Iontophoretic transport of charged macromolecules across human sclera
The mechanisms of transscleral iontophoresis have been investigated previously with small molecules in rabbit sclera. The objective of the present study was to examine transscleral iontophoretic transport of charged macromolecules across excised human sclera. Passive and 2 mA iontophoretic transport...
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description | The mechanisms of transscleral iontophoresis have been investigated previously with small molecules in rabbit sclera. The objective of the present study was to examine transscleral iontophoretic transport of charged macromolecules across excised human sclera. Passive and 2
mA iontophoretic transport experiments were conducted in side-by-side diffusion cells with human sclera. The effects of iontophoresis upon transscleral transport of model permeants bovine serum albumin (BSA) and polystyrene sulfonic acid (PSS) as well as a model drug bevacizumab (BEV) were determined. Passive and iontophoretic transport experiments of tetraethylammonium (TEA) and salicylic acid (SA) and passive transport experiments of the macromolecules served as the controls. The results of iontophoresis enhanced transport of TEA and SA across human sclera were consistent with those in a previous rabbit sclera study. For the iontophoretic transport of macromolecules BSA and BEV, higher iontophoretic fluxes were observed in anodal iontophoresis as compared to passive and cathodal iontophoresis. This suggests the importance of electroosmosis. For the polyelectrolyte PSS, higher iontophoretic flux was observed in cathodal iontophoresis compared to anodal iontophoresis. Both electroosmosis and electrophoresis affected iontophoretic fluxes of the macromolecules; the relative contributions of electroosmosis and electrophoresis were a function of molecular size and charge of the macromolecules. |
doi_str_mv | 10.1016/j.ijpharm.2009.12.046 |
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mA iontophoretic transport experiments were conducted in side-by-side diffusion cells with human sclera. The effects of iontophoresis upon transscleral transport of model permeants bovine serum albumin (BSA) and polystyrene sulfonic acid (PSS) as well as a model drug bevacizumab (BEV) were determined. Passive and iontophoretic transport experiments of tetraethylammonium (TEA) and salicylic acid (SA) and passive transport experiments of the macromolecules served as the controls. The results of iontophoresis enhanced transport of TEA and SA across human sclera were consistent with those in a previous rabbit sclera study. For the iontophoretic transport of macromolecules BSA and BEV, higher iontophoretic fluxes were observed in anodal iontophoresis as compared to passive and cathodal iontophoresis. This suggests the importance of electroosmosis. For the polyelectrolyte PSS, higher iontophoretic flux was observed in cathodal iontophoresis compared to anodal iontophoresis. Both electroosmosis and electrophoresis affected iontophoretic fluxes of the macromolecules; the relative contributions of electroosmosis and electrophoresis were a function of molecular size and charge of the macromolecules.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2009.12.046</identifier><identifier>PMID: 20045044</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Administration, Topical ; Animals ; Antibodies, Monoclonal - administration & dosage ; Antibodies, Monoclonal - pharmacokinetics ; Antibodies, Monoclonal, Humanized ; Bevacizumab ; Biological and medical sciences ; Biological Transport ; Cattle ; Charged macromolecules ; Electroosmosis ; Electrophoresis ; General pharmacology ; Human sclera ; Humans ; Iontophoresis ; Medical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Polystyrenes - administration & dosage ; Polystyrenes - pharmacokinetics ; Rabbits ; Salicylic Acid - administration & dosage ; Salicylic Acid - pharmacokinetics ; Sclera - metabolism ; Serum Albumin, Bovine - administration & dosage ; Serum Albumin, Bovine - pharmacokinetics ; Tetraethylammonium - administration & dosage ; Tetraethylammonium - pharmacokinetics</subject><ispartof>International journal of pharmaceutics, 2010-03, Vol.388 (1), p.107-113</ispartof><rights>2009 Elsevier B.V.</rights><rights>2015 INIST-CNRS</rights><rights>Copyright (c) 2009 Elsevier B.V. All rights reserved.</rights><rights>2009 Elsevier B.V. All rights reserved. 2009</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c562t-66b62b57c59ab3132b7f9bae337f8d4573a1ebc9e3527872028c1df1f30838893</citedby><cites>FETCH-LOGICAL-c562t-66b62b57c59ab3132b7f9bae337f8d4573a1ebc9e3527872028c1df1f30838893</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.2009.12.046$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3536,27903,27904,45974</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22605608$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20045044$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chopra, Poonam</creatorcontrib><creatorcontrib>Hao, Jinsong</creatorcontrib><creatorcontrib>Li, S. Kevin</creatorcontrib><title>Iontophoretic transport of charged macromolecules across human sclera</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The mechanisms of transscleral iontophoresis have been investigated previously with small molecules in rabbit sclera. The objective of the present study was to examine transscleral iontophoretic transport of charged macromolecules across excised human sclera. Passive and 2
mA iontophoretic transport experiments were conducted in side-by-side diffusion cells with human sclera. The effects of iontophoresis upon transscleral transport of model permeants bovine serum albumin (BSA) and polystyrene sulfonic acid (PSS) as well as a model drug bevacizumab (BEV) were determined. Passive and iontophoretic transport experiments of tetraethylammonium (TEA) and salicylic acid (SA) and passive transport experiments of the macromolecules served as the controls. The results of iontophoresis enhanced transport of TEA and SA across human sclera were consistent with those in a previous rabbit sclera study. For the iontophoretic transport of macromolecules BSA and BEV, higher iontophoretic fluxes were observed in anodal iontophoresis as compared to passive and cathodal iontophoresis. This suggests the importance of electroosmosis. For the polyelectrolyte PSS, higher iontophoretic flux was observed in cathodal iontophoresis compared to anodal iontophoresis. Both electroosmosis and electrophoresis affected iontophoretic fluxes of the macromolecules; the relative contributions of electroosmosis and electrophoresis were a function of molecular size and charge of the macromolecules.</description><subject>Administration, Topical</subject><subject>Animals</subject><subject>Antibodies, Monoclonal - administration & dosage</subject><subject>Antibodies, Monoclonal - pharmacokinetics</subject><subject>Antibodies, Monoclonal, Humanized</subject><subject>Bevacizumab</subject><subject>Biological and medical sciences</subject><subject>Biological Transport</subject><subject>Cattle</subject><subject>Charged macromolecules</subject><subject>Electroosmosis</subject><subject>Electrophoresis</subject><subject>General pharmacology</subject><subject>Human sclera</subject><subject>Humans</subject><subject>Iontophoresis</subject><subject>Medical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polystyrenes - administration & dosage</subject><subject>Polystyrenes - pharmacokinetics</subject><subject>Rabbits</subject><subject>Salicylic Acid - administration & dosage</subject><subject>Salicylic Acid - pharmacokinetics</subject><subject>Sclera - metabolism</subject><subject>Serum Albumin, Bovine - administration & dosage</subject><subject>Serum Albumin, Bovine - pharmacokinetics</subject><subject>Tetraethylammonium - administration & dosage</subject><subject>Tetraethylammonium - pharmacokinetics</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMlOwzAURS0EglL4BFA2LBM8xHayASHEUKkSG1hbjvPSukriyE4r8fe4tEwrVpble67fOwhdEJwRTMT1KrOrYal9l1GMy4zQDOfiAE1IIVnKcikO0QQzWaScSHaCTkNYYYwFJewYnUQk5zjPJ-hh5vrRDUvnYbQmGb3uw-D8mLgmMbF-AXXSaeNd51ow6xZCsr2FkCzXne6TYFrw-gwdNboNcL4_p-jt8eH1_jmdvzzN7u_mqeGCjqkQlaAVl4aXumKE0Uo2ZaWBMdkUdc4l0wQqUwLjVBaSYloYUjekYbhgRVGyKbrZ9Q7rqoPaQB8HbtXgbaf9u3Laqr8vvV2qhdsoGnlBWCzgu4LPHTw03yzBautVrdTeq9p6VYSq6DVyl78__qa-RMbA1T6gg9FtEz0aG35yVGAu4hZTdLvLQdS0seBVMBZ6A7X1YEZVO_vPKB_htJr_</recordid><startdate>20100330</startdate><enddate>20100330</enddate><creator>Chopra, Poonam</creator><creator>Hao, Jinsong</creator><creator>Li, S. Kevin</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>5PM</scope></search><sort><creationdate>20100330</creationdate><title>Iontophoretic transport of charged macromolecules across human sclera</title><author>Chopra, Poonam ; Hao, Jinsong ; Li, S. Kevin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c562t-66b62b57c59ab3132b7f9bae337f8d4573a1ebc9e3527872028c1df1f30838893</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Administration, Topical</topic><topic>Animals</topic><topic>Antibodies, Monoclonal - administration & dosage</topic><topic>Antibodies, Monoclonal - pharmacokinetics</topic><topic>Antibodies, Monoclonal, Humanized</topic><topic>Bevacizumab</topic><topic>Biological and medical sciences</topic><topic>Biological Transport</topic><topic>Cattle</topic><topic>Charged macromolecules</topic><topic>Electroosmosis</topic><topic>Electrophoresis</topic><topic>General pharmacology</topic><topic>Human sclera</topic><topic>Humans</topic><topic>Iontophoresis</topic><topic>Medical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polystyrenes - administration & dosage</topic><topic>Polystyrenes - pharmacokinetics</topic><topic>Rabbits</topic><topic>Salicylic Acid - administration & dosage</topic><topic>Salicylic Acid - pharmacokinetics</topic><topic>Sclera - metabolism</topic><topic>Serum Albumin, Bovine - administration & dosage</topic><topic>Serum Albumin, Bovine - pharmacokinetics</topic><topic>Tetraethylammonium - administration & dosage</topic><topic>Tetraethylammonium - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chopra, Poonam</creatorcontrib><creatorcontrib>Hao, Jinsong</creatorcontrib><creatorcontrib>Li, S. 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Kevin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Iontophoretic transport of charged macromolecules across human sclera</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2010-03-30</date><risdate>2010</risdate><volume>388</volume><issue>1</issue><spage>107</spage><epage>113</epage><pages>107-113</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The mechanisms of transscleral iontophoresis have been investigated previously with small molecules in rabbit sclera. The objective of the present study was to examine transscleral iontophoretic transport of charged macromolecules across excised human sclera. Passive and 2
mA iontophoretic transport experiments were conducted in side-by-side diffusion cells with human sclera. The effects of iontophoresis upon transscleral transport of model permeants bovine serum albumin (BSA) and polystyrene sulfonic acid (PSS) as well as a model drug bevacizumab (BEV) were determined. Passive and iontophoretic transport experiments of tetraethylammonium (TEA) and salicylic acid (SA) and passive transport experiments of the macromolecules served as the controls. The results of iontophoresis enhanced transport of TEA and SA across human sclera were consistent with those in a previous rabbit sclera study. For the iontophoretic transport of macromolecules BSA and BEV, higher iontophoretic fluxes were observed in anodal iontophoresis as compared to passive and cathodal iontophoresis. This suggests the importance of electroosmosis. For the polyelectrolyte PSS, higher iontophoretic flux was observed in cathodal iontophoresis compared to anodal iontophoresis. Both electroosmosis and electrophoresis affected iontophoretic fluxes of the macromolecules; the relative contributions of electroosmosis and electrophoresis were a function of molecular size and charge of the macromolecules.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>20045044</pmid><doi>10.1016/j.ijpharm.2009.12.046</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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subjects | Administration, Topical Animals Antibodies, Monoclonal - administration & dosage Antibodies, Monoclonal - pharmacokinetics Antibodies, Monoclonal, Humanized Bevacizumab Biological and medical sciences Biological Transport Cattle Charged macromolecules Electroosmosis Electrophoresis General pharmacology Human sclera Humans Iontophoresis Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polystyrenes - administration & dosage Polystyrenes - pharmacokinetics Rabbits Salicylic Acid - administration & dosage Salicylic Acid - pharmacokinetics Sclera - metabolism Serum Albumin, Bovine - administration & dosage Serum Albumin, Bovine - pharmacokinetics Tetraethylammonium - administration & dosage Tetraethylammonium - pharmacokinetics |
title | Iontophoretic transport of charged macromolecules across human sclera |
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