O/W Lipid Emulsions for Parenteral Drug Delivery. I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II
The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct=226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compa...
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| Veröffentlicht in: | Biological & pharmaceutical bulletin 1994/11/15, Vol.17(11), pp.1490-1495 |
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| creator | SAKAEDA, Toshiyuki TAKAHASHI, Koji NISHIHARA, Yoshitaka HIRANO, Koichiro |
| description | The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct=226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 micellar and plasma solutions of sudan II, the blood concentration of sudan II was markedly elevated by administration as a lipid emulsion. However, the distribution of sudan II to the liver, lungs, spleen, and adipose tissue was not altered, and that to the brain, heart, kidneys, muscle, and tumor was slightly decreased. To understand these results, pharmacokinetic analysis was performed using a newly derived compartmental model, and moreover, the organ distribution clearance was analyzed. It was suggested that the oil particles deliver the incorporated drug selectively to the liver, lungs, and spleen, and the speed of delivery could be surpressed by using HCO-60. However, in the case of sudan II, its rapid release from the oil particles after i.v. injection prevented a drastic alteration in the distribution of sudan II. The simulation studies suggested that a considerable decrease in the release rate or an increase in partition coefficient (experimentally more than 108) would be required for delivery. |
| doi_str_mv | 10.1248/bpb.17.1490 |
| format | Article |
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I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II</title><source>J-STAGE Free</source><source>MEDLINE</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Free Full-Text Journals in Chemistry</source><creator>SAKAEDA, Toshiyuki ; TAKAHASHI, Koji ; NISHIHARA, Yoshitaka ; HIRANO, Koichiro</creator><creatorcontrib>SAKAEDA, Toshiyuki ; TAKAHASHI, Koji ; NISHIHARA, Yoshitaka ; HIRANO, Koichiro</creatorcontrib><description>The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct=226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 micellar and plasma solutions of sudan II, the blood concentration of sudan II was markedly elevated by administration as a lipid emulsion. However, the distribution of sudan II to the liver, lungs, spleen, and adipose tissue was not altered, and that to the brain, heart, kidneys, muscle, and tumor was slightly decreased. To understand these results, pharmacokinetic analysis was performed using a newly derived compartmental model, and moreover, the organ distribution clearance was analyzed. It was suggested that the oil particles deliver the incorporated drug selectively to the liver, lungs, and spleen, and the speed of delivery could be surpressed by using HCO-60. However, in the case of sudan II, its rapid release from the oil particles after i.v. injection prevented a drastic alteration in the distribution of sudan II. The simulation studies suggested that a considerable decrease in the release rate or an increase in partition coefficient (experimentally more than 108) would be required for delivery.</description><identifier>ISSN: 0918-6158</identifier><identifier>EISSN: 1347-5215</identifier><identifier>DOI: 10.1248/bpb.17.1490</identifier><identifier>PMID: 7703970</identifier><language>eng</language><publisher>Tokyo: The Pharmaceutical Society of Japan</publisher><subject>Adipose Tissue - metabolism ; Animals ; Azo Compounds - administration & dosage ; Azo Compounds - metabolism ; Azo Compounds - pharmacokinetics ; Biological and medical sciences ; Brain - metabolism ; Carcinosarcoma - metabolism ; drug delivery system ; Drug Delivery Systems ; Emulsions ; General pharmacology ; Injections, Intravenous ; Kidney - metabolism ; Liver - metabolism ; Lung - metabolism ; Male ; Medical sciences ; Models, Biological ; Muscles - metabolism ; Myocardium - metabolism ; O/W lipid emulsion ; partition coefficient ; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; release ; Sarcoma, Experimental - metabolism ; Soybean Oil - chemistry ; Soybean Oil - metabolism ; Soybean Oil - pharmacokinetics ; Spleen - metabolism ; Surface-Active Agents - chemistry ; Surface-Active Agents - metabolism ; Tissue Distribution</subject><ispartof>Biological and Pharmaceutical Bulletin, 1994/11/15, Vol.17(11), pp.1490-1495</ispartof><rights>The Pharmaceutical Society of Japan</rights><rights>1995 INIST-CNRS</rights><rights>Copyright Japan Science and Technology Agency 1994</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4790-99ce27cf65235b00be19baf9730fa48684921f3325c8b8e607ed7140a2df44723</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3628656$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7703970$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SAKAEDA, Toshiyuki</creatorcontrib><creatorcontrib>TAKAHASHI, Koji</creatorcontrib><creatorcontrib>NISHIHARA, Yoshitaka</creatorcontrib><creatorcontrib>HIRANO, Koichiro</creatorcontrib><title>O/W Lipid Emulsions for Parenteral Drug Delivery. I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II</title><title>Biological & pharmaceutical bulletin</title><addtitle>Biol Pharm Bull</addtitle><description>The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct=226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 micellar and plasma solutions of sudan II, the blood concentration of sudan II was markedly elevated by administration as a lipid emulsion. However, the distribution of sudan II to the liver, lungs, spleen, and adipose tissue was not altered, and that to the brain, heart, kidneys, muscle, and tumor was slightly decreased. To understand these results, pharmacokinetic analysis was performed using a newly derived compartmental model, and moreover, the organ distribution clearance was analyzed. It was suggested that the oil particles deliver the incorporated drug selectively to the liver, lungs, and spleen, and the speed of delivery could be surpressed by using HCO-60. However, in the case of sudan II, its rapid release from the oil particles after i.v. injection prevented a drastic alteration in the distribution of sudan II. The simulation studies suggested that a considerable decrease in the release rate or an increase in partition coefficient (experimentally more than 108) would be required for delivery.</description><subject>Adipose Tissue - metabolism</subject><subject>Animals</subject><subject>Azo Compounds - administration & dosage</subject><subject>Azo Compounds - metabolism</subject><subject>Azo Compounds - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Carcinosarcoma - metabolism</subject><subject>drug delivery system</subject><subject>Drug Delivery Systems</subject><subject>Emulsions</subject><subject>General pharmacology</subject><subject>Injections, Intravenous</subject><subject>Kidney - metabolism</subject><subject>Liver - metabolism</subject><subject>Lung - metabolism</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Models, Biological</subject><subject>Muscles - metabolism</subject><subject>Myocardium - metabolism</subject><subject>O/W lipid emulsion</subject><subject>partition coefficient</subject><subject>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>release</subject><subject>Sarcoma, Experimental - metabolism</subject><subject>Soybean Oil - chemistry</subject><subject>Soybean Oil - metabolism</subject><subject>Soybean Oil - pharmacokinetics</subject><subject>Spleen - metabolism</subject><subject>Surface-Active Agents - chemistry</subject><subject>Surface-Active Agents - metabolism</subject><subject>Tissue Distribution</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkd2L1DAUxYMo6zj65LMQUHyRdvPVJnmU_dDCwCyo-FjSNNnN2CbdpBX2vzfj1HnwJRdyfveeyz0AvMWoxISJy27qSsxLzCR6BjaYMl5UBFfPwQZJLIoaV-IleJXSASHEEaEX4IJzRCVHGzDvL3_CnZtcD2_GZUgu-ARtiPBOReNnE9UAr-NyD6_N4H6b-FTCpoR3DyqOSodfzpvZ6QSDhfODgXs3HBvz12ASVL6HjdchTiGq2fTw29IrD5vmNXhh1ZDMm7VuwY_bm-9XX4vd_ktz9XlXaMYlKqTUhnBt64rQqkOoM1h2ykpOkVVM1IJJgi2lpNKiE6ZG3PQcM6RIbxnjhG7Bx9PcKYbHxaS5HV3SZhiUN2FJLecCkUrSDL7_DzyEJfq8W4sZk7giIrtuwacTpWNIKRrbTtGNKj61GLXHJNqcRIt5e0wi0-_WmUs3mv7MrqfP-odVV0mrwUbltUtnjNZE1FWdsdsTdkizujdnfb3y0RJLSf_a4n9v9j8DOmfVGk__AJncpvs</recordid><startdate>1994</startdate><enddate>1994</enddate><creator>SAKAEDA, Toshiyuki</creator><creator>TAKAHASHI, Koji</creator><creator>NISHIHARA, Yoshitaka</creator><creator>HIRANO, Koichiro</creator><general>The Pharmaceutical Society of Japan</general><general>Maruzen</general><general>Japan Science and Technology Agency</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U9</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>1994</creationdate><title>O/W Lipid Emulsions for Parenteral Drug Delivery. I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II</title><author>SAKAEDA, Toshiyuki ; TAKAHASHI, Koji ; NISHIHARA, Yoshitaka ; HIRANO, Koichiro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4790-99ce27cf65235b00be19baf9730fa48684921f3325c8b8e607ed7140a2df44723</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>Adipose Tissue - metabolism</topic><topic>Animals</topic><topic>Azo Compounds - administration & dosage</topic><topic>Azo Compounds - metabolism</topic><topic>Azo Compounds - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Carcinosarcoma - metabolism</topic><topic>drug delivery system</topic><topic>Drug Delivery Systems</topic><topic>Emulsions</topic><topic>General pharmacology</topic><topic>Injections, Intravenous</topic><topic>Kidney - metabolism</topic><topic>Liver - metabolism</topic><topic>Lung - metabolism</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Models, Biological</topic><topic>Muscles - metabolism</topic><topic>Myocardium - metabolism</topic><topic>O/W lipid emulsion</topic><topic>partition coefficient</topic><topic>Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>release</topic><topic>Sarcoma, Experimental - metabolism</topic><topic>Soybean Oil - chemistry</topic><topic>Soybean Oil - metabolism</topic><topic>Soybean Oil - pharmacokinetics</topic><topic>Spleen - metabolism</topic><topic>Surface-Active Agents - chemistry</topic><topic>Surface-Active Agents - metabolism</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SAKAEDA, Toshiyuki</creatorcontrib><creatorcontrib>TAKAHASHI, Koji</creatorcontrib><creatorcontrib>NISHIHARA, Yoshitaka</creatorcontrib><creatorcontrib>HIRANO, Koichiro</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>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Biological & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SAKAEDA, Toshiyuki</au><au>TAKAHASHI, Koji</au><au>NISHIHARA, Yoshitaka</au><au>HIRANO, Koichiro</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>O/W Lipid Emulsions for Parenteral Drug Delivery. I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II</atitle><jtitle>Biological & pharmaceutical bulletin</jtitle><addtitle>Biol Pharm Bull</addtitle><date>1994</date><risdate>1994</risdate><volume>17</volume><issue>11</issue><spage>1490</spage><epage>1495</epage><pages>1490-1495</pages><issn>0918-6158</issn><eissn>1347-5215</eissn><abstract>The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct=226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 micellar and plasma solutions of sudan II, the blood concentration of sudan II was markedly elevated by administration as a lipid emulsion. However, the distribution of sudan II to the liver, lungs, spleen, and adipose tissue was not altered, and that to the brain, heart, kidneys, muscle, and tumor was slightly decreased. To understand these results, pharmacokinetic analysis was performed using a newly derived compartmental model, and moreover, the organ distribution clearance was analyzed. It was suggested that the oil particles deliver the incorporated drug selectively to the liver, lungs, and spleen, and the speed of delivery could be surpressed by using HCO-60. However, in the case of sudan II, its rapid release from the oil particles after i.v. injection prevented a drastic alteration in the distribution of sudan II. The simulation studies suggested that a considerable decrease in the release rate or an increase in partition coefficient (experimentally more than 108) would be required for delivery.</abstract><cop>Tokyo</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>7703970</pmid><doi>10.1248/bpb.17.1490</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| source | J-STAGE Free; MEDLINE; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Adipose Tissue - metabolism Animals Azo Compounds - administration & dosage Azo Compounds - metabolism Azo Compounds - pharmacokinetics Biological and medical sciences Brain - metabolism Carcinosarcoma - metabolism drug delivery system Drug Delivery Systems Emulsions General pharmacology Injections, Intravenous Kidney - metabolism Liver - metabolism Lung - metabolism Male Medical sciences Models, Biological Muscles - metabolism Myocardium - metabolism O/W lipid emulsion partition coefficient Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions Pharmacology. Drug treatments Rats Rats, Wistar release Sarcoma, Experimental - metabolism Soybean Oil - chemistry Soybean Oil - metabolism Soybean Oil - pharmacokinetics Spleen - metabolism Surface-Active Agents - chemistry Surface-Active Agents - metabolism Tissue Distribution |
| title | O/W Lipid Emulsions for Parenteral Drug Delivery. I. Pharmacokinetics of the Oil Particles and Incorporated Sudan II |
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