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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres<sup><xref ref-type="fn" rid="FN2">☆</xref></sup></title><author><name sortKey="Gref, R" sort="Gref, R" uniqKey="Gref R" first="R." last="Gref">R. Gref</name><affiliation><nlm:aff id="A1">Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451, 54001 Nancy Cedex, France</nlm:aff></affiliation></author><author><name sortKey="Domb, A" sort="Domb, A" uniqKey="Domb A" first="A." last="Domb">A. Domb</name><affiliation><nlm:aff id="A2">Department of Pharmaceutical Chemistry, Hebrew University, 91120 Jerusalem, Israel</nlm:aff></affiliation></author><author><name sortKey="Quellec, P" sort="Quellec, P" uniqKey="Quellec P" first="P." last="Quellec">P. Quellec</name><affiliation><nlm:aff id="A1">Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451, 54001 Nancy Cedex, France</nlm:aff></affiliation></author><author><name sortKey="Blunk, T" sort="Blunk, T" uniqKey="Blunk T" first="T." last="Blunk">T. Blunk</name><affiliation><nlm:aff id="A3">Department of Pharmaceutics and Biopharmaceutics, Christian-Albrechts-University Kiel, Gutenbergstr, 76–78, 24118 Kiel, Germany</nlm:aff></affiliation></author><author><name sortKey="Muller, R H" sort="Muller, R H" uniqKey="Muller R" first="R. H." last="Müller">R. H. Müller</name><affiliation><nlm:aff id="A4">Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Kelchstr, 31, 12169 Berlin, Germany</nlm:aff></affiliation></author><author><name sortKey="Verbavatz, J M" sort="Verbavatz, J M" uniqKey="Verbavatz J" first="J. M." last="Verbavatz">J. M. Verbavatz</name><affiliation><nlm:aff id="A5">Service de Biologie Cellulaire, CEA Saclay, 91191 Gif sur Yvette, France</nlm:aff></affiliation></author><author><name sortKey="Langer, R" sort="Langer, R" uniqKey="Langer R" first="R." last="Langer">R. Langer</name><affiliation><nlm:aff id="A6">Department of Chemical Engineering, MIT, E25-342, 45 Carlton St., Cambridge, MA 02139, USA</nlm:aff></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">25170183</idno><idno type="pmc">4144462</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4144462</idno><idno type="RBID">PMC:4144462</idno><idno type="doi">10.1016/0169-409X(95)00026-4</idno><date when="1995">1995</date><idno type="wicri:Area/Pmc/Corpus">000157</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000157</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres<sup><xref ref-type="fn" rid="FN2">☆</xref></sup></title><author><name sortKey="Gref, R" sort="Gref, R" uniqKey="Gref R" first="R." last="Gref">R. Gref</name><affiliation><nlm:aff id="A1">Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451, 54001 Nancy Cedex, France</nlm:aff></affiliation></author><author><name sortKey="Domb, A" sort="Domb, A" uniqKey="Domb A" first="A." last="Domb">A. Domb</name><affiliation><nlm:aff id="A2">Department of Pharmaceutical Chemistry, Hebrew University, 91120 Jerusalem, Israel</nlm:aff></affiliation></author><author><name sortKey="Quellec, P" sort="Quellec, P" uniqKey="Quellec P" first="P." last="Quellec">P. Quellec</name><affiliation><nlm:aff id="A1">Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451, 54001 Nancy Cedex, France</nlm:aff></affiliation></author><author><name sortKey="Blunk, T" sort="Blunk, T" uniqKey="Blunk T" first="T." last="Blunk">T. Blunk</name><affiliation><nlm:aff id="A3">Department of Pharmaceutics and Biopharmaceutics, Christian-Albrechts-University Kiel, Gutenbergstr, 76–78, 24118 Kiel, Germany</nlm:aff></affiliation></author><author><name sortKey="Muller, R H" sort="Muller, R H" uniqKey="Muller R" first="R. H." last="Müller">R. H. Müller</name><affiliation><nlm:aff id="A4">Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Kelchstr, 31, 12169 Berlin, Germany</nlm:aff></affiliation></author><author><name sortKey="Verbavatz, J M" sort="Verbavatz, J M" uniqKey="Verbavatz J" first="J. M." last="Verbavatz">J. M. Verbavatz</name><affiliation><nlm:aff id="A5">Service de Biologie Cellulaire, CEA Saclay, 91191 Gif sur Yvette, France</nlm:aff></affiliation></author><author><name sortKey="Langer, R" sort="Langer, R" uniqKey="Langer R" first="R." last="Langer">R. Langer</name><affiliation><nlm:aff id="A6">Department of Chemical Engineering, MIT, E25-342, 45 Carlton St., Cambridge, MA 02139, USA</nlm:aff></affiliation></author></analytic><series><title level="j">Advanced drug delivery reviews</title><idno type="ISSN">0169-409X</idno><idno type="eISSN">1872-8294</idno><imprint><date when="1995">1995</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><p id="P1">Injectable blood persistent particulate carriers have important therapeutic application in site-specific drug delivery or medical imaging. However, injected particles are generally eliminated by the reticuloendothelial system within minutes after administration and accumulate in the liver and spleen. To obtain a coating that might prevent opsonization and subsequent recognition by the macrophages, sterically stabilized nanospheres were developed using amphiphilic diblock or multiblock copolymers. The nanospheres are composed of a hydrophilic polyethylene glycol coating and a biodegradable core in which various drugs were encapsulated. Hydrophobic drugs, such as lidocaine, were entrapped up to 45 wt% and the release kinetics were governed by the polymer physico-chemical characteristics. Plasma protein adsorption was drastically reduced on PEG-coated particles compared to non-coated ones. Relative protein amounts were time-dependent. The nanospheres exhibited increased blood circulation times and reduced liver accumulation, depending on the coating polyethylene glycol molecular weight and surface density. They could be freeze-dried and redispersed in aqueous solutions and possess good shelf stability. It may be possible to tailor “optimal” polymers for given therapeutic applications.</p></div></front></TEI><pmc article-type="research-article"><pmc-comment>The publisher of this article does not allow downloading of the full text in XML form.</pmc-comment>
<pmc-dir>properties manuscript</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-journal-id">8710523</journal-id><journal-id journal-id-type="pubmed-jr-id">21484</journal-id><journal-id journal-id-type="nlm-ta">Adv Drug Deliv Rev</journal-id><journal-id journal-id-type="iso-abbrev">Adv. Drug Deliv. Rev.</journal-id><journal-title-group><journal-title>Advanced drug delivery reviews</journal-title></journal-title-group><issn pub-type="ppub">0169-409X</issn><issn pub-type="epub">1872-8294</issn></journal-meta><article-meta><article-id pub-id-type="pmid">25170183</article-id><article-id pub-id-type="pmc">4144462</article-id><article-id pub-id-type="doi">10.1016/0169-409X(95)00026-4</article-id><article-id pub-id-type="manuscript">NIHMS582980</article-id><article-categories><subj-group subj-group-type="heading"><subject>Article</subject></subj-group></article-categories><title-group><article-title>The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres<sup><xref ref-type="fn" rid="FN2">☆</xref></sup></article-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>Gref</surname><given-names>R.</given-names></name><xref ref-type="aff" rid="A1">a</xref><xref rid="FN1" ref-type="author-notes">*</xref></contrib><contrib contrib-type="author"><name><surname>Domb</surname><given-names>A.</given-names></name><xref ref-type="aff" rid="A2">b</xref></contrib><contrib contrib-type="author"><name><surname>Quellec</surname><given-names>P.</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Blunk</surname><given-names>T.</given-names></name><xref ref-type="aff" rid="A3">c</xref></contrib><contrib contrib-type="author"><name><surname>Müller</surname><given-names>R.H.</given-names></name><xref ref-type="aff" rid="A4">d</xref></contrib><contrib contrib-type="author"><name><surname>Verbavatz</surname><given-names>J.M.</given-names></name><xref ref-type="aff" rid="A5">e</xref></contrib><contrib contrib-type="author"><name><surname>Langer</surname><given-names>R.</given-names></name><xref ref-type="aff" rid="A6">f</xref></contrib></contrib-group><aff id="A1"><label>a</label>Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451, 54001 Nancy Cedex, France</aff><aff id="A2"><label>b</label>Department of Pharmaceutical Chemistry, Hebrew University, 91120 Jerusalem, Israel</aff><aff id="A3"><label>c</label>Department of Pharmaceutics and Biopharmaceutics, Christian-Albrechts-University Kiel, Gutenbergstr, 76–78, 24118 Kiel, Germany</aff><aff id="A4"><label>d</label>Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Kelchstr, 31, 12169 Berlin, Germany</aff><aff id="A5"><label>e</label>Service de Biologie Cellulaire, CEA Saclay, 91191 Gif sur Yvette, France</aff><aff id="A6"><label>f</label>Department of Chemical Engineering, MIT, E25-342, 45 Carlton St., Cambridge, MA 02139, USA</aff><author-notes><corresp id="FN1"><label>*</label>Corresponding author. Tel.: +33 83175261; fax: +33 83379977. <email>Ruxandra.Gref@cep.u-psud.fr</email> (R. Gref)</corresp></author-notes><pub-date pub-type="nihms-submitted"><day>11</day><month>5</month><year>2014</year></pub-date><pub-date pub-type="ppub"><month>9</month><year>1995</year></pub-date><pub-date pub-type="pmc-release"><day>26</day><month>8</month><year>2014</year></pub-date><volume>16</volume><issue>2-3</issue><fpage>215</fpage><lpage>233</lpage><pmc-comment>elocation-id from pubmed: 10.1016/0169-409X(95)00026-4</pmc-comment>
<permissions><copyright-statement>© 2012 Published by Elsevier B.V.</copyright-statement><copyright-year>2012</copyright-year></permissions><abstract><p id="P1">Injectable blood persistent particulate carriers have important therapeutic application in site-specific drug delivery or medical imaging. However, injected particles are generally eliminated by the reticuloendothelial system within minutes after administration and accumulate in the liver and spleen. To obtain a coating that might prevent opsonization and subsequent recognition by the macrophages, sterically stabilized nanospheres were developed using amphiphilic diblock or multiblock copolymers. The nanospheres are composed of a hydrophilic polyethylene glycol coating and a biodegradable core in which various drugs were encapsulated. Hydrophobic drugs, such as lidocaine, were entrapped up to 45 wt% and the release kinetics were governed by the polymer physico-chemical characteristics. Plasma protein adsorption was drastically reduced on PEG-coated particles compared to non-coated ones. Relative protein amounts were time-dependent. The nanospheres exhibited increased blood circulation times and reduced liver accumulation, depending on the coating polyethylene glycol molecular weight and surface density. They could be freeze-dried and redispersed in aqueous solutions and possess good shelf stability. It may be possible to tailor “optimal” polymers for given therapeutic applications.</p></abstract><kwd-group><kwd>Long-circulating nanoparticles</kwd><kwd>Biodegradable polymers</kwd><kwd>Polyethylene glycol</kwd><kwd>Hydrophilic coating</kwd><kwd>Reduced liver accumulation</kwd><kwd>Intravenous drug administration</kwd></kwd-group></article-meta></front></pmc></record>Pour manipuler ce document sous Unix (Dilib)
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