The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
Identifieur interne : 000917 ( Main/Exploration ); précédent : 000916; suivant : 000918The controlled intravenous delivery of drugs using PEG-coated sterically stabilized nanospheres
Auteurs : R. Gref [France] ; A. Domb [Israël] ; P. Quellec [France] ; T. Blunk [Allemagne] ; R. H. Müller [Allemagne] ; J. M. Verbavatz [France] ; R. Langer [États-Unis]Source :
- Advanced drug delivery reviews [ 0169-409X ] ; 2012.
Descripteurs français
- Pascal (Inist)
- Wicri :
- topic : Médicament.
English descriptors
- KwdEn :
Abstract
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.
Affiliations:
- Allemagne, France, Israël, États-Unis
- Berlin, Grand Est, Lorraine (région), Massachusetts, Schleswig-Holstein, Île-de-France
- Berlin, Gif sur Yvette, Kiel, Nancy
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Le document en format XML
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Domb</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Department of Pharmaceutical Chemistry, Hebrew University</s1><s2>91120 Jerusalem</s2><s3>ISR</s3><sZ>2 aut.</sZ></inist:fA14><country>Israël</country><wicri:noRegion>91120 Jerusalem</wicri:noRegion></affiliation></author><author><name sortKey="Quellec, P" sort="Quellec, P" uniqKey="Quellec P" first="P." last="Quellec">P. Quellec</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451</s1><s2>54001 Nancy</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Grand Est</region><region type="old region" nuts="2">Lorraine (région)</region><settlement type="city">Nancy</settlement></placeName></affiliation></author><author><name sortKey="Blunk, T" sort="Blunk, T" uniqKey="Blunk T" first="T." last="Blunk">T. 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Gref</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451</s1><s2>54001 Nancy</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Grand Est</region><region type="old region" nuts="2">Lorraine (région)</region><settlement type="city">Nancy</settlement></placeName></affiliation></author><author><name sortKey="Domb, A" sort="Domb, A" uniqKey="Domb A" first="A." last="Domb">A. Domb</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Department of Pharmaceutical Chemistry, Hebrew University</s1><s2>91120 Jerusalem</s2><s3>ISR</s3><sZ>2 aut.</sZ></inist:fA14><country>Israël</country><wicri:noRegion>91120 Jerusalem</wicri:noRegion></affiliation></author><author><name sortKey="Quellec, P" sort="Quellec, P" uniqKey="Quellec P" first="P." last="Quellec">P. Quellec</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Laboratoire de Chimie-Physique Macromoléculaire, URA CNRS 494, ENSIC, 1, Rue Grandville, BP 451</s1><s2>54001 Nancy</s2><s3>FRA</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Grand Est</region><region type="old region" nuts="2">Lorraine (région)</region><settlement type="city">Nancy</settlement></placeName></affiliation></author><author><name sortKey="Blunk, T" sort="Blunk, T" uniqKey="Blunk T" first="T." last="Blunk">T. Blunk</name><affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Department of Pharmaceutics and Biopharmaceutics, Christian-Albrechts-University Kiel, Gutenbergstr, 76-78</s1><s2>24118 Kiel</s2><s3>DEU</s3><sZ>4 aut.</sZ></inist:fA14><country>Allemagne</country><placeName><region type="land" nuts="2">Schleswig-Holstein</region><settlement type="city">Kiel</settlement></placeName></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 wicri:level="3"><inist:fA14 i1="04"><s1>Department of Pharmaceutics, Biopharmaceutics and Biotechnology, Free University of Berlin, Kelchstr, 31</s1><s2>12169 Berlin</s2><s3>DEU</s3><sZ>5 aut.</sZ></inist:fA14><country>Allemagne</country><placeName><region type="land" nuts="3">Berlin</region><settlement type="city">Berlin</settlement></placeName></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 wicri:level="3"><inist:fA14 i1="05"><s1>Service de Biologie Cellulaire, CEA Saclay</s1><s2>91191 Gif sur Yvette</s2><s3>FRA</s3><sZ>6 aut.</sZ></inist:fA14><country>France</country><placeName><region type="region" nuts="2">Île-de-France</region><settlement type="city">Gif sur Yvette</settlement></placeName></affiliation></author><author><name sortKey="Langer, R" sort="Langer, R" uniqKey="Langer R" first="R." last="Langer">R. Langer</name><affiliation wicri:level="2"><inist:fA14 i1="06"><s1>Department of Chemical Engineering, MIT, E25-342, 45 Carlton St</s1><s2>Cambridge, MA 02139</s2><s3>USA</s3><sZ>7 aut.</sZ></inist:fA14><country>États-Unis</country><placeName><region type="state">Massachusetts</region></placeName></affiliation></author></analytic><series><title level="j" type="main">Advanced drug delivery reviews</title><title level="j" type="abbreviated">Adv. drug deliv. rev.</title><idno type="ISSN">0169-409X</idno><imprint><date when="2012">2012</date></imprint></series></biblStruct></sourceDesc><seriesStmt><title level="j" type="main">Advanced drug delivery reviews</title><title level="j" type="abbreviated">Adv. drug deliv. rev.</title><idno type="ISSN">0169-409X</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Coating</term><term>Coating material</term><term>Controlled release form</term><term>Cyclic ether polymer</term><term>Drug</term><term>Drug carrier</term><term>Ethylene oxide polymer</term><term>Hydrophily</term><term>Intravenous administration</term><term>Liver</term><term>Nanoparticle</term><term>Nanosphere</term><term>Pharmaceutical technology</term></keywords><keywords scheme="Pascal" xml:lang="fr"><term>Forme libération contrôlée</term><term>Voie intraveineuse</term><term>Vecteur médicament</term><term>Ethylène oxyde polymère</term><term>Nanosphère</term><term>Nanoparticule</term><term>Hydrophilie</term><term>Enrobage</term><term>Matériau revêtement</term><term>Foie</term><term>Médicament</term><term>Technologie pharmaceutique</term><term>Ether cyclique polymère</term><term>Polymère biodégradable</term></keywords><keywords scheme="Wicri" type="topic" xml:lang="fr"><term>Médicament</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">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.</div></front></TEI><affiliations><list><country><li>Allemagne</li><li>France</li><li>Israël</li><li>États-Unis</li></country><region><li>Berlin</li><li>Grand Est</li><li>Lorraine (région)</li><li>Massachusetts</li><li>Schleswig-Holstein</li><li>Île-de-France</li></region><settlement><li>Berlin</li><li>Gif sur Yvette</li><li>Kiel</li><li>Nancy</li></settlement></list><tree><country name="France"><region name="Grand Est"><name sortKey="Gref, R" sort="Gref, R" uniqKey="Gref R" first="R." last="Gref">R. Gref</name></region><name sortKey="Quellec, P" sort="Quellec, P" uniqKey="Quellec P" first="P." last="Quellec">P. Quellec</name><name sortKey="Verbavatz, J M" sort="Verbavatz, J M" uniqKey="Verbavatz J" first="J. M." last="Verbavatz">J. M. Verbavatz</name></country><country name="Israël"><noRegion><name sortKey="Domb, A" sort="Domb, A" uniqKey="Domb A" first="A." last="Domb">A. Domb</name></noRegion></country><country name="Allemagne"><region name="Schleswig-Holstein"><name sortKey="Blunk, T" sort="Blunk, T" uniqKey="Blunk T" first="T." last="Blunk">T. Blunk</name></region><name sortKey="Muller, R H" sort="Muller, R H" uniqKey="Muller R" first="R. H." last="Müller">R. H. Müller</name></country><country name="États-Unis"><region name="Massachusetts"><name sortKey="Langer, R" sort="Langer, R" uniqKey="Langer R" first="R." last="Langer">R. Langer</name></region></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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