Long-circulating liposomes of indomethacin in arthritic rats — a biodisposition study
To improve the targeting efficiency of liposomes of indomethacin to the arthritic joints, circulation half-life of the liposomes was increased by grafting amphipathic polyethylene glycol-2000 to the bilayer surface. A comparative biodistribution study was performed between the conventional liposomes...
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| Veröffentlicht in: | Pharmaceutica acta Helvetiae 2000-04, Vol.74 (4), p.399-404 |
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| container_title | Pharmaceutica acta Helvetiae |
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| creator | Srinath, P. Chary, M.G. Vyas, S.P. Diwan, P.V. |
| description | To improve the targeting efficiency of liposomes of indomethacin to the arthritic joints, circulation half-life of the liposomes was increased by grafting amphipathic polyethylene glycol-2000 to the bilayer surface. A comparative biodistribution study was performed between the conventional liposomes (PC:CH:PE — 1:0.5:0.16) and long-circulating liposomes (PC:CH:PE-PEG — 1:0.5:0.16) in arthritic rats. Pharmocokinetics of the drug changed significantly when administered in liposomal form. Pharmacokinetic parameters of the drug such as AUC0-t (trapezoidal), clearance and t1/2 (elimination half-life) changed significantly (p |
| doi_str_mv | 10.1016/S0031-6865(00)00023-6 |
| format | Article |
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A comparative biodistribution study was performed between the conventional liposomes (PC:CH:PE — 1:0.5:0.16) and long-circulating liposomes (PC:CH:PE-PEG — 1:0.5:0.16) in arthritic rats. Pharmocokinetics of the drug changed significantly when administered in liposomal form. Pharmacokinetic parameters of the drug such as AUC0-t (trapezoidal), clearance and t1/2 (elimination half-life) changed significantly (p<0.05) when encapsulated in liposomes. Significant difference in pharmacokinetics was observed in AUC0-t and clearance between the conventional liposomes and long-circulating liposomes. The increased AUC0-t and reduced clearance of the durg with long-circulating liposomes, increased the availability of the drug by reducing RES uptake, in turn localization in arthritic paw tissue was also increased. A concentration of 0.33 μg of indomethacin/g of the tissue was achieved with S-liposomes after 24 h whereas it was only 0.26 μg of drug/g of the tissue with conventional liposomes. From the study, in may be concluded that the targeting efficiency of the long-circulating liposomes was about four times more than the conventional liposomes.</description><identifier>ISSN: 0031-6865</identifier><identifier>DOI: 10.1016/S0031-6865(00)00023-6</identifier><identifier>PMID: 10812940</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics ; Arthritis ; Biodistribution ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Drug Carriers ; Drug targeting ; General pharmacology ; Indomethacin ; Indomethacin - administration & dosage ; Indomethacin - pharmacokinetics ; Liposomes ; Long-circulating liposomes ; Male ; Medical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacokinetics ; Pharmacology. Drug treatments ; Phosphatidylcholines ; Phosphatidylethanolamines ; Rats ; Rats, Wistar ; Tissue Distribution</subject><ispartof>Pharmaceutica acta Helvetiae, 2000-04, Vol.74 (4), p.399-404</ispartof><rights>2000 Elsevier Science B.V.</rights><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c305t-3d42064c2e8d12fb361d10d3777fa98fb495e04de8c2ed01ec228bc4597ed8d73</citedby><cites>FETCH-LOGICAL-c305t-3d42064c2e8d12fb361d10d3777fa98fb495e04de8c2ed01ec228bc4597ed8d73</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=1347020$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10812940$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Srinath, P.</creatorcontrib><creatorcontrib>Chary, M.G.</creatorcontrib><creatorcontrib>Vyas, S.P.</creatorcontrib><creatorcontrib>Diwan, P.V.</creatorcontrib><title>Long-circulating liposomes of indomethacin in arthritic rats — a biodisposition study</title><title>Pharmaceutica acta Helvetiae</title><addtitle>Pharm Acta Helv</addtitle><description>To improve the targeting efficiency of liposomes of indomethacin to the arthritic joints, circulation half-life of the liposomes was increased by grafting amphipathic polyethylene glycol-2000 to the bilayer surface. A comparative biodistribution study was performed between the conventional liposomes (PC:CH:PE — 1:0.5:0.16) and long-circulating liposomes (PC:CH:PE-PEG — 1:0.5:0.16) in arthritic rats. Pharmocokinetics of the drug changed significantly when administered in liposomal form. Pharmacokinetic parameters of the drug such as AUC0-t (trapezoidal), clearance and t1/2 (elimination half-life) changed significantly (p<0.05) when encapsulated in liposomes. Significant difference in pharmacokinetics was observed in AUC0-t and clearance between the conventional liposomes and long-circulating liposomes. The increased AUC0-t and reduced clearance of the durg with long-circulating liposomes, increased the availability of the drug by reducing RES uptake, in turn localization in arthritic paw tissue was also increased. A concentration of 0.33 μg of indomethacin/g of the tissue was achieved with S-liposomes after 24 h whereas it was only 0.26 μg of drug/g of the tissue with conventional liposomes. From the study, in may be concluded that the targeting efficiency of the long-circulating liposomes was about four times more than the conventional liposomes.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</subject><subject>Arthritis</subject><subject>Biodistribution</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Drug Carriers</subject><subject>Drug targeting</subject><subject>General pharmacology</subject><subject>Indomethacin</subject><subject>Indomethacin - administration & dosage</subject><subject>Indomethacin - pharmacokinetics</subject><subject>Liposomes</subject><subject>Long-circulating liposomes</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Phosphatidylcholines</subject><subject>Phosphatidylethanolamines</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Tissue Distribution</subject><issn>0031-6865</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkDtOAzEQhl2ACK8jgFwgBMXCeL3PCqGIlxSJAhCl5bVnwWizDrYXKR2H4IScBIdEQEdle-b7Z6yPkD0GJwxYcXoHwFlSVEV-BHAMAClPijWy-VMekS3vX2KD15xvkBGDiqV1BpvkcWL7p0QZp4ZOBtM_0c7MrLdT9NS21PQ6XsOzVKaPDypdeHYmGEWdDJ5-vn9QSRtjtfExFRu2pz4Mer5D1lvZedxdndvk4fLifnydTG6vbsbnk0RxyEPCdZZCkakUK83StuEF0ww0L8uylXXVNlmdI2Qaq4hoYKjStGpUltcl6kqXfJscLufOnH0d0AcxNV5h18ke7eBFyVgWF1QRzJegctZ7h62YOTOVbi4YiIVF8W1RLHQJAPFtURQxt79aMDRT1H9SS4UROFgB0ivZtU72yvhfjmclpAvsbIlhtPFm0AmvDPYKtXGogtDW_POTL80Okf8</recordid><startdate>200004</startdate><enddate>200004</enddate><creator>Srinath, P.</creator><creator>Chary, M.G.</creator><creator>Vyas, S.P.</creator><creator>Diwan, P.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>200004</creationdate><title>Long-circulating liposomes of indomethacin in arthritic rats — a biodisposition study</title><author>Srinath, P. ; Chary, M.G. ; Vyas, S.P. ; Diwan, P.V.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c305t-3d42064c2e8d12fb361d10d3777fa98fb495e04de8c2ed01ec228bc4597ed8d73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</topic><topic>Arthritis</topic><topic>Biodistribution</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Drug Carriers</topic><topic>Drug targeting</topic><topic>General pharmacology</topic><topic>Indomethacin</topic><topic>Indomethacin - administration & dosage</topic><topic>Indomethacin - pharmacokinetics</topic><topic>Liposomes</topic><topic>Long-circulating liposomes</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Phosphatidylcholines</topic><topic>Phosphatidylethanolamines</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Srinath, P.</creatorcontrib><creatorcontrib>Chary, M.G.</creatorcontrib><creatorcontrib>Vyas, S.P.</creatorcontrib><creatorcontrib>Diwan, P.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>Pharmaceutica acta Helvetiae</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Srinath, P.</au><au>Chary, M.G.</au><au>Vyas, S.P.</au><au>Diwan, P.V.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Long-circulating liposomes of indomethacin in arthritic rats — a biodisposition study</atitle><jtitle>Pharmaceutica acta Helvetiae</jtitle><addtitle>Pharm Acta Helv</addtitle><date>2000-04</date><risdate>2000</risdate><volume>74</volume><issue>4</issue><spage>399</spage><epage>404</epage><pages>399-404</pages><issn>0031-6865</issn><abstract>To improve the targeting efficiency of liposomes of indomethacin to the arthritic joints, circulation half-life of the liposomes was increased by grafting amphipathic polyethylene glycol-2000 to the bilayer surface. A comparative biodistribution study was performed between the conventional liposomes (PC:CH:PE — 1:0.5:0.16) and long-circulating liposomes (PC:CH:PE-PEG — 1:0.5:0.16) in arthritic rats. Pharmocokinetics of the drug changed significantly when administered in liposomal form. Pharmacokinetic parameters of the drug such as AUC0-t (trapezoidal), clearance and t1/2 (elimination half-life) changed significantly (p<0.05) when encapsulated in liposomes. Significant difference in pharmacokinetics was observed in AUC0-t and clearance between the conventional liposomes and long-circulating liposomes. The increased AUC0-t and reduced clearance of the durg with long-circulating liposomes, increased the availability of the drug by reducing RES uptake, in turn localization in arthritic paw tissue was also increased. A concentration of 0.33 μg of indomethacin/g of the tissue was achieved with S-liposomes after 24 h whereas it was only 0.26 μg of drug/g of the tissue with conventional liposomes. From the study, in may be concluded that the targeting efficiency of the long-circulating liposomes was about four times more than the conventional liposomes.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10812940</pmid><doi>10.1016/S0031-6865(00)00023-6</doi><tpages>6</tpages></addata></record> |
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| subjects | Animals Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Arthritis Biodistribution Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Drug Carriers Drug targeting General pharmacology Indomethacin Indomethacin - administration & dosage Indomethacin - pharmacokinetics Liposomes Long-circulating liposomes Male Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacokinetics Pharmacology. Drug treatments Phosphatidylcholines Phosphatidylethanolamines Rats Rats, Wistar Tissue Distribution |
| title | Long-circulating liposomes of indomethacin in arthritic rats — a biodisposition study |
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