Premature drug release of polymeric micelles and its effects on tumor targeting.
Identifieur interne : 000461 ( Main/Exploration ); précédent : 000460; suivant : 000462Premature drug release of polymeric micelles and its effects on tumor targeting.
Auteurs : RBID : pubmed:23384729English descriptors
- KwdEn :
- Animals, Cell Line, Tumor, Drug Carriers (chemistry), Female, Fenofibrate (administration & dosage), Fenofibrate (analogs & derivatives), Fenofibrate (chemistry), Fenofibrate (pharmacokinetics), Mice, Micelles, Neoplasms (drug therapy), Neoplasms (metabolism), Polyethylene Glycols (chemistry), Rats, Tissue Distribution.
- MESH :
- chemical , administration & dosage : Fenofibrate.
- chemical , analogs & derivatives : Fenofibrate.
- chemical , chemistry : Drug Carriers, Fenofibrate, Polyethylene Glycols.
- chemical , pharmacokinetics : Fenofibrate.
- drug therapy : Neoplasms.
- metabolism : Neoplasms.
- Animals, Cell Line, Tumor, Female, Mice, Micelles, Rats, Tissue Distribution.
Abstract
Based on the enhanced permeability and retention (EPR) effect, nanoparticles are believed to accumulate in tumors. In this conjunction, the stability of drug encapsulation is assumed to be sufficient. For clarification purposes, PEGylated poly-(D,L-lactic acid) (PEG-PDLLA) micelles which incorporated the hydrophobic model drug dechloro-4-iodo-fenofibrate (IFF) were investigated. H2N-PEG-PDLLA was synthesized, coupled to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and labeled with 111-indium. From this polymeric species, mixed micelles with H3CO-PEG-PDLLA were prepared which encapsulated the 125-iodine or 131-iodine labeled drug IFF. Bioimaging and biodistribution experiments in healthy and AR42J-tumor bearing mice were carried out to quantify the uptake of the drug and its carrier in single organs. As a result, upon injection of this system, a rapid dissociation of the polymeric carrier and the incorporated drug (<10 min post inj.) was revealed. Regardless of the premature release, the drug showed an enhanced tumor accumulation compared to the polymeric carrier. In conclusion, the self-assembling system allowed for successful solubilization of the hydrophobic drug by physical incorporation into micelles whereas the tumor targeting properties of the drug delivery system could not be sufficiently shown.
DOI: 10.1016/j.ijpharm.2013.01.059
PubMed: 23384729
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Premature drug release of polymeric micelles and its effects on tumor targeting.</title><author><name sortKey="Miller, Tobias" uniqKey="Miller T">Tobias Miller</name><affiliation wicri:level="3"><nlm:affiliation>Merck KGaA, Exploratory Pharmaceutical Development, Frankfurter Straße 250, 64293 Darmstadt, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>Merck KGaA, Exploratory Pharmaceutical Development, Frankfurter Straße 250, 64293 Darmstadt</wicri:regionArea><placeName><region type="land" nuts="1">Hesse (Land)</region><region type="district" nuts="2">District de Darmstadt</region><settlement type="city">Darmstadt</settlement></placeName></affiliation></author><author><name sortKey="Breyer, Sandra" uniqKey="Breyer S">Sandra Breyer</name></author><author><name sortKey="Van Colen, Gwenaelle" uniqKey="Van Colen G">Gwenaelle van Colen</name></author><author><name sortKey="Mier, Walter" uniqKey="Mier W">Walter Mier</name></author><author><name sortKey="Haberkorn, Uwe" uniqKey="Haberkorn U">Uwe Haberkorn</name></author><author><name sortKey="Geissler, Simon" uniqKey="Geissler S">Simon Geissler</name></author><author><name sortKey="Voss, Senta" uniqKey="Voss S">Senta Voss</name></author><author><name sortKey="Weigandt, Markus" uniqKey="Weigandt M">Markus Weigandt</name></author><author><name sortKey="Goepferich, Achim" uniqKey="Goepferich A">Achim Goepferich</name></author></titleStmt><publicationStmt><date when="2013">2013</date><idno type="doi">10.1016/j.ijpharm.2013.01.059</idno><idno type="RBID">pubmed:23384729</idno><idno type="pmid">23384729</idno><idno type="wicri:Area/Main/Corpus">000817</idno><idno type="wicri:Area/Main/Curation">000817</idno><idno type="wicri:Area/Main/Exploration">000461</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Drug Carriers (chemistry)</term><term>Female</term><term>Fenofibrate (administration & dosage)</term><term>Fenofibrate (analogs & derivatives)</term><term>Fenofibrate (chemistry)</term><term>Fenofibrate (pharmacokinetics)</term><term>Mice</term><term>Micelles</term><term>Neoplasms (drug therapy)</term><term>Neoplasms (metabolism)</term><term>Polyethylene Glycols (chemistry)</term><term>Rats</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" type="chemical" qualifier="administration & dosage" xml:lang="en"><term>Fenofibrate</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Fenofibrate</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Drug Carriers</term><term>Fenofibrate</term><term>Polyethylene Glycols</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Fenofibrate</term></keywords><keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Neoplasms</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Neoplasms</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Female</term><term>Mice</term><term>Micelles</term><term>Rats</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Based on the enhanced permeability and retention (EPR) effect, nanoparticles are believed to accumulate in tumors. In this conjunction, the stability of drug encapsulation is assumed to be sufficient. For clarification purposes, PEGylated poly-(D,L-lactic acid) (PEG-PDLLA) micelles which incorporated the hydrophobic model drug dechloro-4-iodo-fenofibrate (IFF) were investigated. H2N-PEG-PDLLA was synthesized, coupled to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and labeled with 111-indium. From this polymeric species, mixed micelles with H3CO-PEG-PDLLA were prepared which encapsulated the 125-iodine or 131-iodine labeled drug IFF. Bioimaging and biodistribution experiments in healthy and AR42J-tumor bearing mice were carried out to quantify the uptake of the drug and its carrier in single organs. As a result, upon injection of this system, a rapid dissociation of the polymeric carrier and the incorporated drug (<10 min post inj.) was revealed. Regardless of the premature release, the drug showed an enhanced tumor accumulation compared to the polymeric carrier. In conclusion, the self-assembling system allowed for successful solubilization of the hydrophobic drug by physical incorporation into micelles whereas the tumor targeting properties of the drug delivery system could not be sufficiently shown.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">23384729</PMID><DateCreated><Year>2013</Year><Month>03</Month><Day>13</Day></DateCreated><DateCompleted><Year>2013</Year><Month>08</Month><Day>30</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1873-3476</ISSN><JournalIssue CitedMedium="Internet"><Volume>445</Volume><Issue>1-2</Issue><PubDate><Year>2013</Year><Month>Mar</Month><Day>10</Day></PubDate></JournalIssue><Title>International journal of pharmaceutics</Title><ISOAbbreviation>Int J Pharm</ISOAbbreviation></Journal><ArticleTitle>Premature drug release of polymeric micelles and its effects on tumor targeting.</ArticleTitle><Pagination><MedlinePgn>117-24</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1016/j.ijpharm.2013.01.059</ELocationID><ELocationID EIdType="pii" ValidYN="Y">S0378-5173(13)00110-5</ELocationID><Abstract><AbstractText>Based on the enhanced permeability and retention (EPR) effect, nanoparticles are believed to accumulate in tumors. In this conjunction, the stability of drug encapsulation is assumed to be sufficient. For clarification purposes, PEGylated poly-(D,L-lactic acid) (PEG-PDLLA) micelles which incorporated the hydrophobic model drug dechloro-4-iodo-fenofibrate (IFF) were investigated. H2N-PEG-PDLLA was synthesized, coupled to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and labeled with 111-indium. From this polymeric species, mixed micelles with H3CO-PEG-PDLLA were prepared which encapsulated the 125-iodine or 131-iodine labeled drug IFF. Bioimaging and biodistribution experiments in healthy and AR42J-tumor bearing mice were carried out to quantify the uptake of the drug and its carrier in single organs. As a result, upon injection of this system, a rapid dissociation of the polymeric carrier and the incorporated drug (<10 min post inj.) was revealed. Regardless of the premature release, the drug showed an enhanced tumor accumulation compared to the polymeric carrier. In conclusion, the self-assembling system allowed for successful solubilization of the hydrophobic drug by physical incorporation into micelles whereas the tumor targeting properties of the drug delivery system could not be sufficiently shown.</AbstractText><CopyrightInformation>Copyright © 2013 Elsevier B.V. All rights reserved.</CopyrightInformation></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Miller</LastName><ForeName>Tobias</ForeName><Initials>T</Initials><Affiliation>Merck KGaA, Exploratory Pharmaceutical Development, Frankfurter Straße 250, 64293 Darmstadt, Germany.</Affiliation></Author><Author ValidYN="Y"><LastName>Breyer</LastName><ForeName>Sandra</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>van Colen</LastName><ForeName>Gwenaelle</ForeName><Initials>G</Initials></Author><Author ValidYN="Y"><LastName>Mier</LastName><ForeName>Walter</ForeName><Initials>W</Initials></Author><Author ValidYN="Y"><LastName>Haberkorn</LastName><ForeName>Uwe</ForeName><Initials>U</Initials></Author><Author ValidYN="Y"><LastName>Geissler</LastName><ForeName>Simon</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Voss</LastName><ForeName>Senta</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Weigandt</LastName><ForeName>Markus</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Goepferich</LastName><ForeName>Achim</ForeName><Initials>A</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2013</Year><Month>02</Month><Day>04</Day></ArticleDate></Article><MedlineJournalInfo><Country>Netherlands</Country><MedlineTA>Int J Pharm</MedlineTA><NlmUniqueID>7804127</NlmUniqueID><ISSNLinking>0378-5173</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Drug Carriers</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Micelles</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Polyethylene Glycols</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>monomethoxypolyethyleneglycol-polylactide block copolymer</NameOfSubstance></Chemical><Chemical><RegistryNumber>U202363UOS</RegistryNumber><NameOfSubstance>Fenofibrate</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Carriers</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Fenofibrate</DescriptorName><QualifierName MajorTopicYN="N">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Micelles</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasms</DescriptorName><QualifierName MajorTopicYN="N">drug therapy</QualifierName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Polyethylene Glycols</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2012</Year><Month>11</Month><Day>16</Day></PubMedPubDate><PubMedPubDate PubStatus="revised"><Year>2013</Year><Month>1</Month><Day>18</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2013</Year><Month>1</Month><Day>21</Day></PubMedPubDate><PubMedPubDate PubStatus="aheadofprint"><Year>2013</Year><Month>2</Month><Day>4</Day></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2013</Year><Month>2</Month><Day>7</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2013</Year><Month>2</Month><Day>7</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2013</Year><Month>8</Month><Day>31</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">S0378-5173(13)00110-5</ArticleId><ArticleId IdType="doi">10.1016/j.ijpharm.2013.01.059</ArticleId><ArticleId IdType="pubmed">23384729</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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