Antitumor Activity and Pharmacokinetics of Liposomes Containing Lipophilic Gemcitabine Prodrugs
Background: Gemcitabine is a deoxycytidine analogue that exhibits antitumoral activity against adenocarcinomas of the colon, lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2â²-deoxy-2â²,2â²-difluorouridine by cytidine deaminase. Materia...
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| Veröffentlicht in: | Anticancer research 2007-01, Vol.27 (1A), p.195-199 |
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| creator | BRUSA, Paola IMMORDINO, Maria Laura ROCCO, Flavio CATTEL, Luigi |
| description | Background: Gemcitabine is a deoxycytidine analogue that exhibits antitumoral activity against adenocarcinomas of the colon,
lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2â²-deoxy-2â²,2â²-difluorouridine
by cytidine deaminase. Materials and Methods: To improve the pharmacokinetic behavior and the antitumor activity of the drug,
the gemcitabine prodrug, 4-(N)-stearoylgemcitabine (C18gem) was incorporated in liposomes and both the pharmacokinetic and
the in vivo activity of this formulation intravenously or peritumorally administered in nude female CR1:Nu/Nu(CD-1)BR mice
grafted with HT-29 and KB 396p cells were studied. Results: The C18gem-liposomes showed both higher plasma half life and tumor
regression than control and gemcitabine. Conclusion: The incorporation of C18gem-prodrug in liposomes increased the plasma
half life of the drug resulting in increased accumulation in the tumor cells and a higher level of antitumoral efficacy. The
results obtained with different tumors sensitive to gemcitabine support the efficacy of this proposed drug delivery system. |
| format | Article |
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lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2â²-deoxy-2â²,2â²-difluorouridine
by cytidine deaminase. Materials and Methods: To improve the pharmacokinetic behavior and the antitumor activity of the drug,
the gemcitabine prodrug, 4-(N)-stearoylgemcitabine (C18gem) was incorporated in liposomes and both the pharmacokinetic and
the in vivo activity of this formulation intravenously or peritumorally administered in nude female CR1:Nu/Nu(CD-1)BR mice
grafted with HT-29 and KB 396p cells were studied. Results: The C18gem-liposomes showed both higher plasma half life and tumor
regression than control and gemcitabine. Conclusion: The incorporation of C18gem-prodrug in liposomes increased the plasma
half life of the drug resulting in increased accumulation in the tumor cells and a higher level of antitumoral efficacy. The
results obtained with different tumors sensitive to gemcitabine support the efficacy of this proposed drug delivery system.</description><identifier>ISSN: 0250-7005</identifier><identifier>EISSN: 1791-7530</identifier><identifier>PMID: 17352232</identifier><language>eng</language><publisher>Attiki: International Institute of Anticancer Research</publisher><subject>Animals ; Antimetabolites, Antineoplastic - administration & dosage ; Antimetabolites, Antineoplastic - pharmacokinetics ; Biological and medical sciences ; Colonic Neoplasms - drug therapy ; Colonic Neoplasms - metabolism ; Deoxycytidine - administration & dosage ; Deoxycytidine - analogs & derivatives ; Deoxycytidine - pharmacokinetics ; Female ; HT29 Cells ; Humans ; Liposomes ; Medical sciences ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Nasopharyngeal Neoplasms - drug therapy ; Nasopharyngeal Neoplasms - metabolism ; Prodrugs - administration & dosage ; Prodrugs - pharmacokinetics ; Stearates - administration & dosage ; Stearates - pharmacokinetics ; Tumors ; Xenograft Model Antitumor Assays</subject><ispartof>Anticancer research, 2007-01, Vol.27 (1A), p.195-199</ispartof><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18562371$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17352232$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>BRUSA, Paola</creatorcontrib><creatorcontrib>IMMORDINO, Maria Laura</creatorcontrib><creatorcontrib>ROCCO, Flavio</creatorcontrib><creatorcontrib>CATTEL, Luigi</creatorcontrib><title>Antitumor Activity and Pharmacokinetics of Liposomes Containing Lipophilic Gemcitabine Prodrugs</title><title>Anticancer research</title><addtitle>Anticancer Res</addtitle><description>Background: Gemcitabine is a deoxycytidine analogue that exhibits antitumoral activity against adenocarcinomas of the colon,
lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2â²-deoxy-2â²,2â²-difluorouridine
by cytidine deaminase. Materials and Methods: To improve the pharmacokinetic behavior and the antitumor activity of the drug,
the gemcitabine prodrug, 4-(N)-stearoylgemcitabine (C18gem) was incorporated in liposomes and both the pharmacokinetic and
the in vivo activity of this formulation intravenously or peritumorally administered in nude female CR1:Nu/Nu(CD-1)BR mice
grafted with HT-29 and KB 396p cells were studied. Results: The C18gem-liposomes showed both higher plasma half life and tumor
regression than control and gemcitabine. Conclusion: The incorporation of C18gem-prodrug in liposomes increased the plasma
half life of the drug resulting in increased accumulation in the tumor cells and a higher level of antitumoral efficacy. The
results obtained with different tumors sensitive to gemcitabine support the efficacy of this proposed drug delivery system.</description><subject>Animals</subject><subject>Antimetabolites, Antineoplastic - administration & dosage</subject><subject>Antimetabolites, Antineoplastic - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Colonic Neoplasms - drug therapy</subject><subject>Colonic Neoplasms - metabolism</subject><subject>Deoxycytidine - administration & dosage</subject><subject>Deoxycytidine - analogs & derivatives</subject><subject>Deoxycytidine - pharmacokinetics</subject><subject>Female</subject><subject>HT29 Cells</subject><subject>Humans</subject><subject>Liposomes</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>Mice, Nude</subject><subject>Nasopharyngeal Neoplasms - drug therapy</subject><subject>Nasopharyngeal Neoplasms - metabolism</subject><subject>Prodrugs - administration & dosage</subject><subject>Prodrugs - pharmacokinetics</subject><subject>Stearates - administration & dosage</subject><subject>Stearates - pharmacokinetics</subject><subject>Tumors</subject><subject>Xenograft Model Antitumor Assays</subject><issn>0250-7005</issn><issn>1791-7530</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpF0E1PwzAMBuAIgdgY_AWUC9wq5WNp2mM18SVNYofdIzdN10DTjCQF7d9TYGgnS9bj15bP0JzKkmZScHKO5oQJkklCxAxdxfhGSJ6XBb9EMyq5YIyzOVLVkGwanQ-40sl-2nTAMDR400FwoP27HUyyOmLf4rXd--idiXjlhwR2sMPut7nvbG81fjJO2wT1NII3wTdh3MVrdNFCH83NsS7Q9vFhu3rO1q9PL6tqnXWckJS1ZU5LRkU9Xb-sG87yQjJSt5wVTLQmZ4SWy7oGbrhhdCkLzpiWuZZQQmskX6D7v9h98B-jiUk5G7XpexiMH6OipSiEEHyCt0c41s40ah-sg3BQ_x-ZwN0RQNTQtwEGbePJFSJnXNKT6-yu-7LBqOig76dYriAwqWj1s5V_A6vfd9o</recordid><startdate>20070101</startdate><enddate>20070101</enddate><creator>BRUSA, Paola</creator><creator>IMMORDINO, Maria Laura</creator><creator>ROCCO, Flavio</creator><creator>CATTEL, Luigi</creator><general>International Institute of Anticancer Research</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20070101</creationdate><title>Antitumor Activity and Pharmacokinetics of Liposomes Containing Lipophilic Gemcitabine Prodrugs</title><author>BRUSA, Paola ; IMMORDINO, Maria Laura ; ROCCO, Flavio ; CATTEL, Luigi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-h300t-f9619215b7914bd3268720bf32825fe620194bba3e3e21478322c76c7a9afe73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Animals</topic><topic>Antimetabolites, Antineoplastic - administration & dosage</topic><topic>Antimetabolites, Antineoplastic - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Colonic Neoplasms - drug therapy</topic><topic>Colonic Neoplasms - metabolism</topic><topic>Deoxycytidine - administration & dosage</topic><topic>Deoxycytidine - analogs & derivatives</topic><topic>Deoxycytidine - pharmacokinetics</topic><topic>Female</topic><topic>HT29 Cells</topic><topic>Humans</topic><topic>Liposomes</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred BALB C</topic><topic>Mice, Nude</topic><topic>Nasopharyngeal Neoplasms - drug therapy</topic><topic>Nasopharyngeal Neoplasms - metabolism</topic><topic>Prodrugs - administration & dosage</topic><topic>Prodrugs - pharmacokinetics</topic><topic>Stearates - administration & dosage</topic><topic>Stearates - pharmacokinetics</topic><topic>Tumors</topic><topic>Xenograft Model Antitumor Assays</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>BRUSA, Paola</creatorcontrib><creatorcontrib>IMMORDINO, Maria Laura</creatorcontrib><creatorcontrib>ROCCO, Flavio</creatorcontrib><creatorcontrib>CATTEL, Luigi</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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Anticancer research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>BRUSA, Paola</au><au>IMMORDINO, Maria Laura</au><au>ROCCO, Flavio</au><au>CATTEL, Luigi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antitumor Activity and Pharmacokinetics of Liposomes Containing Lipophilic Gemcitabine Prodrugs</atitle><jtitle>Anticancer research</jtitle><addtitle>Anticancer Res</addtitle><date>2007-01-01</date><risdate>2007</risdate><volume>27</volume><issue>1A</issue><spage>195</spage><epage>199</epage><pages>195-199</pages><issn>0250-7005</issn><eissn>1791-7530</eissn><abstract>Background: Gemcitabine is a deoxycytidine analogue that exhibits antitumoral activity against adenocarcinomas of the colon,
lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2â²-deoxy-2â²,2â²-difluorouridine
by cytidine deaminase. Materials and Methods: To improve the pharmacokinetic behavior and the antitumor activity of the drug,
the gemcitabine prodrug, 4-(N)-stearoylgemcitabine (C18gem) was incorporated in liposomes and both the pharmacokinetic and
the in vivo activity of this formulation intravenously or peritumorally administered in nude female CR1:Nu/Nu(CD-1)BR mice
grafted with HT-29 and KB 396p cells were studied. Results: The C18gem-liposomes showed both higher plasma half life and tumor
regression than control and gemcitabine. Conclusion: The incorporation of C18gem-prodrug in liposomes increased the plasma
half life of the drug resulting in increased accumulation in the tumor cells and a higher level of antitumoral efficacy. The
results obtained with different tumors sensitive to gemcitabine support the efficacy of this proposed drug delivery system.</abstract><cop>Attiki</cop><pub>International Institute of Anticancer Research</pub><pmid>17352232</pmid><tpages>5</tpages></addata></record> |
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| subjects | Animals Antimetabolites, Antineoplastic - administration & dosage Antimetabolites, Antineoplastic - pharmacokinetics Biological and medical sciences Colonic Neoplasms - drug therapy Colonic Neoplasms - metabolism Deoxycytidine - administration & dosage Deoxycytidine - analogs & derivatives Deoxycytidine - pharmacokinetics Female HT29 Cells Humans Liposomes Medical sciences Mice Mice, Inbred BALB C Mice, Nude Nasopharyngeal Neoplasms - drug therapy Nasopharyngeal Neoplasms - metabolism Prodrugs - administration & dosage Prodrugs - pharmacokinetics Stearates - administration & dosage Stearates - pharmacokinetics Tumors Xenograft Model Antitumor Assays |
| title | Antitumor Activity and Pharmacokinetics of Liposomes Containing Lipophilic Gemcitabine Prodrugs |
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