Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin
ABSTRACT Purpose To utilize a novel type of polymer-drug conjugate micelle to enhance the delivery of low-potency curcumin. Methods Multiple curcumin molecules were conjugated to poly(lactic acid) (PLA) via tris(hydroxymethyl)aminomethane (Tris) linker producing the hydrophobic drug-binding block; m...
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| Veröffentlicht in: | Pharmaceutical research 2012-12, Vol.29 (12), p.3512-3525 |
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| creator | Yang, Rulei Zhang, Suai Kong, Deling Gao, Xuli Zhao, Yanjun Wang, Zheng |
| description | ABSTRACT
Purpose
To utilize a novel type of polymer-drug conjugate micelle to enhance the delivery of low-potency curcumin.
Methods
Multiple curcumin molecules were conjugated to poly(lactic acid) (PLA) via tris(hydroxymethyl)aminomethane (Tris) linker producing the hydrophobic drug-binding block; methoxy-poly(ethylene glycol) (mPEG) was employed as the hydrophilic block. Micelles were characterized by size, loading capacity, stability, and critical micelle concentration (CMC). Human hepatocellular carcinoma (HepG2) cells were employed to assess cytotoxicity and intracellular targeting ability of micelles.
Results
mPEG-PLA-Tris-Cur micelles were within nanorange ( |
| doi_str_mv | 10.1007/s11095-012-0848-8 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1434013748</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2815226211</sourcerecordid><originalsourceid>FETCH-LOGICAL-c435t-38a7debcd111f7d07c32f4826ab2c60f4dc7eb0294a8786aecfc8a6f1ae4bd0d3</originalsourceid><addsrcrecordid>eNp1kdGK1DAUhoMo7uzqA3gjARG8ieakaZNeuuOuCiPuhYJ3IU1OZzu0yZq0yry9GWZWRfAqkHznz8_5CHkG_DVwrt5kAN7WjINgXEvN9AOyglpVrOXy20Oy4kpIppWEM3Ke845zrqGVj8mZEG0DtdYrsrscosdtst52I9KbOO4nTGy9JLdMQ6DrGHbL1s5IPw0OxxEzvQq3Njik8y3STbR-CFtqg6fvcBx-YNrT2Jf7n-wmzhjcnt5nPSGPejtmfHo6L8jX66sv6w9s8_n9x_XbDXOyqmdWaas8ds4DQK88V64SvdSisZ1wDe-ldwo7LlpptdKNRdc7bZseLMrOc19dkFfH3LsUvy-YZzMN-dDdBoxLNiAryaFSUhf0xT_oLi4plHYGoAbN60pAoeBIuRRzTtibuzRMNu0NcHMQYY4iTBFhDiLMIfn5KXnpJvS_J-43X4CXJ8BmZ8c-lZ0O-Q_XFIcNrwonjlwuT2GL6a-K__39Fw-PoPc</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1151805321</pqid></control><display><type>article</type><title>Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin</title><source>MEDLINE</source><source>SpringerLink Journals - AutoHoldings</source><creator>Yang, Rulei ; Zhang, Suai ; Kong, Deling ; Gao, Xuli ; Zhao, Yanjun ; Wang, Zheng</creator><creatorcontrib>Yang, Rulei ; Zhang, Suai ; Kong, Deling ; Gao, Xuli ; Zhao, Yanjun ; Wang, Zheng</creatorcontrib><description>ABSTRACT
Purpose
To utilize a novel type of polymer-drug conjugate micelle to enhance the delivery of low-potency curcumin.
Methods
Multiple curcumin molecules were conjugated to poly(lactic acid) (PLA) via tris(hydroxymethyl)aminomethane (Tris) linker producing the hydrophobic drug-binding block; methoxy-poly(ethylene glycol) (mPEG) was employed as the hydrophilic block. Micelles were characterized by size, loading capacity, stability, and critical micelle concentration (CMC). Human hepatocellular carcinoma (HepG2) cells were employed to assess cytotoxicity and intracellular targeting ability of micelles.
Results
mPEG-PLA-Tris-Cur micelles were within nanorange (<100 nm). CMC of such micelles (2.3 ± 0.4 μg/mL) was 10 times lower than mPEG-PLA micelles (27.4 ± 0.8 μg/mL). Curcumin loading in mPEG-PLA-Tris-Cur micelles reached 18.5 ± 1.3% (w/w), compared to traditional mPEG-PLA micelles at 3.6 ± 0.4% (w/w). IC
50
of mPEG-PLA-Tris-Cur micelles (~22 μg/mL at curcumin-equivalent dose) was similar to unmodified curcumin. Placebo and drug-encapsulated conjugate micelles could be efficiently internalized to cytoplasmic compartment of HepG2 cells.
Conclusions
Micelle-forming polymer-drug conjugates containing multiple drug molecules were an efficient means to increase loading and intracellular delivery of low-potency curcumin.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1007/s11095-012-0848-8</identifier><identifier>PMID: 22961588</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Antineoplastic Agents - administration & dosage ; Antineoplastic Agents - pharmacokinetics ; Antineoplastic Agents - pharmacology ; Biochemistry ; Biodegradable materials ; Biological and medical sciences ; Biomedical and Life Sciences ; Biomedical Engineering and Bioengineering ; Biomedicine ; Biopolymers ; Cell Survival - drug effects ; Curcumin - administration & dosage ; Curcumin - pharmacokinetics ; Curcumin - pharmacology ; Drug Carriers - chemistry ; Drug delivery systems ; General pharmacology ; Hep G2 Cells ; Humans ; Medical Law ; Medical sciences ; Micelles ; Neoplasms - drug therapy ; Pharmaceutical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Pharmacology/Toxicology ; Pharmacy ; Polyesters - chemistry ; Polyethylene Glycols - chemistry ; Research Paper</subject><ispartof>Pharmaceutical research, 2012-12, Vol.29 (12), p.3512-3525</ispartof><rights>Springer Science+Business Media, LLC 2012</rights><rights>2014 INIST-CNRS</rights><rights>Springer Science+Business Media New York 2012</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c435t-38a7debcd111f7d07c32f4826ab2c60f4dc7eb0294a8786aecfc8a6f1ae4bd0d3</citedby><cites>FETCH-LOGICAL-c435t-38a7debcd111f7d07c32f4826ab2c60f4dc7eb0294a8786aecfc8a6f1ae4bd0d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11095-012-0848-8$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11095-012-0848-8$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26904603$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22961588$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yang, Rulei</creatorcontrib><creatorcontrib>Zhang, Suai</creatorcontrib><creatorcontrib>Kong, Deling</creatorcontrib><creatorcontrib>Gao, Xuli</creatorcontrib><creatorcontrib>Zhao, Yanjun</creatorcontrib><creatorcontrib>Wang, Zheng</creatorcontrib><title>Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><addtitle>Pharm Res</addtitle><description>ABSTRACT
Purpose
To utilize a novel type of polymer-drug conjugate micelle to enhance the delivery of low-potency curcumin.
Methods
Multiple curcumin molecules were conjugated to poly(lactic acid) (PLA) via tris(hydroxymethyl)aminomethane (Tris) linker producing the hydrophobic drug-binding block; methoxy-poly(ethylene glycol) (mPEG) was employed as the hydrophilic block. Micelles were characterized by size, loading capacity, stability, and critical micelle concentration (CMC). Human hepatocellular carcinoma (HepG2) cells were employed to assess cytotoxicity and intracellular targeting ability of micelles.
Results
mPEG-PLA-Tris-Cur micelles were within nanorange (<100 nm). CMC of such micelles (2.3 ± 0.4 μg/mL) was 10 times lower than mPEG-PLA micelles (27.4 ± 0.8 μg/mL). Curcumin loading in mPEG-PLA-Tris-Cur micelles reached 18.5 ± 1.3% (w/w), compared to traditional mPEG-PLA micelles at 3.6 ± 0.4% (w/w). IC
50
of mPEG-PLA-Tris-Cur micelles (~22 μg/mL at curcumin-equivalent dose) was similar to unmodified curcumin. Placebo and drug-encapsulated conjugate micelles could be efficiently internalized to cytoplasmic compartment of HepG2 cells.
Conclusions
Micelle-forming polymer-drug conjugates containing multiple drug molecules were an efficient means to increase loading and intracellular delivery of low-potency curcumin.</description><subject>Antineoplastic Agents - administration & dosage</subject><subject>Antineoplastic Agents - pharmacokinetics</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Biochemistry</subject><subject>Biodegradable materials</subject><subject>Biological and medical sciences</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedical Engineering and Bioengineering</subject><subject>Biomedicine</subject><subject>Biopolymers</subject><subject>Cell Survival - drug effects</subject><subject>Curcumin - administration & dosage</subject><subject>Curcumin - pharmacokinetics</subject><subject>Curcumin - pharmacology</subject><subject>Drug Carriers - chemistry</subject><subject>Drug delivery systems</subject><subject>General pharmacology</subject><subject>Hep G2 Cells</subject><subject>Humans</subject><subject>Medical Law</subject><subject>Medical sciences</subject><subject>Micelles</subject><subject>Neoplasms - drug therapy</subject><subject>Pharmaceutical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Polyesters - chemistry</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Research Paper</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNp1kdGK1DAUhoMo7uzqA3gjARG8ieakaZNeuuOuCiPuhYJ3IU1OZzu0yZq0yry9GWZWRfAqkHznz8_5CHkG_DVwrt5kAN7WjINgXEvN9AOyglpVrOXy20Oy4kpIppWEM3Ke845zrqGVj8mZEG0DtdYrsrscosdtst52I9KbOO4nTGy9JLdMQ6DrGHbL1s5IPw0OxxEzvQq3Njik8y3STbR-CFtqg6fvcBx-YNrT2Jf7n-wmzhjcnt5nPSGPejtmfHo6L8jX66sv6w9s8_n9x_XbDXOyqmdWaas8ds4DQK88V64SvdSisZ1wDe-ldwo7LlpptdKNRdc7bZseLMrOc19dkFfH3LsUvy-YZzMN-dDdBoxLNiAryaFSUhf0xT_oLi4plHYGoAbN60pAoeBIuRRzTtibuzRMNu0NcHMQYY4iTBFhDiLMIfn5KXnpJvS_J-43X4CXJ8BmZ8c-lZ0O-Q_XFIcNrwonjlwuT2GL6a-K__39Fw-PoPc</recordid><startdate>20121201</startdate><enddate>20121201</enddate><creator>Yang, Rulei</creator><creator>Zhang, Suai</creator><creator>Kong, Deling</creator><creator>Gao, Xuli</creator><creator>Zhao, Yanjun</creator><creator>Wang, Zheng</creator><general>Springer US</general><general>Springer</general><general>Springer Nature B.V</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>3V.</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>K9.</scope><scope>KB0</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>7QO</scope><scope>7T7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20121201</creationdate><title>Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin</title><author>Yang, Rulei ; Zhang, Suai ; Kong, Deling ; Gao, Xuli ; Zhao, Yanjun ; Wang, Zheng</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c435t-38a7debcd111f7d07c32f4826ab2c60f4dc7eb0294a8786aecfc8a6f1ae4bd0d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Antineoplastic Agents - administration & dosage</topic><topic>Antineoplastic Agents - pharmacokinetics</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Biochemistry</topic><topic>Biodegradable materials</topic><topic>Biological and medical sciences</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedical Engineering and Bioengineering</topic><topic>Biomedicine</topic><topic>Biopolymers</topic><topic>Cell Survival - drug effects</topic><topic>Curcumin - administration & dosage</topic><topic>Curcumin - pharmacokinetics</topic><topic>Curcumin - pharmacology</topic><topic>Drug Carriers - chemistry</topic><topic>Drug delivery systems</topic><topic>General pharmacology</topic><topic>Hep G2 Cells</topic><topic>Humans</topic><topic>Medical Law</topic><topic>Medical sciences</topic><topic>Micelles</topic><topic>Neoplasms - drug therapy</topic><topic>Pharmaceutical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Polyesters - chemistry</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Research Paper</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yang, Rulei</creatorcontrib><creatorcontrib>Zhang, Suai</creatorcontrib><creatorcontrib>Kong, Deling</creatorcontrib><creatorcontrib>Gao, Xuli</creatorcontrib><creatorcontrib>Zhao, Yanjun</creatorcontrib><creatorcontrib>Wang, Zheng</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>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>Biotechnology Research Abstracts</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yang, Rulei</au><au>Zhang, Suai</au><au>Kong, Deling</au><au>Gao, Xuli</au><au>Zhao, Yanjun</au><au>Wang, Zheng</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin</atitle><jtitle>Pharmaceutical research</jtitle><stitle>Pharm Res</stitle><addtitle>Pharm Res</addtitle><date>2012-12-01</date><risdate>2012</risdate><volume>29</volume><issue>12</issue><spage>3512</spage><epage>3525</epage><pages>3512-3525</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>ABSTRACT
Purpose
To utilize a novel type of polymer-drug conjugate micelle to enhance the delivery of low-potency curcumin.
Methods
Multiple curcumin molecules were conjugated to poly(lactic acid) (PLA) via tris(hydroxymethyl)aminomethane (Tris) linker producing the hydrophobic drug-binding block; methoxy-poly(ethylene glycol) (mPEG) was employed as the hydrophilic block. Micelles were characterized by size, loading capacity, stability, and critical micelle concentration (CMC). Human hepatocellular carcinoma (HepG2) cells were employed to assess cytotoxicity and intracellular targeting ability of micelles.
Results
mPEG-PLA-Tris-Cur micelles were within nanorange (<100 nm). CMC of such micelles (2.3 ± 0.4 μg/mL) was 10 times lower than mPEG-PLA micelles (27.4 ± 0.8 μg/mL). Curcumin loading in mPEG-PLA-Tris-Cur micelles reached 18.5 ± 1.3% (w/w), compared to traditional mPEG-PLA micelles at 3.6 ± 0.4% (w/w). IC
50
of mPEG-PLA-Tris-Cur micelles (~22 μg/mL at curcumin-equivalent dose) was similar to unmodified curcumin. Placebo and drug-encapsulated conjugate micelles could be efficiently internalized to cytoplasmic compartment of HepG2 cells.
Conclusions
Micelle-forming polymer-drug conjugates containing multiple drug molecules were an efficient means to increase loading and intracellular delivery of low-potency curcumin.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>22961588</pmid><doi>10.1007/s11095-012-0848-8</doi><tpages>14</tpages></addata></record> |
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| identifier | ISSN: 0724-8741 |
| ispartof | Pharmaceutical research, 2012-12, Vol.29 (12), p.3512-3525 |
| issn | 0724-8741 1573-904X |
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| subjects | Antineoplastic Agents - administration & dosage Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Biochemistry Biodegradable materials Biological and medical sciences Biomedical and Life Sciences Biomedical Engineering and Bioengineering Biomedicine Biopolymers Cell Survival - drug effects Curcumin - administration & dosage Curcumin - pharmacokinetics Curcumin - pharmacology Drug Carriers - chemistry Drug delivery systems General pharmacology Hep G2 Cells Humans Medical Law Medical sciences Micelles Neoplasms - drug therapy Pharmaceutical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Pharmacology/Toxicology Pharmacy Polyesters - chemistry Polyethylene Glycols - chemistry Research Paper |
| title | Biodegradable Polymer-Curcumin Conjugate Micelles Enhance the Loading and Delivery of Low-Potency Curcumin |
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