Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches
Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal delivery of glimepiride (GMD). Methods: Matrix-type transdermal patches containing GMD, drug coprecipitate or its inclusion complex were prepared using different gelling a...
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| Veröffentlicht in: | Tropical journal of pharmaceutical research 2014-09, Vol.13 (8), p.1207 |
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| creator | Ahmed, Osama A.A Ahmed, Tarek A Abdel-Naim, Ashraf B Khedr, Alaa Banjar, Zainy M Afouna, Mohsen I |
| description | Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and
polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal
delivery of glimepiride (GMD). Methods: Matrix-type transdermal patches
containing GMD, drug coprecipitate or its inclusion complex were
prepared using different gelling agents, viz, hydroxypropyl
methylcellulose (HPMC), hydroxypropyl cellulose (HPC), carbopol and
chitosan. In vitro skin permeation evaluation of the formulations was
conducted using automated diffusion system. Selected patch formulations
were assessed for hypoglycemic activity as well as for GMD plasma
concentration in rats. Results: GMD- hydroxybutyl-β-cyclodextrin
(HB-β-CD) binary systems (1:2 molar ratio) enhanced GMD aqueous
solubility by > 10-fold. Diffusion test showed improved release of
GMD-HB-β-CD inclusion complex compared with GMD alone. Maximum
cumulative amounts of GMD- HB-β-CD that permeated through rat skin
was 26.97 and 14.28 μg/cm2 for patches prepared with fchitosan and
HPMC, respectively. Thus, GMD-chitosan patches showed significantly
higher (p < 0.05) drug permeation than GMD-HPMC after 6 h. Both
chitosan and HPMC patches of GMD-HB-β-CD demonstrated substantial
reduction (p < 0.05) in blood glucose level (192.67 ± 21.18 and
201 ± 15.11 mg/ dl, respectively), compared with the baseline
value of 240 mg/ dl. Conclusion: Application of chitosan and HPMC
transdermal patches of GMD-HB-β-CD can serve as a potential
alternative to peroral GMD with improved bioavailability and patient
compliance. |
| doi_str_mv | 10.4314/tjpr.v13i8.3 |
| format | Article |
| fullrecord | <record><control><sourceid>bioline_cross</sourceid><recordid>TN_cdi_crossref_primary_10_4314_tjpr_v13i8_3</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>cria_bioline_pr_pr14167</sourcerecordid><originalsourceid>FETCH-LOGICAL-b189t-91c69c572b3b7ca4fca3932cadcf2b09479fd71cfbeb14e95a40957cd0155af03</originalsourceid><addsrcrecordid>eNpFkFFLwzAQx4MoOKdvfoB8AFuTJmmWRxlzGwwUnL6G9Jq4bG1a0jLot3ezQ-Hgjrvf7x7-CD1SknJG-XO_b2N6pMzPUnaFJlSoPFGzTF5fZqFUfovuum5PiMiVohN0WISdCWBrG3rcOLwO-Mv3scEfBx_wNprQtU3ssQnleDs2eDW0zXc1nCQPeOGcBwPDWV5Wvratj760o1raWJsKv5sedra7RzfOVJ19uPQp-nxdbOerZPO2XM9fNklBZ6pPFIVcgZBZwQoJhjswTLEMTAkuK4jiUrlSUnCFLSi3ShhOlJBQEiqEcYRN0dP4F2LTddE63UZfmzhoSvQ5KH0OSv8GpdkJT0e88E3lg_2jIXqj_5enopzmkv0AuRFwfg</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches</title><source>DOAJ Directory of Open Access Journals</source><source>African Journals Online (Open Access)</source><source>Bioline International</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Free Full-Text Journals in Chemistry</source><creator>Ahmed, Osama A.A ; Ahmed, Tarek A ; Abdel-Naim, Ashraf B ; Khedr, Alaa ; Banjar, Zainy M ; Afouna, Mohsen I</creator><creatorcontrib>Ahmed, Osama A.A ; Ahmed, Tarek A ; Abdel-Naim, Ashraf B ; Khedr, Alaa ; Banjar, Zainy M ; Afouna, Mohsen I</creatorcontrib><description>Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and
polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal
delivery of glimepiride (GMD). Methods: Matrix-type transdermal patches
containing GMD, drug coprecipitate or its inclusion complex were
prepared using different gelling agents, viz, hydroxypropyl
methylcellulose (HPMC), hydroxypropyl cellulose (HPC), carbopol and
chitosan. In vitro skin permeation evaluation of the formulations was
conducted using automated diffusion system. Selected patch formulations
were assessed for hypoglycemic activity as well as for GMD plasma
concentration in rats. Results: GMD- hydroxybutyl-β-cyclodextrin
(HB-β-CD) binary systems (1:2 molar ratio) enhanced GMD aqueous
solubility by > 10-fold. Diffusion test showed improved release of
GMD-HB-β-CD inclusion complex compared with GMD alone. Maximum
cumulative amounts of GMD- HB-β-CD that permeated through rat skin
was 26.97 and 14.28 μg/cm2 for patches prepared with fchitosan and
HPMC, respectively. Thus, GMD-chitosan patches showed significantly
higher (p < 0.05) drug permeation than GMD-HPMC after 6 h. Both
chitosan and HPMC patches of GMD-HB-β-CD demonstrated substantial
reduction (p < 0.05) in blood glucose level (192.67 ± 21.18 and
201 ± 15.11 mg/ dl, respectively), compared with the baseline
value of 240 mg/ dl. Conclusion: Application of chitosan and HPMC
transdermal patches of GMD-HB-β-CD can serve as a potential
alternative to peroral GMD with improved bioavailability and patient
compliance.</description><identifier>ISSN: 1596-5996</identifier><identifier>EISSN: 1596-9827</identifier><identifier>DOI: 10.4314/tjpr.v13i8.3</identifier><language>eng</language><publisher>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</publisher><subject>Chitosan ; Coprecipitate ; Glimepiride ; Hydroxypropyl methylcellulose ; Inclusion complex ; Polyvinyl pyrrolidone ; Skin permeation ; Transdermal patch</subject><ispartof>Tropical journal of pharmaceutical research, 2014-09, Vol.13 (8), p.1207</ispartof><rights>Copyright 2014 - Tropical Journal of Pharmaceutical Research</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-b189t-91c69c572b3b7ca4fca3932cadcf2b09479fd71cfbeb14e95a40957cd0155af03</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,864,27924,27925,79426</link.rule.ids></links><search><creatorcontrib>Ahmed, Osama A.A</creatorcontrib><creatorcontrib>Ahmed, Tarek A</creatorcontrib><creatorcontrib>Abdel-Naim, Ashraf B</creatorcontrib><creatorcontrib>Khedr, Alaa</creatorcontrib><creatorcontrib>Banjar, Zainy M</creatorcontrib><creatorcontrib>Afouna, Mohsen I</creatorcontrib><title>Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches</title><title>Tropical journal of pharmaceutical research</title><description>Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and
polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal
delivery of glimepiride (GMD). Methods: Matrix-type transdermal patches
containing GMD, drug coprecipitate or its inclusion complex were
prepared using different gelling agents, viz, hydroxypropyl
methylcellulose (HPMC), hydroxypropyl cellulose (HPC), carbopol and
chitosan. In vitro skin permeation evaluation of the formulations was
conducted using automated diffusion system. Selected patch formulations
were assessed for hypoglycemic activity as well as for GMD plasma
concentration in rats. Results: GMD- hydroxybutyl-β-cyclodextrin
(HB-β-CD) binary systems (1:2 molar ratio) enhanced GMD aqueous
solubility by > 10-fold. Diffusion test showed improved release of
GMD-HB-β-CD inclusion complex compared with GMD alone. Maximum
cumulative amounts of GMD- HB-β-CD that permeated through rat skin
was 26.97 and 14.28 μg/cm2 for patches prepared with fchitosan and
HPMC, respectively. Thus, GMD-chitosan patches showed significantly
higher (p < 0.05) drug permeation than GMD-HPMC after 6 h. Both
chitosan and HPMC patches of GMD-HB-β-CD demonstrated substantial
reduction (p < 0.05) in blood glucose level (192.67 ± 21.18 and
201 ± 15.11 mg/ dl, respectively), compared with the baseline
value of 240 mg/ dl. Conclusion: Application of chitosan and HPMC
transdermal patches of GMD-HB-β-CD can serve as a potential
alternative to peroral GMD with improved bioavailability and patient
compliance.</description><subject>Chitosan</subject><subject>Coprecipitate</subject><subject>Glimepiride</subject><subject>Hydroxypropyl methylcellulose</subject><subject>Inclusion complex</subject><subject>Polyvinyl pyrrolidone</subject><subject>Skin permeation</subject><subject>Transdermal patch</subject><issn>1596-5996</issn><issn>1596-9827</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>RBI</sourceid><recordid>eNpFkFFLwzAQx4MoOKdvfoB8AFuTJmmWRxlzGwwUnL6G9Jq4bG1a0jLot3ezQ-Hgjrvf7x7-CD1SknJG-XO_b2N6pMzPUnaFJlSoPFGzTF5fZqFUfovuum5PiMiVohN0WISdCWBrG3rcOLwO-Mv3scEfBx_wNprQtU3ssQnleDs2eDW0zXc1nCQPeOGcBwPDWV5Wvratj760o1raWJsKv5sedra7RzfOVJ19uPQp-nxdbOerZPO2XM9fNklBZ6pPFIVcgZBZwQoJhjswTLEMTAkuK4jiUrlSUnCFLSi3ShhOlJBQEiqEcYRN0dP4F2LTddE63UZfmzhoSvQ5KH0OSv8GpdkJT0e88E3lg_2jIXqj_5enopzmkv0AuRFwfg</recordid><startdate>20140923</startdate><enddate>20140923</enddate><creator>Ahmed, Osama A.A</creator><creator>Ahmed, Tarek A</creator><creator>Abdel-Naim, Ashraf B</creator><creator>Khedr, Alaa</creator><creator>Banjar, Zainy M</creator><creator>Afouna, Mohsen I</creator><general>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</general><scope>RBI</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20140923</creationdate><title>Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches</title><author>Ahmed, Osama A.A ; Ahmed, Tarek A ; Abdel-Naim, Ashraf B ; Khedr, Alaa ; Banjar, Zainy M ; Afouna, Mohsen I</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-b189t-91c69c572b3b7ca4fca3932cadcf2b09479fd71cfbeb14e95a40957cd0155af03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Chitosan</topic><topic>Coprecipitate</topic><topic>Glimepiride</topic><topic>Hydroxypropyl methylcellulose</topic><topic>Inclusion complex</topic><topic>Polyvinyl pyrrolidone</topic><topic>Skin permeation</topic><topic>Transdermal patch</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ahmed, Osama A.A</creatorcontrib><creatorcontrib>Ahmed, Tarek A</creatorcontrib><creatorcontrib>Abdel-Naim, Ashraf B</creatorcontrib><creatorcontrib>Khedr, Alaa</creatorcontrib><creatorcontrib>Banjar, Zainy M</creatorcontrib><creatorcontrib>Afouna, Mohsen I</creatorcontrib><collection>Bioline International</collection><collection>CrossRef</collection><jtitle>Tropical journal of pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ahmed, Osama A.A</au><au>Ahmed, Tarek A</au><au>Abdel-Naim, Ashraf B</au><au>Khedr, Alaa</au><au>Banjar, Zainy M</au><au>Afouna, Mohsen I</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches</atitle><jtitle>Tropical journal of pharmaceutical research</jtitle><date>2014-09-23</date><risdate>2014</risdate><volume>13</volume><issue>8</issue><spage>1207</spage><pages>1207-</pages><issn>1596-5996</issn><eissn>1596-9827</eissn><abstract>Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and
polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal
delivery of glimepiride (GMD). Methods: Matrix-type transdermal patches
containing GMD, drug coprecipitate or its inclusion complex were
prepared using different gelling agents, viz, hydroxypropyl
methylcellulose (HPMC), hydroxypropyl cellulose (HPC), carbopol and
chitosan. In vitro skin permeation evaluation of the formulations was
conducted using automated diffusion system. Selected patch formulations
were assessed for hypoglycemic activity as well as for GMD plasma
concentration in rats. Results: GMD- hydroxybutyl-β-cyclodextrin
(HB-β-CD) binary systems (1:2 molar ratio) enhanced GMD aqueous
solubility by > 10-fold. Diffusion test showed improved release of
GMD-HB-β-CD inclusion complex compared with GMD alone. Maximum
cumulative amounts of GMD- HB-β-CD that permeated through rat skin
was 26.97 and 14.28 μg/cm2 for patches prepared with fchitosan and
HPMC, respectively. Thus, GMD-chitosan patches showed significantly
higher (p < 0.05) drug permeation than GMD-HPMC after 6 h. Both
chitosan and HPMC patches of GMD-HB-β-CD demonstrated substantial
reduction (p < 0.05) in blood glucose level (192.67 ± 21.18 and
201 ± 15.11 mg/ dl, respectively), compared with the baseline
value of 240 mg/ dl. Conclusion: Application of chitosan and HPMC
transdermal patches of GMD-HB-β-CD can serve as a potential
alternative to peroral GMD with improved bioavailability and patient
compliance.</abstract><pub>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</pub><doi>10.4314/tjpr.v13i8.3</doi></addata></record> |
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| ispartof | Tropical journal of pharmaceutical research, 2014-09, Vol.13 (8), p.1207 |
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| language | eng |
| recordid | cdi_crossref_primary_10_4314_tjpr_v13i8_3 |
| source | DOAJ Directory of Open Access Journals; African Journals Online (Open Access); Bioline International; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Chitosan Coprecipitate Glimepiride Hydroxypropyl methylcellulose Inclusion complex Polyvinyl pyrrolidone Skin permeation Transdermal patch |
| title | Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches |
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