Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis
A folate‐conjugated copolymer PEG‐PLA‐PLL/folate was synthesized and mixed with pure PEG‐PLA‐PLL and a fluorescent model drug mFITC to prepare folate‐conjugated micelles. The distribution of micelles was studied on cancer‐cell‐bearing mice via frozen slicing. The results show that mFITC is successfu...
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| Veröffentlicht in: | Macromolecular bioscience 2009-11, Vol.9 (11), p.1059-1068 |
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| creator | Lu, Tiancheng Sun, Jing Chen, Xuexi Zhang, Peibiao Jing, Xiabin |
| description | A folate‐conjugated copolymer PEG‐PLA‐PLL/folate was synthesized and mixed with pure PEG‐PLA‐PLL and a fluorescent model drug mFITC to prepare folate‐conjugated micelles. The distribution of micelles was studied on cancer‐cell‐bearing mice via frozen slicing. The results show that mFITC is successfully encapsulated into folate(+) and folate(−)micelles; PEG‐PLA‐PLL micelles the latter can be internalized by both HeLa and CHO cells without selectivity due to their cationic surface charges, while folate(+)micelles exhibit more preferential endocytosis by HeLa cells than by CHO cells. The folate(−)micelles showed retention in both organs and tumors. The folate(+)micelles are a promising active targeting drug delivery system for FR over‐expressing cells and they accumulate in tumor beds.
Folate‐conjugated micelles for the selective delivery of hydrophobic molecules are developed. They have potential to deliver drugs into folate‐receptor over‐expressing cancer cells HeLa via folate receptors mediated endocytosis in vitro and in vivo. These micelle systems can be used in the delivery of anticancer drugs and their selective target to cancer cells. |
| doi_str_mv | 10.1002/mabi.200900134 |
| format | Article |
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Folate‐conjugated micelles for the selective delivery of hydrophobic molecules are developed. They have potential to deliver drugs into folate‐receptor over‐expressing cancer cells HeLa via folate receptors mediated endocytosis in vitro and in vivo. These micelle systems can be used in the delivery of anticancer drugs and their selective target to cancer cells.</description><identifier>ISSN: 1616-5187</identifier><identifier>EISSN: 1616-5195</identifier><identifier>DOI: 10.1002/mabi.200900134</identifier><identifier>PMID: 19688723</identifier><language>eng</language><publisher>Weinheim: WILEY-VCH Verlag</publisher><subject>Animals ; Applied sciences ; Biocompatible Materials - chemistry ; Biocompatible Materials - metabolism ; Biological and medical sciences ; Carrier Proteins - metabolism ; Chemical modifications ; Chemical reactions and properties ; CHO Cells ; Cricetinae ; Cricetulus ; Drug Carriers - chemistry ; Drug Carriers - metabolism ; Drug Delivery Systems ; endocytosis ; Endocytosis - physiology ; Exact sciences and technology ; Folate Receptors, GPI-Anchored ; folic acid ; Folic Acid - chemistry ; Folic Acid - metabolism ; Folic Acid - therapeutic use ; General pharmacology ; HeLa Cells ; Humans ; Materials Testing ; Medical sciences ; Mice ; Micelles ; Molecular Structure ; Neoplasms - drug therapy ; Neoplasms - pathology ; Organic polymers ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Physicochemistry of polymers ; Polymers - chemistry ; Polymers - metabolism ; receptor ; Receptors, Cell Surface - metabolism ; targeting ; Vitamin B Complex - chemistry ; Vitamin B Complex - metabolism ; Vitamin B Complex - therapeutic use</subject><ispartof>Macromolecular bioscience, 2009-11, Vol.9 (11), p.1059-1068</ispartof><rights>Copyright © 2009 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4444-53a3948f095c9a47bf78a3800145bbc73817dab2eaed8a2c7712b20929eb19293</citedby><cites>FETCH-LOGICAL-c4444-53a3948f095c9a47bf78a3800145bbc73817dab2eaed8a2c7712b20929eb19293</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fmabi.200900134$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fmabi.200900134$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22125372$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19688723$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lu, Tiancheng</creatorcontrib><creatorcontrib>Sun, Jing</creatorcontrib><creatorcontrib>Chen, Xuexi</creatorcontrib><creatorcontrib>Zhang, Peibiao</creatorcontrib><creatorcontrib>Jing, Xiabin</creatorcontrib><title>Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis</title><title>Macromolecular bioscience</title><addtitle>Macromol. Biosci</addtitle><description>A folate‐conjugated copolymer PEG‐PLA‐PLL/folate was synthesized and mixed with pure PEG‐PLA‐PLL and a fluorescent model drug mFITC to prepare folate‐conjugated micelles. The distribution of micelles was studied on cancer‐cell‐bearing mice via frozen slicing. The results show that mFITC is successfully encapsulated into folate(+) and folate(−)micelles; PEG‐PLA‐PLL micelles the latter can be internalized by both HeLa and CHO cells without selectivity due to their cationic surface charges, while folate(+)micelles exhibit more preferential endocytosis by HeLa cells than by CHO cells. The folate(−)micelles showed retention in both organs and tumors. The folate(+)micelles are a promising active targeting drug delivery system for FR over‐expressing cells and they accumulate in tumor beds.
Folate‐conjugated micelles for the selective delivery of hydrophobic molecules are developed. They have potential to deliver drugs into folate‐receptor over‐expressing cancer cells HeLa via folate receptors mediated endocytosis in vitro and in vivo. These micelle systems can be used in the delivery of anticancer drugs and their selective target to cancer cells.</description><subject>Animals</subject><subject>Applied sciences</subject><subject>Biocompatible Materials - chemistry</subject><subject>Biocompatible Materials - metabolism</subject><subject>Biological and medical sciences</subject><subject>Carrier Proteins - metabolism</subject><subject>Chemical modifications</subject><subject>Chemical reactions and properties</subject><subject>CHO Cells</subject><subject>Cricetinae</subject><subject>Cricetulus</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - metabolism</subject><subject>Drug Delivery Systems</subject><subject>endocytosis</subject><subject>Endocytosis - physiology</subject><subject>Exact sciences and technology</subject><subject>Folate Receptors, GPI-Anchored</subject><subject>folic acid</subject><subject>Folic Acid - chemistry</subject><subject>Folic Acid - metabolism</subject><subject>Folic Acid - therapeutic use</subject><subject>General pharmacology</subject><subject>HeLa Cells</subject><subject>Humans</subject><subject>Materials Testing</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Micelles</subject><subject>Molecular Structure</subject><subject>Neoplasms - drug therapy</subject><subject>Neoplasms - pathology</subject><subject>Organic polymers</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Physicochemistry of polymers</subject><subject>Polymers - chemistry</subject><subject>Polymers - metabolism</subject><subject>receptor</subject><subject>Receptors, Cell Surface - metabolism</subject><subject>targeting</subject><subject>Vitamin B Complex - chemistry</subject><subject>Vitamin B Complex - metabolism</subject><subject>Vitamin B Complex - therapeutic use</subject><issn>1616-5187</issn><issn>1616-5195</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0M9P2zAUB3ALgYAVrjtOvSBOKf4Z20dWAaugG4IijpbjvIBZmhQ7Fet_P5dGhRs-2O_wec9PX4S-EzwiGNOzuS38iGKsMSaM76BDkpM8E0SL3W2t5AH6FuNLIlJpuo8OiM6VkpQdosllW9sOsnHbvCyfUlUOp95BXUMc2qYczp7Bh2GP7sDBomtDNoXSv9uLpmzdqmujj0dor7J1hOP-HaCHy4vZ-Fd28-dqMj6_yRxPJxPMMs1VhbVw2nJZVFJZptJuXBSFk0wRWdqCgoVSWeqkJLSgWFMNBUk3G6DTzdxFaF-XEDsz93G9sW2gXUYjBRc5x1x8LRknDEsikxxtpAttjAEqswh-bsPKEGzWOZt1zmabc2r40Y9eFnMoP3gfbAInPbDR2boKtnE-bh2lhAqW4ADpjXvzNay--NZMz39OPi-RbXp97ODftteGvyaXTArz-PvK3F5P8X0-k-aR_QeHkqRP</recordid><startdate>20091110</startdate><enddate>20091110</enddate><creator>Lu, Tiancheng</creator><creator>Sun, Jing</creator><creator>Chen, Xuexi</creator><creator>Zhang, Peibiao</creator><creator>Jing, Xiabin</creator><general>WILEY-VCH Verlag</general><general>WILEY‐VCH Verlag</general><general>Wiley-VCH</general><scope>BSCLL</scope><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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20091110</creationdate><title>Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis</title><author>Lu, Tiancheng ; Sun, Jing ; Chen, Xuexi ; Zhang, Peibiao ; Jing, Xiabin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4444-53a3948f095c9a47bf78a3800145bbc73817dab2eaed8a2c7712b20929eb19293</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Applied sciences</topic><topic>Biocompatible Materials - chemistry</topic><topic>Biocompatible Materials - metabolism</topic><topic>Biological and medical sciences</topic><topic>Carrier Proteins - metabolism</topic><topic>Chemical modifications</topic><topic>Chemical reactions and properties</topic><topic>CHO Cells</topic><topic>Cricetinae</topic><topic>Cricetulus</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - metabolism</topic><topic>Drug Delivery Systems</topic><topic>endocytosis</topic><topic>Endocytosis - physiology</topic><topic>Exact sciences and technology</topic><topic>Folate Receptors, GPI-Anchored</topic><topic>folic acid</topic><topic>Folic Acid - chemistry</topic><topic>Folic Acid - metabolism</topic><topic>Folic Acid - therapeutic use</topic><topic>General pharmacology</topic><topic>HeLa Cells</topic><topic>Humans</topic><topic>Materials Testing</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Micelles</topic><topic>Molecular Structure</topic><topic>Neoplasms - drug therapy</topic><topic>Neoplasms - pathology</topic><topic>Organic polymers</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Physicochemistry of polymers</topic><topic>Polymers - chemistry</topic><topic>Polymers - metabolism</topic><topic>receptor</topic><topic>Receptors, Cell Surface - metabolism</topic><topic>targeting</topic><topic>Vitamin B Complex - chemistry</topic><topic>Vitamin B Complex - metabolism</topic><topic>Vitamin B Complex - therapeutic use</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lu, Tiancheng</creatorcontrib><creatorcontrib>Sun, Jing</creatorcontrib><creatorcontrib>Chen, Xuexi</creatorcontrib><creatorcontrib>Zhang, Peibiao</creatorcontrib><creatorcontrib>Jing, Xiabin</creatorcontrib><collection>Istex</collection><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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Macromolecular bioscience</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lu, Tiancheng</au><au>Sun, Jing</au><au>Chen, Xuexi</au><au>Zhang, Peibiao</au><au>Jing, Xiabin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis</atitle><jtitle>Macromolecular bioscience</jtitle><addtitle>Macromol. Biosci</addtitle><date>2009-11-10</date><risdate>2009</risdate><volume>9</volume><issue>11</issue><spage>1059</spage><epage>1068</epage><pages>1059-1068</pages><issn>1616-5187</issn><eissn>1616-5195</eissn><abstract>A folate‐conjugated copolymer PEG‐PLA‐PLL/folate was synthesized and mixed with pure PEG‐PLA‐PLL and a fluorescent model drug mFITC to prepare folate‐conjugated micelles. The distribution of micelles was studied on cancer‐cell‐bearing mice via frozen slicing. The results show that mFITC is successfully encapsulated into folate(+) and folate(−)micelles; PEG‐PLA‐PLL micelles the latter can be internalized by both HeLa and CHO cells without selectivity due to their cationic surface charges, while folate(+)micelles exhibit more preferential endocytosis by HeLa cells than by CHO cells. The folate(−)micelles showed retention in both organs and tumors. The folate(+)micelles are a promising active targeting drug delivery system for FR over‐expressing cells and they accumulate in tumor beds.
Folate‐conjugated micelles for the selective delivery of hydrophobic molecules are developed. They have potential to deliver drugs into folate‐receptor over‐expressing cancer cells HeLa via folate receptors mediated endocytosis in vitro and in vivo. These micelle systems can be used in the delivery of anticancer drugs and their selective target to cancer cells.</abstract><cop>Weinheim</cop><pub>WILEY-VCH Verlag</pub><pmid>19688723</pmid><doi>10.1002/mabi.200900134</doi><tpages>10</tpages></addata></record> |
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| subjects | Animals Applied sciences Biocompatible Materials - chemistry Biocompatible Materials - metabolism Biological and medical sciences Carrier Proteins - metabolism Chemical modifications Chemical reactions and properties CHO Cells Cricetinae Cricetulus Drug Carriers - chemistry Drug Carriers - metabolism Drug Delivery Systems endocytosis Endocytosis - physiology Exact sciences and technology Folate Receptors, GPI-Anchored folic acid Folic Acid - chemistry Folic Acid - metabolism Folic Acid - therapeutic use General pharmacology HeLa Cells Humans Materials Testing Medical sciences Mice Micelles Molecular Structure Neoplasms - drug therapy Neoplasms - pathology Organic polymers Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Physicochemistry of polymers Polymers - chemistry Polymers - metabolism receptor Receptors, Cell Surface - metabolism targeting Vitamin B Complex - chemistry Vitamin B Complex - metabolism Vitamin B Complex - therapeutic use |
| title | Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis |
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