Polymeric micelle for tumor pH and folate-mediated targeting
Novel pH-sensitive polymeric mixed micelles composed of poly( l-histidine) (polyHis; M w 5000)/PEG ( M n 2000) and poly( l-lactic acid) (PLLA) ( M n 3000)/PEG ( M n 2000) block copolymers with or without folate conjugation were prepared by diafiltration. The micelles were investigated for pH-depende...
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| Veröffentlicht in: | Journal of controlled release 2003-08, Vol.91 (1), p.103-113 |
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| creator | Lee, Eun Seong Na, Kun Bae, You Han |
| description | Novel pH-sensitive polymeric mixed micelles composed of poly(
l-histidine) (polyHis;
M
w 5000)/PEG (
M
n 2000) and poly(
l-lactic acid) (PLLA) (
M
n 3000)/PEG (
M
n 2000) block copolymers with or without folate conjugation were prepared by diafiltration. The micelles were investigated for pH-dependent drug release, folate receptor-mediated internalization and cytotoxicity using MCF-7 cells in vitro. The polyHis/PEG micelles showed accelerated adriamycin release as the pH decreased from 8.0. When the cumulative release for 24 h was plotted as a function of pH, the gradual transition in release rate appeared in a pH range from 8.0 to 6.8. In order to tailor the triggering pH of the polymeric micelles to the more acidic extracellular pH of tumors, while improving the micelle stability at pH 7.4, the PLLA/PEG block copolymer was blended with polyHis/PEG to form mixed micelles. Blending shifted the triggering pH to a lower value. Depending on the amount of PLLA/PEG, the mixed micelles were destabilized in the pH range of 7.2–6.6 (triggering pH for adriamycin release). When the mixed micelles were conjugated with folic acid, the in vitro results demonstrated that the micelles were more effective in tumor cell kill due to accelerated drug release and folate receptor-mediated tumor uptake. In addition, after internalization polyHis was found to be effective for cytosolic ADR delivery by virtue of fusogenic activity. This approach is expected to be useful for treatment of solid tumors in vivo. |
| doi_str_mv | 10.1016/S0168-3659(03)00239-6 |
| format | Article |
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l-histidine) (polyHis;
M
w 5000)/PEG (
M
n 2000) and poly(
l-lactic acid) (PLLA) (
M
n 3000)/PEG (
M
n 2000) block copolymers with or without folate conjugation were prepared by diafiltration. The micelles were investigated for pH-dependent drug release, folate receptor-mediated internalization and cytotoxicity using MCF-7 cells in vitro. The polyHis/PEG micelles showed accelerated adriamycin release as the pH decreased from 8.0. When the cumulative release for 24 h was plotted as a function of pH, the gradual transition in release rate appeared in a pH range from 8.0 to 6.8. In order to tailor the triggering pH of the polymeric micelles to the more acidic extracellular pH of tumors, while improving the micelle stability at pH 7.4, the PLLA/PEG block copolymer was blended with polyHis/PEG to form mixed micelles. Blending shifted the triggering pH to a lower value. Depending on the amount of PLLA/PEG, the mixed micelles were destabilized in the pH range of 7.2–6.6 (triggering pH for adriamycin release). When the mixed micelles were conjugated with folic acid, the in vitro results demonstrated that the micelles were more effective in tumor cell kill due to accelerated drug release and folate receptor-mediated tumor uptake. In addition, after internalization polyHis was found to be effective for cytosolic ADR delivery by virtue of fusogenic activity. This approach is expected to be useful for treatment of solid tumors in vivo.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/S0168-3659(03)00239-6</identifier><identifier>PMID: 12932642</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>adriamycin ; Antibiotics, Antineoplastic - administration & dosage ; Antibiotics, Antineoplastic - chemistry ; Biological and medical sciences ; Carrier Proteins - chemistry ; Chemical Phenomena ; Chemistry, Physical ; Doxorubicin - administration & dosage ; Doxorubicin - chemistry ; Drug Delivery Systems ; Endocytosis - drug effects ; Female ; Folate ; Folate Receptors, GPI-Anchored ; Folic Acid - chemistry ; General pharmacology ; Histidine - chemical synthesis ; Histidine - chemistry ; Humans ; Hydrogen-Ion Concentration ; Lactic Acid - chemical synthesis ; Lactic Acid - chemistry ; Light ; Medical sciences ; Micelles ; Microscopy, Confocal ; Mixed polymeric micelle ; Neoplasms - drug therapy ; Neoplasms - metabolism ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Poly( l-histidine)/PEG block copolymer ; poly(L-lactic acid) ; Polyglycolic Acid - chemical synthesis ; Polyglycolic Acid - chemistry ; Polymers - chemical synthesis ; Polymers - chemistry ; Receptor-mediated endocytosis ; Receptors, Cell Surface ; Scattering, Radiation ; Tumor Cells, Cultured ; Tumor extracellular pH</subject><ispartof>Journal of controlled release, 2003-08, Vol.91 (1), p.103-113</ispartof><rights>2003 Elsevier B.V.</rights><rights>2004 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c540t-33a95e969df0fc703c9d9ab34c1491042451636379d438c7cfc966a7e784105e3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0168-3659(03)00239-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>309,310,314,780,784,789,790,3550,23930,23931,25140,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=15177715$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12932642$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lee, Eun Seong</creatorcontrib><creatorcontrib>Na, Kun</creatorcontrib><creatorcontrib>Bae, You Han</creatorcontrib><title>Polymeric micelle for tumor pH and folate-mediated targeting</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>Novel pH-sensitive polymeric mixed micelles composed of poly(
l-histidine) (polyHis;
M
w 5000)/PEG (
M
n 2000) and poly(
l-lactic acid) (PLLA) (
M
n 3000)/PEG (
M
n 2000) block copolymers with or without folate conjugation were prepared by diafiltration. The micelles were investigated for pH-dependent drug release, folate receptor-mediated internalization and cytotoxicity using MCF-7 cells in vitro. The polyHis/PEG micelles showed accelerated adriamycin release as the pH decreased from 8.0. When the cumulative release for 24 h was plotted as a function of pH, the gradual transition in release rate appeared in a pH range from 8.0 to 6.8. In order to tailor the triggering pH of the polymeric micelles to the more acidic extracellular pH of tumors, while improving the micelle stability at pH 7.4, the PLLA/PEG block copolymer was blended with polyHis/PEG to form mixed micelles. Blending shifted the triggering pH to a lower value. Depending on the amount of PLLA/PEG, the mixed micelles were destabilized in the pH range of 7.2–6.6 (triggering pH for adriamycin release). When the mixed micelles were conjugated with folic acid, the in vitro results demonstrated that the micelles were more effective in tumor cell kill due to accelerated drug release and folate receptor-mediated tumor uptake. In addition, after internalization polyHis was found to be effective for cytosolic ADR delivery by virtue of fusogenic activity. This approach is expected to be useful for treatment of solid tumors in vivo.</description><subject>adriamycin</subject><subject>Antibiotics, Antineoplastic - administration & dosage</subject><subject>Antibiotics, Antineoplastic - chemistry</subject><subject>Biological and medical sciences</subject><subject>Carrier Proteins - chemistry</subject><subject>Chemical Phenomena</subject><subject>Chemistry, Physical</subject><subject>Doxorubicin - administration & dosage</subject><subject>Doxorubicin - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Endocytosis - drug effects</subject><subject>Female</subject><subject>Folate</subject><subject>Folate Receptors, GPI-Anchored</subject><subject>Folic Acid - chemistry</subject><subject>General pharmacology</subject><subject>Histidine - chemical synthesis</subject><subject>Histidine - chemistry</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>Lactic Acid - chemical synthesis</subject><subject>Lactic Acid - chemistry</subject><subject>Light</subject><subject>Medical sciences</subject><subject>Micelles</subject><subject>Microscopy, Confocal</subject><subject>Mixed polymeric micelle</subject><subject>Neoplasms - drug therapy</subject><subject>Neoplasms - metabolism</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Poly( l-histidine)/PEG block copolymer</subject><subject>poly(L-lactic acid)</subject><subject>Polyglycolic Acid - chemical synthesis</subject><subject>Polyglycolic Acid - chemistry</subject><subject>Polymers - chemical synthesis</subject><subject>Polymers - chemistry</subject><subject>Receptor-mediated endocytosis</subject><subject>Receptors, Cell Surface</subject><subject>Scattering, Radiation</subject><subject>Tumor Cells, Cultured</subject><subject>Tumor extracellular pH</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMlKBDEQhoMozrg8gtIXRQ-tSVeWDggigxsICuo5xHT1EOllTLoF396MM-jRSxWEryp_fYQcMHrGKJPnz6mUOUihTyicUlqAzuUGmbJSQc61Fptk-otMyE6M75RSAVxtkwkrNBSSF1Ny8dQ3Xy0G77LWO2wazOo-ZMPYprq4y2xXpYfGDpi3WPnUq2ywYY6D7-Z7ZKu2TcT9dd8lrzfXL7O7_OHx9n529ZA7wemQA1gtUEtd1bR2ioLTlbZvwB3jmlFecMEkSFC64lA65WqnpbQKVckZFQi75Hi1dxH6jxHjYFofl2Fth_0YjQKZLi3hX5CVWnBZigSKFehCH2PA2iyCb234MoyapV_z49cs5RkK5sevkWnucP3B-JZ8_E2thSbgaA3Y6GxTB9s5H_84wZRSbBngcsVh8vbpMZjoPHYuOQ7oBlP1_p8o3-valS0</recordid><startdate>20030828</startdate><enddate>20030828</enddate><creator>Lee, Eun Seong</creator><creator>Na, Kun</creator><creator>Bae, You Han</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20030828</creationdate><title>Polymeric micelle for tumor pH and folate-mediated targeting</title><author>Lee, Eun Seong ; Na, Kun ; Bae, You Han</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c540t-33a95e969df0fc703c9d9ab34c1491042451636379d438c7cfc966a7e784105e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>adriamycin</topic><topic>Antibiotics, Antineoplastic - administration & dosage</topic><topic>Antibiotics, Antineoplastic - chemistry</topic><topic>Biological and medical sciences</topic><topic>Carrier Proteins - chemistry</topic><topic>Chemical Phenomena</topic><topic>Chemistry, Physical</topic><topic>Doxorubicin - administration & dosage</topic><topic>Doxorubicin - chemistry</topic><topic>Drug Delivery Systems</topic><topic>Endocytosis - drug effects</topic><topic>Female</topic><topic>Folate</topic><topic>Folate Receptors, GPI-Anchored</topic><topic>Folic Acid - chemistry</topic><topic>General pharmacology</topic><topic>Histidine - chemical synthesis</topic><topic>Histidine - chemistry</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>Lactic Acid - chemical synthesis</topic><topic>Lactic Acid - chemistry</topic><topic>Light</topic><topic>Medical sciences</topic><topic>Micelles</topic><topic>Microscopy, Confocal</topic><topic>Mixed polymeric micelle</topic><topic>Neoplasms - drug therapy</topic><topic>Neoplasms - metabolism</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Poly( l-histidine)/PEG block copolymer</topic><topic>poly(L-lactic acid)</topic><topic>Polyglycolic Acid - chemical synthesis</topic><topic>Polyglycolic Acid - chemistry</topic><topic>Polymers - chemical synthesis</topic><topic>Polymers - chemistry</topic><topic>Receptor-mediated endocytosis</topic><topic>Receptors, Cell Surface</topic><topic>Scattering, Radiation</topic><topic>Tumor Cells, Cultured</topic><topic>Tumor extracellular pH</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lee, Eun Seong</creatorcontrib><creatorcontrib>Na, Kun</creatorcontrib><creatorcontrib>Bae, You Han</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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lee, Eun Seong</au><au>Na, Kun</au><au>Bae, You Han</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Polymeric micelle for tumor pH and folate-mediated targeting</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2003-08-28</date><risdate>2003</risdate><volume>91</volume><issue>1</issue><spage>103</spage><epage>113</epage><pages>103-113</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>Novel pH-sensitive polymeric mixed micelles composed of poly(
l-histidine) (polyHis;
M
w 5000)/PEG (
M
n 2000) and poly(
l-lactic acid) (PLLA) (
M
n 3000)/PEG (
M
n 2000) block copolymers with or without folate conjugation were prepared by diafiltration. The micelles were investigated for pH-dependent drug release, folate receptor-mediated internalization and cytotoxicity using MCF-7 cells in vitro. The polyHis/PEG micelles showed accelerated adriamycin release as the pH decreased from 8.0. When the cumulative release for 24 h was plotted as a function of pH, the gradual transition in release rate appeared in a pH range from 8.0 to 6.8. In order to tailor the triggering pH of the polymeric micelles to the more acidic extracellular pH of tumors, while improving the micelle stability at pH 7.4, the PLLA/PEG block copolymer was blended with polyHis/PEG to form mixed micelles. Blending shifted the triggering pH to a lower value. Depending on the amount of PLLA/PEG, the mixed micelles were destabilized in the pH range of 7.2–6.6 (triggering pH for adriamycin release). When the mixed micelles were conjugated with folic acid, the in vitro results demonstrated that the micelles were more effective in tumor cell kill due to accelerated drug release and folate receptor-mediated tumor uptake. In addition, after internalization polyHis was found to be effective for cytosolic ADR delivery by virtue of fusogenic activity. This approach is expected to be useful for treatment of solid tumors in vivo.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>12932642</pmid><doi>10.1016/S0168-3659(03)00239-6</doi><tpages>11</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0168-3659 |
| ispartof | Journal of controlled release, 2003-08, Vol.91 (1), p.103-113 |
| issn | 0168-3659 1873-4995 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | adriamycin Antibiotics, Antineoplastic - administration & dosage Antibiotics, Antineoplastic - chemistry Biological and medical sciences Carrier Proteins - chemistry Chemical Phenomena Chemistry, Physical Doxorubicin - administration & dosage Doxorubicin - chemistry Drug Delivery Systems Endocytosis - drug effects Female Folate Folate Receptors, GPI-Anchored Folic Acid - chemistry General pharmacology Histidine - chemical synthesis Histidine - chemistry Humans Hydrogen-Ion Concentration Lactic Acid - chemical synthesis Lactic Acid - chemistry Light Medical sciences Micelles Microscopy, Confocal Mixed polymeric micelle Neoplasms - drug therapy Neoplasms - metabolism Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Poly( l-histidine)/PEG block copolymer poly(L-lactic acid) Polyglycolic Acid - chemical synthesis Polyglycolic Acid - chemistry Polymers - chemical synthesis Polymers - chemistry Receptor-mediated endocytosis Receptors, Cell Surface Scattering, Radiation Tumor Cells, Cultured Tumor extracellular pH |
| title | Polymeric micelle for tumor pH and folate-mediated targeting |
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