-47 and 194+/- 82 microg cm( -2), respectively (cf. non-quantifiable levels, 0.1 and 1.0+/-0.7 microg cm(-2) after ACV iontophoresis).
These delivery rates provide ample room to reduce either current density or the duration of current application. Preliminary in vitro data serve to emphasize the potential of VCV iontophoresis to improve the topical therapy of cutaneous herpes simplex infections and merit further investigation to demonstrate clinical efficacy.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>16850271</pmid><doi>10.1007/s11095-006-9017-2</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Acyclovir - administration & dosage Acyclovir - analogs & derivatives Acyclovir - pharmacokinetics Administration, Topical Algorithms Animals Antiviral Agents - administration & dosage Antiviral Agents - pharmacokinetics Biological and medical sciences Chromatography, High Pressure Liquid Drug Delivery Systems Drug dosages Epidermis - metabolism General pharmacology Herpes viruses Humans Hydrogen-Ion Concentration In Vitro Techniques Iontophoresis Medical sciences Mice Mice, Hairless Pharmaceutical technology. Pharmaceutical industry Pharmacology Pharmacology. Drug treatments Prodrugs Rabbits Rodents Skin Skin Absorption - physiology Spectrophotometry, Ultraviolet Swine Transdermal medication Valine - administration & dosage Valine - analogs & derivatives Valine - pharmacokinetics |
| title | Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery |
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