Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines
Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 bo...
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Veröffentlicht in: | British journal of cancer 1995-04, Vol.71 (4), p.727-732 |
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description | Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards MS-2 fibrosarcoma. |
doi_str_mv | 10.1038/bjc.1995.142 |
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The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards MS-2 fibrosarcoma.</description><identifier>ISSN: 0007-0920</identifier><identifier>EISSN: 1532-1827</identifier><identifier>DOI: 10.1038/bjc.1995.142</identifier><identifier>PMID: 7710936</identifier><identifier>CODEN: BJCAAI</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>1,2-Dipalmitoylphosphatidylcholine ; Animals ; Biological and medical sciences ; Biomedical and Life Sciences ; Biomedicine ; Cancer Research ; Drug Carriers ; Drug Resistance ; Emulsions ; Epidemiology ; experimental-oncology ; Female ; Fibrosarcoma - drug therapy ; Fibrosarcoma - metabolism ; Indoles - chemical synthesis ; Indoles - pharmacokinetics ; Indoles - therapeutic use ; Injections, Intravenous ; Lipoproteins, LDL - blood ; Liposomes ; Liver - metabolism ; Medical sciences ; Mice ; Mice, Inbred BALB C ; Molecular Medicine ; Muscles - metabolism ; Oncology ; Organometallic Compounds - chemical synthesis ; Organometallic Compounds - pharmacokinetics ; Organometallic Compounds - therapeutic use ; Photochemotherapy ; Photoradiation therapy and photosensitizing agent ; Polyethylene Glycols ; Radiation-Sensitizing Agents - pharmacokinetics ; Radiation-Sensitizing Agents - therapeutic use ; Skin - metabolism ; Spleen - metabolism ; Structure-Activity Relationship ; Treatment with physical agents ; Treatment. General aspects ; Tumors</subject><ispartof>British journal of cancer, 1995-04, Vol.71 (4), p.727-732</ispartof><rights>Cancer Research Campaign 1995</rights><rights>1995 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3612-7f0e6f97924b06d6968f23f8743b39c2cbe2ee027d6689ddec82685ac118e7d33</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2033732/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2033732/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,881,27903,27904,41467,42536,51298,53770,53772</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3477470$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7710936$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Soncin, M</creatorcontrib><creatorcontrib>Polo, L</creatorcontrib><creatorcontrib>Reddi, E</creatorcontrib><creatorcontrib>Jori, G</creatorcontrib><creatorcontrib>Kenney, ME</creatorcontrib><creatorcontrib>Cheng, G</creatorcontrib><creatorcontrib>Rodgers, MAJ</creatorcontrib><title>Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines</title><title>British journal of cancer</title><addtitle>Br J Cancer</addtitle><addtitle>Br J Cancer</addtitle><description>Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards MS-2 fibrosarcoma.</description><subject>1,2-Dipalmitoylphosphatidylcholine</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Cancer Research</subject><subject>Drug Carriers</subject><subject>Drug Resistance</subject><subject>Emulsions</subject><subject>Epidemiology</subject><subject>experimental-oncology</subject><subject>Female</subject><subject>Fibrosarcoma - drug therapy</subject><subject>Fibrosarcoma - metabolism</subject><subject>Indoles - chemical synthesis</subject><subject>Indoles - pharmacokinetics</subject><subject>Indoles - therapeutic use</subject><subject>Injections, Intravenous</subject><subject>Lipoproteins, LDL - blood</subject><subject>Liposomes</subject><subject>Liver - metabolism</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>Molecular Medicine</subject><subject>Muscles - metabolism</subject><subject>Oncology</subject><subject>Organometallic Compounds - chemical synthesis</subject><subject>Organometallic Compounds - pharmacokinetics</subject><subject>Organometallic Compounds - therapeutic use</subject><subject>Photochemotherapy</subject><subject>Photoradiation therapy and photosensitizing agent</subject><subject>Polyethylene Glycols</subject><subject>Radiation-Sensitizing Agents - pharmacokinetics</subject><subject>Radiation-Sensitizing Agents - therapeutic use</subject><subject>Skin - metabolism</subject><subject>Spleen - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Treatment with physical agents</subject><subject>Treatment. General aspects</subject><subject>Tumors</subject><issn>0007-0920</issn><issn>1532-1827</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkc2KFDEUhYMoYzu6cyvUQkTBavNTnVQ2ggzjODDgRt2GVOqmO01VUiapYeoZfGnTdtMouAq558s54R6EXhK8Jpi1H7q9WRMpN2vS0EdoRTaM1qSl4jFaYYxFjSXFT9GzlPblKnErLtCFEARLxlfo17W1YHIVbKUfnB6qwW11dsFX2vdVD4O7h7hUaUkZxqqM8w6qPI9hjvUQjB5ccn77B66nXcghgU8uH6dTDBPE7CAd_G_g7e2Pd3UwWXdzDg9LeZB3urgs2jsP6Tl6YvWQ4MXpvETfP19_u_pS3329ub36dFcbxgmthcXArRSSNh3mPZe8tZTZVjSsY9JQ0wEFwFT0nLey78G0lLcbbQhpQfSMXaKPR99p7kboDfgc9aCm6EYdFxW0U_8q3u3UNtwrihkTjBaDNyeDGH7OkLIaXTIwDNpDmJMSghIi2SHp_RE0MaQUwZ5DCFaH8lQpTx3KU6W8gr_6-2Nn-NRW0V-fdJ3K6m3U3rh0xlgjRCNwweojloritxDVvtTly0r_H_sbeKi1Fw</recordid><startdate>19950401</startdate><enddate>19950401</enddate><creator>Soncin, M</creator><creator>Polo, L</creator><creator>Reddi, E</creator><creator>Jori, G</creator><creator>Kenney, ME</creator><creator>Cheng, G</creator><creator>Rodgers, MAJ</creator><general>Nature Publishing Group UK</general><general>Nature Publishing Group</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><scope>5PM</scope></search><sort><creationdate>19950401</creationdate><title>Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines</title><author>Soncin, M ; Polo, L ; Reddi, E ; Jori, G ; Kenney, ME ; Cheng, G ; Rodgers, MAJ</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3612-7f0e6f97924b06d6968f23f8743b39c2cbe2ee027d6689ddec82685ac118e7d33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>1,2-Dipalmitoylphosphatidylcholine</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Cancer Research</topic><topic>Drug Carriers</topic><topic>Drug Resistance</topic><topic>Emulsions</topic><topic>Epidemiology</topic><topic>experimental-oncology</topic><topic>Female</topic><topic>Fibrosarcoma - drug therapy</topic><topic>Fibrosarcoma - metabolism</topic><topic>Indoles - chemical synthesis</topic><topic>Indoles - pharmacokinetics</topic><topic>Indoles - therapeutic use</topic><topic>Injections, Intravenous</topic><topic>Lipoproteins, LDL - blood</topic><topic>Liposomes</topic><topic>Liver - metabolism</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred BALB C</topic><topic>Molecular Medicine</topic><topic>Muscles - metabolism</topic><topic>Oncology</topic><topic>Organometallic Compounds - chemical synthesis</topic><topic>Organometallic Compounds - pharmacokinetics</topic><topic>Organometallic Compounds - therapeutic use</topic><topic>Photochemotherapy</topic><topic>Photoradiation therapy and photosensitizing agent</topic><topic>Polyethylene Glycols</topic><topic>Radiation-Sensitizing Agents - pharmacokinetics</topic><topic>Radiation-Sensitizing Agents - therapeutic use</topic><topic>Skin - metabolism</topic><topic>Spleen - metabolism</topic><topic>Structure-Activity Relationship</topic><topic>Treatment with physical agents</topic><topic>Treatment. General aspects</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Soncin, M</creatorcontrib><creatorcontrib>Polo, L</creatorcontrib><creatorcontrib>Reddi, E</creatorcontrib><creatorcontrib>Jori, G</creatorcontrib><creatorcontrib>Kenney, ME</creatorcontrib><creatorcontrib>Cheng, G</creatorcontrib><creatorcontrib>Rodgers, MAJ</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><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of cancer</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Soncin, M</au><au>Polo, L</au><au>Reddi, E</au><au>Jori, G</au><au>Kenney, ME</au><au>Cheng, G</au><au>Rodgers, MAJ</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines</atitle><jtitle>British journal of cancer</jtitle><stitle>Br J Cancer</stitle><addtitle>Br J Cancer</addtitle><date>1995-04-01</date><risdate>1995</risdate><volume>71</volume><issue>4</issue><spage>727</spage><epage>732</epage><pages>727-732</pages><issn>0007-0920</issn><eissn>1532-1827</eissn><coden>BJCAAI</coden><abstract>Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.35 mumol kg-1 body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards MS-2 fibrosarcoma.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>7710936</pmid><doi>10.1038/bjc.1995.142</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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subjects | 1,2-Dipalmitoylphosphatidylcholine Animals Biological and medical sciences Biomedical and Life Sciences Biomedicine Cancer Research Drug Carriers Drug Resistance Emulsions Epidemiology experimental-oncology Female Fibrosarcoma - drug therapy Fibrosarcoma - metabolism Indoles - chemical synthesis Indoles - pharmacokinetics Indoles - therapeutic use Injections, Intravenous Lipoproteins, LDL - blood Liposomes Liver - metabolism Medical sciences Mice Mice, Inbred BALB C Molecular Medicine Muscles - metabolism Oncology Organometallic Compounds - chemical synthesis Organometallic Compounds - pharmacokinetics Organometallic Compounds - therapeutic use Photochemotherapy Photoradiation therapy and photosensitizing agent Polyethylene Glycols Radiation-Sensitizing Agents - pharmacokinetics Radiation-Sensitizing Agents - therapeutic use Skin - metabolism Spleen - metabolism Structure-Activity Relationship Treatment with physical agents Treatment. General aspects Tumors |
title | Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines |
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