Development of a folate-modified curcumin loaded micelle delivery system for cancer targeting
The Cur-FPPs’ preparing flow chart and cellular uptake on MCF-7 and HepG2 cells in vitro. •The folate-modified Curcumin loaded micelles (Cur-FPPs) were prepared by thin-film hydration method.•The Cur-FPPs increased the cytotoxicity and cellular uptake of Cur on MCF-7 and HepG2 cells in vitro.•The Cu...
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Veröffentlicht in: | Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2014-09, Vol.121, p.206-213 |
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creator | Yang, Chunfen Chen, Hao Zhao, Jie Pang, Xin Xi, Yanwei Zhai, Guangxi |
description | The Cur-FPPs’ preparing flow chart and cellular uptake on MCF-7 and HepG2 cells in vitro.
•The folate-modified Curcumin loaded micelles (Cur-FPPs) were prepared by thin-film hydration method.•The Cur-FPPs increased the cytotoxicity and cellular uptake of Cur on MCF-7 and HepG2 cells in vitro.•The Cur-FPPs prolonged the half-life of Cur in rats.
Targeted drug delivery system for tumor cells is an appealing platform on enhancing the therapeutic effects and reducing the side effects of the drug. In this study, we developed folate-modified curcumin (Cur) loaded micelles (Cur-FPPs) for cancer chemotherapy. The targeting material, Folate-PEG3000-PLA2000, was synthesized by the amide bond formation reaction. And the Cur loaded micelles were prepared by thin-film hydration method with mPEG2000-PLA2000 (Cur-PPs) or mPEG2000-PLA2000 and Folate-PEG3000-PLA2000 (Cur-FPPs) as carrier. A central composite design (CCD) was used to optimize the formulation, and the optimized Cur-FPPs was prepared with the weight ratio of Folate-PEG3000-PLA2000 and mPEG2000-PLA2000 at 1:9. The average size of the mixed micelles was 70nm, the encapsulating efficiency and drug-loading were 80.73±0.16% and 4.84±0.01%, respectively. Compared with the Cur propylene glycol solution, the in vitro release of Cur from Cur-FPPs showed a sustained manner. Furthermore, the in vitro cytotoxicity and cellular uptake of Cur-FPPs were significantly enhanced towards MCF-7 and HepG2 cells. The pharmacokinetic studies in rats indicated that a 3-fold increase in the half-life was achieved for Cur loaded micelle formulations relative to solubilized Cur. All the results demonstrated that folate-modified Cur micelles could serve as a potential nanocarrier to improve the solubility and anti-cancer activity of Cur. |
doi_str_mv | 10.1016/j.colsurfb.2014.05.005 |
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•The folate-modified Curcumin loaded micelles (Cur-FPPs) were prepared by thin-film hydration method.•The Cur-FPPs increased the cytotoxicity and cellular uptake of Cur on MCF-7 and HepG2 cells in vitro.•The Cur-FPPs prolonged the half-life of Cur in rats.
Targeted drug delivery system for tumor cells is an appealing platform on enhancing the therapeutic effects and reducing the side effects of the drug. In this study, we developed folate-modified curcumin (Cur) loaded micelles (Cur-FPPs) for cancer chemotherapy. The targeting material, Folate-PEG3000-PLA2000, was synthesized by the amide bond formation reaction. And the Cur loaded micelles were prepared by thin-film hydration method with mPEG2000-PLA2000 (Cur-PPs) or mPEG2000-PLA2000 and Folate-PEG3000-PLA2000 (Cur-FPPs) as carrier. A central composite design (CCD) was used to optimize the formulation, and the optimized Cur-FPPs was prepared with the weight ratio of Folate-PEG3000-PLA2000 and mPEG2000-PLA2000 at 1:9. The average size of the mixed micelles was 70nm, the encapsulating efficiency and drug-loading were 80.73±0.16% and 4.84±0.01%, respectively. Compared with the Cur propylene glycol solution, the in vitro release of Cur from Cur-FPPs showed a sustained manner. Furthermore, the in vitro cytotoxicity and cellular uptake of Cur-FPPs were significantly enhanced towards MCF-7 and HepG2 cells. The pharmacokinetic studies in rats indicated that a 3-fold increase in the half-life was achieved for Cur loaded micelle formulations relative to solubilized Cur. All the results demonstrated that folate-modified Cur micelles could serve as a potential nanocarrier to improve the solubility and anti-cancer activity of Cur.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2014.05.005</identifier><identifier>PMID: 24984268</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Animals ; Cancer ; Cell Death - drug effects ; Cell Survival - drug effects ; Cellular ; Charge coupled devices ; Curcumin ; Curcumin - administration & dosage ; Curcumin - pharmacokinetics ; Curcumin - pharmacology ; Curcumin - therapeutic use ; Delivery systems ; Drug Delivery Systems ; Endocytosis - drug effects ; Folate ; Folic Acid - chemistry ; Formulations ; Hemolysis - drug effects ; Hep G2 Cells ; Humans ; In vitro testing ; Irritants - pharmacology ; Lactic Acid - chemical synthesis ; Lactic Acid - chemistry ; Male ; MCF-7 Cells ; Micelles ; Microscopy, Fluorescence ; mPEG-PLA ; Nanostructure ; Neoplasms - drug therapy ; Particle Size ; Polyesters ; Polyethylene Glycols - chemical synthesis ; Polyethylene Glycols - chemistry ; Polymers - chemical synthesis ; Polymers - chemistry ; Rabbits ; Rats ; Static Electricity ; Surface-Active Agents - chemical synthesis ; Surface-Active Agents - chemistry</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2014-09, Vol.121, p.206-213</ispartof><rights>2014</rights><rights>Crown Copyright © 2014. Published by Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c434t-4c2a85e364f9797d1ba869c0e173009f9d8b5a6cf80ccd0d2b54ffecae31f7b23</citedby><cites>FETCH-LOGICAL-c434t-4c2a85e364f9797d1ba869c0e173009f9d8b5a6cf80ccd0d2b54ffecae31f7b23</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0927776514002318$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24984268$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yang, Chunfen</creatorcontrib><creatorcontrib>Chen, Hao</creatorcontrib><creatorcontrib>Zhao, Jie</creatorcontrib><creatorcontrib>Pang, Xin</creatorcontrib><creatorcontrib>Xi, Yanwei</creatorcontrib><creatorcontrib>Zhai, Guangxi</creatorcontrib><title>Development of a folate-modified curcumin loaded micelle delivery system for cancer targeting</title><title>Colloids and surfaces, B, Biointerfaces</title><addtitle>Colloids Surf B Biointerfaces</addtitle><description>The Cur-FPPs’ preparing flow chart and cellular uptake on MCF-7 and HepG2 cells in vitro.
•The folate-modified Curcumin loaded micelles (Cur-FPPs) were prepared by thin-film hydration method.•The Cur-FPPs increased the cytotoxicity and cellular uptake of Cur on MCF-7 and HepG2 cells in vitro.•The Cur-FPPs prolonged the half-life of Cur in rats.
Targeted drug delivery system for tumor cells is an appealing platform on enhancing the therapeutic effects and reducing the side effects of the drug. In this study, we developed folate-modified curcumin (Cur) loaded micelles (Cur-FPPs) for cancer chemotherapy. The targeting material, Folate-PEG3000-PLA2000, was synthesized by the amide bond formation reaction. And the Cur loaded micelles were prepared by thin-film hydration method with mPEG2000-PLA2000 (Cur-PPs) or mPEG2000-PLA2000 and Folate-PEG3000-PLA2000 (Cur-FPPs) as carrier. A central composite design (CCD) was used to optimize the formulation, and the optimized Cur-FPPs was prepared with the weight ratio of Folate-PEG3000-PLA2000 and mPEG2000-PLA2000 at 1:9. The average size of the mixed micelles was 70nm, the encapsulating efficiency and drug-loading were 80.73±0.16% and 4.84±0.01%, respectively. Compared with the Cur propylene glycol solution, the in vitro release of Cur from Cur-FPPs showed a sustained manner. Furthermore, the in vitro cytotoxicity and cellular uptake of Cur-FPPs were significantly enhanced towards MCF-7 and HepG2 cells. The pharmacokinetic studies in rats indicated that a 3-fold increase in the half-life was achieved for Cur loaded micelle formulations relative to solubilized Cur. All the results demonstrated that folate-modified Cur micelles could serve as a potential nanocarrier to improve the solubility and anti-cancer activity of Cur.</description><subject>Animals</subject><subject>Cancer</subject><subject>Cell Death - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>Cellular</subject><subject>Charge coupled devices</subject><subject>Curcumin</subject><subject>Curcumin - administration & dosage</subject><subject>Curcumin - pharmacokinetics</subject><subject>Curcumin - pharmacology</subject><subject>Curcumin - therapeutic use</subject><subject>Delivery systems</subject><subject>Drug Delivery Systems</subject><subject>Endocytosis - drug effects</subject><subject>Folate</subject><subject>Folic Acid - chemistry</subject><subject>Formulations</subject><subject>Hemolysis - drug effects</subject><subject>Hep G2 Cells</subject><subject>Humans</subject><subject>In vitro testing</subject><subject>Irritants - pharmacology</subject><subject>Lactic Acid - chemical synthesis</subject><subject>Lactic Acid - chemistry</subject><subject>Male</subject><subject>MCF-7 Cells</subject><subject>Micelles</subject><subject>Microscopy, Fluorescence</subject><subject>mPEG-PLA</subject><subject>Nanostructure</subject><subject>Neoplasms - drug therapy</subject><subject>Particle Size</subject><subject>Polyesters</subject><subject>Polyethylene Glycols - chemical synthesis</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Polymers - chemical synthesis</subject><subject>Polymers - chemistry</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Static Electricity</subject><subject>Surface-Active Agents - chemical synthesis</subject><subject>Surface-Active Agents - chemistry</subject><issn>0927-7765</issn><issn>1873-4367</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkU1v1DAQhi0EokvhL1Q-ckkYO_7KDVTKh1SJCxyR5djjyqskXuxkpf33ZLUt13IajfS8M6N5CLlh0DJg6sO-9Xmsa4lDy4GJFmQLIF-QHTO6a0Sn9Euyg57rRmslr8ibWvcAwAXTr8kVF70RXJkd-f0Zjzjmw4TzQnOkjsY8ugWbKYcUEwbq1-LXKc10zC5s_ZQ8jiPSgGM6YjnReqoLTluuUO9mj4UurjzgkuaHt-RVdGPFd4_1mvz6cvfz9ltz_-Pr99tP940XnVga4bkzEjslYq97HdjgjOo9INMdQB_7YAbplI8GvA8Q-CBFjOgddizqgXfX5P1l7qHkPyvWxU6pns90M-a1WqYE7zjrFPwHynUvTM_F86iUzDCjgG2ouqC-5FoLRnsoaXLlZBnYszC7t0_C7FmYBWk3YVvw5nHHOkwY_sWeDG3AxwuA2_-OCYutPuH25pAK-sWGnJ7b8Rewm6tq</recordid><startdate>20140901</startdate><enddate>20140901</enddate><creator>Yang, Chunfen</creator><creator>Chen, Hao</creator><creator>Zhao, Jie</creator><creator>Pang, Xin</creator><creator>Xi, Yanwei</creator><creator>Zhai, Guangxi</creator><general>Elsevier B.V</general><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><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>JG9</scope><scope>L7M</scope></search><sort><creationdate>20140901</creationdate><title>Development of a folate-modified curcumin loaded micelle delivery system for cancer targeting</title><author>Yang, Chunfen ; Chen, Hao ; Zhao, Jie ; Pang, Xin ; Xi, Yanwei ; Zhai, Guangxi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c434t-4c2a85e364f9797d1ba869c0e173009f9d8b5a6cf80ccd0d2b54ffecae31f7b23</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Animals</topic><topic>Cancer</topic><topic>Cell Death - drug effects</topic><topic>Cell Survival - drug effects</topic><topic>Cellular</topic><topic>Charge coupled devices</topic><topic>Curcumin</topic><topic>Curcumin - administration & dosage</topic><topic>Curcumin - pharmacokinetics</topic><topic>Curcumin - pharmacology</topic><topic>Curcumin - therapeutic use</topic><topic>Delivery systems</topic><topic>Drug Delivery Systems</topic><topic>Endocytosis - drug effects</topic><topic>Folate</topic><topic>Folic Acid - chemistry</topic><topic>Formulations</topic><topic>Hemolysis - drug effects</topic><topic>Hep G2 Cells</topic><topic>Humans</topic><topic>In vitro testing</topic><topic>Irritants - pharmacology</topic><topic>Lactic Acid - chemical synthesis</topic><topic>Lactic Acid - chemistry</topic><topic>Male</topic><topic>MCF-7 Cells</topic><topic>Micelles</topic><topic>Microscopy, Fluorescence</topic><topic>mPEG-PLA</topic><topic>Nanostructure</topic><topic>Neoplasms - drug therapy</topic><topic>Particle Size</topic><topic>Polyesters</topic><topic>Polyethylene Glycols - chemical synthesis</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Polymers - chemical synthesis</topic><topic>Polymers - chemistry</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Static Electricity</topic><topic>Surface-Active Agents - chemical synthesis</topic><topic>Surface-Active Agents - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yang, Chunfen</creatorcontrib><creatorcontrib>Chen, Hao</creatorcontrib><creatorcontrib>Zhao, Jie</creatorcontrib><creatorcontrib>Pang, Xin</creatorcontrib><creatorcontrib>Xi, Yanwei</creatorcontrib><creatorcontrib>Zhai, Guangxi</creatorcontrib><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><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yang, Chunfen</au><au>Chen, Hao</au><au>Zhao, Jie</au><au>Pang, Xin</au><au>Xi, Yanwei</au><au>Zhai, Guangxi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of a folate-modified curcumin loaded micelle delivery system for cancer targeting</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2014-09-01</date><risdate>2014</risdate><volume>121</volume><spage>206</spage><epage>213</epage><pages>206-213</pages><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>The Cur-FPPs’ preparing flow chart and cellular uptake on MCF-7 and HepG2 cells in vitro.
•The folate-modified Curcumin loaded micelles (Cur-FPPs) were prepared by thin-film hydration method.•The Cur-FPPs increased the cytotoxicity and cellular uptake of Cur on MCF-7 and HepG2 cells in vitro.•The Cur-FPPs prolonged the half-life of Cur in rats.
Targeted drug delivery system for tumor cells is an appealing platform on enhancing the therapeutic effects and reducing the side effects of the drug. In this study, we developed folate-modified curcumin (Cur) loaded micelles (Cur-FPPs) for cancer chemotherapy. The targeting material, Folate-PEG3000-PLA2000, was synthesized by the amide bond formation reaction. And the Cur loaded micelles were prepared by thin-film hydration method with mPEG2000-PLA2000 (Cur-PPs) or mPEG2000-PLA2000 and Folate-PEG3000-PLA2000 (Cur-FPPs) as carrier. A central composite design (CCD) was used to optimize the formulation, and the optimized Cur-FPPs was prepared with the weight ratio of Folate-PEG3000-PLA2000 and mPEG2000-PLA2000 at 1:9. The average size of the mixed micelles was 70nm, the encapsulating efficiency and drug-loading were 80.73±0.16% and 4.84±0.01%, respectively. Compared with the Cur propylene glycol solution, the in vitro release of Cur from Cur-FPPs showed a sustained manner. Furthermore, the in vitro cytotoxicity and cellular uptake of Cur-FPPs were significantly enhanced towards MCF-7 and HepG2 cells. The pharmacokinetic studies in rats indicated that a 3-fold increase in the half-life was achieved for Cur loaded micelle formulations relative to solubilized Cur. All the results demonstrated that folate-modified Cur micelles could serve as a potential nanocarrier to improve the solubility and anti-cancer activity of Cur.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>24984268</pmid><doi>10.1016/j.colsurfb.2014.05.005</doi><tpages>8</tpages></addata></record> |
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subjects | Animals Cancer Cell Death - drug effects Cell Survival - drug effects Cellular Charge coupled devices Curcumin Curcumin - administration & dosage Curcumin - pharmacokinetics Curcumin - pharmacology Curcumin - therapeutic use Delivery systems Drug Delivery Systems Endocytosis - drug effects Folate Folic Acid - chemistry Formulations Hemolysis - drug effects Hep G2 Cells Humans In vitro testing Irritants - pharmacology Lactic Acid - chemical synthesis Lactic Acid - chemistry Male MCF-7 Cells Micelles Microscopy, Fluorescence mPEG-PLA Nanostructure Neoplasms - drug therapy Particle Size Polyesters Polyethylene Glycols - chemical synthesis Polyethylene Glycols - chemistry Polymers - chemical synthesis Polymers - chemistry Rabbits Rats Static Electricity Surface-Active Agents - chemical synthesis Surface-Active Agents - chemistry |
title | Development of a folate-modified curcumin loaded micelle delivery system for cancer targeting |
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