Transdermal microgels of gentamicin
Poloxamer 407 encapsulating phospholipid-based (P90H) solid lipid microparticles (microgels) demonstrates fast antibacterial activity and good permeation through rat skin to deliver gentamicin sulfate as an alternative transdermal low dose regimen devoid of the drug’s adverse effects. Phospholipid-m...
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Veröffentlicht in: | European journal of pharmaceutics and biopharmaceutics 2013-06, Vol.84 (2), p.345-354 |
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creator | Nnamani, P.O. Kenechukwu, F.C. Dibua, E.U. Ogbonna, C.C. Monemeh, U.L. Attama, A.A. |
description | Poloxamer 407 encapsulating phospholipid-based (P90H) solid lipid microparticles (microgels) demonstrates fast antibacterial activity and good permeation through rat skin to deliver gentamicin sulfate as an alternative transdermal low dose regimen devoid of the drug’s adverse effects.
Phospholipid-modified solid lipid microparticles (SLMs) of Phospholipon® 90G and 90H encapsulating the hydrophilic drug, gentamicin were produced and loaded into three polymeric hydrogels of Poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P). The SLMs were characterized by morphology and particle size, drug encapsulation efficiency, thermal properties, pH, and storage stability, whereas the microgels were evaluated for viscosity, spreadability, pH, drug content, and in vitro antimicrobial drug release against five microorganisms (Klebsiella spp., Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa). Our results generally showed Poloxamer 407 microgels of P90H and P90G as having the most desirable properties in terms of fast antibacterial activity on all tested microorganisms, in vitro diffusion-dependent permeation through rat abdominal skin, spreadability, pH, and viscosity, superior to polyacrylic acids microgels. |
doi_str_mv | 10.1016/j.ejpb.2012.11.015 |
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Phospholipid-modified solid lipid microparticles (SLMs) of Phospholipon® 90G and 90H encapsulating the hydrophilic drug, gentamicin were produced and loaded into three polymeric hydrogels of Poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P). The SLMs were characterized by morphology and particle size, drug encapsulation efficiency, thermal properties, pH, and storage stability, whereas the microgels were evaluated for viscosity, spreadability, pH, drug content, and in vitro antimicrobial drug release against five microorganisms (Klebsiella spp., Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa). Our results generally showed Poloxamer 407 microgels of P90H and P90G as having the most desirable properties in terms of fast antibacterial activity on all tested microorganisms, in vitro diffusion-dependent permeation through rat abdominal skin, spreadability, pH, and viscosity, superior to polyacrylic acids microgels.</description><identifier>ISSN: 0939-6411</identifier><identifier>EISSN: 1873-3441</identifier><identifier>DOI: 10.1016/j.ejpb.2012.11.015</identifier><identifier>PMID: 23220381</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Acrylates - chemistry ; Administration, Cutaneous ; Animals ; Anti-Infective Agents - administration & dosage ; Antimicrobial action ; Drug Carriers - chemistry ; Gels ; Gentamicin ; Gentamicins - administration & dosage ; Hydrogels - chemistry ; Hydrogen-Ion Concentration ; Lipids ; Male ; Microbial Sensitivity Tests ; Particle Size ; Phosphatidylcholines - chemistry ; Phospholipids - chemistry ; Poloxamer - chemistry ; Poloxamer 407 ; Polyacrylic acids ; Rats ; Rats, Wistar ; Rheology ; Skin - drug effects ; Solid lipid microparticles ; Transdermal system ; Viscosity</subject><ispartof>European journal of pharmaceutics and biopharmaceutics, 2013-06, Vol.84 (2), p.345-354</ispartof><rights>2012 Elsevier B.V.</rights><rights>Copyright © 2012 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-c908661b19423d1601a72112e49df2712a25ac93b199134557d4645e47f09613</citedby><cites>FETCH-LOGICAL-c356t-c908661b19423d1601a72112e49df2712a25ac93b199134557d4645e47f09613</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ejpb.2012.11.015$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23220381$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nnamani, P.O.</creatorcontrib><creatorcontrib>Kenechukwu, F.C.</creatorcontrib><creatorcontrib>Dibua, E.U.</creatorcontrib><creatorcontrib>Ogbonna, C.C.</creatorcontrib><creatorcontrib>Monemeh, U.L.</creatorcontrib><creatorcontrib>Attama, A.A.</creatorcontrib><title>Transdermal microgels of gentamicin</title><title>European journal of pharmaceutics and biopharmaceutics</title><addtitle>Eur J Pharm Biopharm</addtitle><description>Poloxamer 407 encapsulating phospholipid-based (P90H) solid lipid microparticles (microgels) demonstrates fast antibacterial activity and good permeation through rat skin to deliver gentamicin sulfate as an alternative transdermal low dose regimen devoid of the drug’s adverse effects.
Phospholipid-modified solid lipid microparticles (SLMs) of Phospholipon® 90G and 90H encapsulating the hydrophilic drug, gentamicin were produced and loaded into three polymeric hydrogels of Poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P). The SLMs were characterized by morphology and particle size, drug encapsulation efficiency, thermal properties, pH, and storage stability, whereas the microgels were evaluated for viscosity, spreadability, pH, drug content, and in vitro antimicrobial drug release against five microorganisms (Klebsiella spp., Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa). Our results generally showed Poloxamer 407 microgels of P90H and P90G as having the most desirable properties in terms of fast antibacterial activity on all tested microorganisms, in vitro diffusion-dependent permeation through rat abdominal skin, spreadability, pH, and viscosity, superior to polyacrylic acids microgels.</description><subject>Acrylates - chemistry</subject><subject>Administration, Cutaneous</subject><subject>Animals</subject><subject>Anti-Infective Agents - administration & dosage</subject><subject>Antimicrobial action</subject><subject>Drug Carriers - chemistry</subject><subject>Gels</subject><subject>Gentamicin</subject><subject>Gentamicins - administration & dosage</subject><subject>Hydrogels - chemistry</subject><subject>Hydrogen-Ion Concentration</subject><subject>Lipids</subject><subject>Male</subject><subject>Microbial Sensitivity Tests</subject><subject>Particle Size</subject><subject>Phosphatidylcholines - chemistry</subject><subject>Phospholipids - chemistry</subject><subject>Poloxamer - chemistry</subject><subject>Poloxamer 407</subject><subject>Polyacrylic acids</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Rheology</subject><subject>Skin - drug effects</subject><subject>Solid lipid microparticles</subject><subject>Transdermal system</subject><subject>Viscosity</subject><issn>0939-6411</issn><issn>1873-3441</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLAzEUhYMotlb_gAspuHEzY26eDbiR4gsKbroPaeZOyTCPmkwF_70pVZeuLhy-c7h8hFwDLYGCum9KbHabklFgJUBJQZ6QKSw0L7gQcEqm1HBTKAEwIRcpNZRSoeXinEwYZ4zyBUzJ7Tq6PlUYO9fOu-DjsMU2zYd6vsV-dDkJ_SU5q12b8Ornzsj6-Wm9fC1W7y9vy8dV4blUY-ENXSgFGzCC8QoUBacZAENhqpppYI5J5w3PgAEupNSVUEKi0DU1CviM3B1nd3H42GMabReSx7Z1PQ77ZIFLLYxWjGWUHdH8b0oRa7uLoXPxywK1Bze2sQc39uDGAtjsJpdufvb3mw6rv8qvjAw8HIFsAD8DRpt8wN5jFSL60VZD-G__G8rxccU</recordid><startdate>201306</startdate><enddate>201306</enddate><creator>Nnamani, P.O.</creator><creator>Kenechukwu, F.C.</creator><creator>Dibua, E.U.</creator><creator>Ogbonna, C.C.</creator><creator>Monemeh, U.L.</creator><creator>Attama, A.A.</creator><general>Elsevier B.V</general><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>201306</creationdate><title>Transdermal microgels of gentamicin</title><author>Nnamani, P.O. ; Kenechukwu, F.C. ; Dibua, E.U. ; Ogbonna, C.C. ; Monemeh, U.L. ; Attama, A.A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-c908661b19423d1601a72112e49df2712a25ac93b199134557d4645e47f09613</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Acrylates - chemistry</topic><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Anti-Infective Agents - administration & dosage</topic><topic>Antimicrobial action</topic><topic>Drug Carriers - chemistry</topic><topic>Gels</topic><topic>Gentamicin</topic><topic>Gentamicins - administration & dosage</topic><topic>Hydrogels - chemistry</topic><topic>Hydrogen-Ion Concentration</topic><topic>Lipids</topic><topic>Male</topic><topic>Microbial Sensitivity Tests</topic><topic>Particle Size</topic><topic>Phosphatidylcholines - chemistry</topic><topic>Phospholipids - chemistry</topic><topic>Poloxamer - chemistry</topic><topic>Poloxamer 407</topic><topic>Polyacrylic acids</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Rheology</topic><topic>Skin - drug effects</topic><topic>Solid lipid microparticles</topic><topic>Transdermal system</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nnamani, P.O.</creatorcontrib><creatorcontrib>Kenechukwu, F.C.</creatorcontrib><creatorcontrib>Dibua, E.U.</creatorcontrib><creatorcontrib>Ogbonna, C.C.</creatorcontrib><creatorcontrib>Monemeh, U.L.</creatorcontrib><creatorcontrib>Attama, A.A.</creatorcontrib><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>European journal of pharmaceutics and biopharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nnamani, P.O.</au><au>Kenechukwu, F.C.</au><au>Dibua, E.U.</au><au>Ogbonna, C.C.</au><au>Monemeh, U.L.</au><au>Attama, A.A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Transdermal microgels of gentamicin</atitle><jtitle>European journal of pharmaceutics and biopharmaceutics</jtitle><addtitle>Eur J Pharm Biopharm</addtitle><date>2013-06</date><risdate>2013</risdate><volume>84</volume><issue>2</issue><spage>345</spage><epage>354</epage><pages>345-354</pages><issn>0939-6411</issn><eissn>1873-3441</eissn><abstract>Poloxamer 407 encapsulating phospholipid-based (P90H) solid lipid microparticles (microgels) demonstrates fast antibacterial activity and good permeation through rat skin to deliver gentamicin sulfate as an alternative transdermal low dose regimen devoid of the drug’s adverse effects.
Phospholipid-modified solid lipid microparticles (SLMs) of Phospholipon® 90G and 90H encapsulating the hydrophilic drug, gentamicin were produced and loaded into three polymeric hydrogels of Poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P). The SLMs were characterized by morphology and particle size, drug encapsulation efficiency, thermal properties, pH, and storage stability, whereas the microgels were evaluated for viscosity, spreadability, pH, drug content, and in vitro antimicrobial drug release against five microorganisms (Klebsiella spp., Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa). Our results generally showed Poloxamer 407 microgels of P90H and P90G as having the most desirable properties in terms of fast antibacterial activity on all tested microorganisms, in vitro diffusion-dependent permeation through rat abdominal skin, spreadability, pH, and viscosity, superior to polyacrylic acids microgels.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23220381</pmid><doi>10.1016/j.ejpb.2012.11.015</doi><tpages>10</tpages></addata></record> |
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subjects | Acrylates - chemistry Administration, Cutaneous Animals Anti-Infective Agents - administration & dosage Antimicrobial action Drug Carriers - chemistry Gels Gentamicin Gentamicins - administration & dosage Hydrogels - chemistry Hydrogen-Ion Concentration Lipids Male Microbial Sensitivity Tests Particle Size Phosphatidylcholines - chemistry Phospholipids - chemistry Poloxamer - chemistry Poloxamer 407 Polyacrylic acids Rats Rats, Wistar Rheology Skin - drug effects Solid lipid microparticles Transdermal system Viscosity |
title | Transdermal microgels of gentamicin |
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