Influence of dendrimer generation and polyethylene glycol length on the biodistribution of PEGylated dendrimers
Identifieur interne : 003E94 ( Main/Repository ); précédent : 003E93; suivant : 003E95Influence of dendrimer generation and polyethylene glycol length on the biodistribution of PEGylated dendrimers
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Abstract
Dendrimers are a potential drug carrier. Because modification with polyethylene glycol (PEG) is known to improve the blood retention, PEGylated dendrimers have been studied as a useful drug carrier. In this study, three types of PEGylated L-lysine-bearing polyamidoamine dendrimers (PEG2k-Lys-PAMAM (G4), PEG5k-Lys-PAMAM (G4), PEG2k-Lys-PAMAM (G5)) were synthesized, which are composed of a dendrimer of different generations (generations 4 and 5) and PEG chains with different molecular weights (2k and 5k). An acetylated L-lysine-bearing dendrimer was also synthesized as a non-PEGylated dendrimer. Bifunctional diethylenetriaminepentaacetic acid (pSCN-benzyl-DTPA) was bound to the epsilon -amino group of lysine in a dendrimer, to be labeled with radioactive indium-111. These PEGylayed dendrimers showed longer blood retention and lower accumulation in other normal organs such as the kidneys than the non-PEGylated dendrimer. The PEGylated dendrimers with the higher generation and the longer PEG led the greater blood retention.
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en" level="a">Influence of dendrimer generation and polyethylene glycol length on the biodistribution of PEGylated dendrimers</title><author><name sortKey="Kojima, Chie" uniqKey="Kojima C">Chie Kojima</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University</s1><s2>Osaka</s2><s3>JPN</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ><sZ>5 aut.</sZ></inist:fA14><country>Japon</country><wicri:noRegion>Osaka</wicri:noRegion></affiliation></author><author><name sortKey="Regino, Celeste" uniqKey="Regino C">Celeste Regino</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Molecular Imaging Program, Center for Cancer Research, National Cancer Institute, NIH</s1><s2>MD</s2><s3>USA</s3><sZ>2 aut.</sZ><sZ>4 aut.</sZ></inist:fA14><country>États-Unis</country><placeName><region type="state">Maryland</region></placeName></affiliation></author><author><name sortKey="Umeda, Yasuhito" uniqKey="Umeda Y">Yasuhito Umeda</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University</s1><s2>Osaka</s2><s3>JPN</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ><sZ>5 aut.</sZ></inist:fA14><country>Japon</country><wicri:noRegion>Osaka</wicri:noRegion></affiliation></author><author><name sortKey="Kobayashi, Hisataka" uniqKey="Kobayashi H">Hisataka Kobayashi</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Molecular Imaging Program, Center for Cancer Research, National Cancer Institute, NIH</s1><s2>MD</s2><s3>USA</s3><sZ>2 aut.</sZ><sZ>4 aut.</sZ></inist:fA14><country>États-Unis</country><placeName><region type="state">Maryland</region></placeName></affiliation></author><author><name sortKey="Kono, Kenji" uniqKey="Kono K">Kenji Kono</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University</s1><s2>Osaka</s2><s3>JPN</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ><sZ>5 aut.</sZ></inist:fA14><country>Japon</country><wicri:noRegion>Osaka</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="inist">10-0065091</idno><date when="2010">2010</date><idno type="stanalyst">PASCAL 10-0065091 INIST</idno><idno type="RBID">Pascal:10-0065091</idno><idno type="wicri:Area/Main/Corpus">004A91</idno><idno type="wicri:Area/Main/Repository">003E94</idno></publicationStmt><seriesStmt><idno type="ISSN">0378-5173</idno><title level="j" type="abbreviated">Int. j. pharm.</title><title level="j" type="main">International journal of pharmaceutics</title></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Dendrimer</term><term>Dendritic structure</term><term>Distribution</term><term>Drug</term><term>Drug carrier</term><term>Ethylene oxide polymer</term><term>Pegylated form</term><term>Pharmaceutical technology</term></keywords><keywords scheme="Pascal" xml:lang="fr"><term>Ethylène oxyde polymère</term><term>Distribution</term><term>Forme pégylée</term><term>Médicament</term><term>Vecteur médicament</term><term>Technologie pharmaceutique</term><term>Structure dendritique</term><term>Dendrimère</term></keywords><keywords scheme="Wicri" type="concept" xml:lang="fr"><term>Médicament</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Dendrimers are a potential drug carrier. Because modification with polyethylene glycol (PEG) is known to improve the blood retention, PEGylated dendrimers have been studied as a useful drug carrier. In this study, three types of PEGylated L-lysine-bearing polyamidoamine dendrimers (PEG2k-Lys-PAMAM (G4), PEG5k-Lys-PAMAM (G4), PEG2k-Lys-PAMAM (G5)) were synthesized, which are composed of a dendrimer of different generations (generations 4 and 5) and PEG chains with different molecular weights (2k and 5k). An acetylated L-lysine-bearing dendrimer was also synthesized as a non-PEGylated dendrimer. Bifunctional diethylenetriaminepentaacetic acid (pSCN-benzyl-DTPA) was bound to the epsilon -amino group of lysine in a dendrimer, to be labeled with radioactive indium-111. These PEGylayed dendrimers showed longer blood retention and lower accumulation in other normal organs such as the kidneys than the non-PEGylated dendrimer. The PEGylated dendrimers with the higher generation and the longer PEG led the greater blood retention.</div></front></TEI><inist><standard h6="B"><pA><fA01 i1="01" i2="1"><s0>0378-5173</s0></fA01><fA02 i1="01"><s0>IJPHDE</s0></fA02><fA03 i2="1"><s0>Int. j. pharm.</s0></fA03><fA05><s2>383</s2></fA05><fA06><s2>1-2</s2></fA06><fA08 i1="01" i2="1" l="ENG"><s1>Influence of dendrimer generation and polyethylene glycol length on the biodistribution of PEGylated dendrimers</s1></fA08><fA11 i1="01" i2="1"><s1>KOJIMA (Chie)</s1></fA11><fA11 i1="02" i2="1"><s1>REGINO (Celeste)</s1></fA11><fA11 i1="03" i2="1"><s1>UMEDA (Yasuhito)</s1></fA11><fA11 i1="04" i2="1"><s1>KOBAYASHI (Hisataka)</s1></fA11><fA11 i1="05" i2="1"><s1>KONO (Kenji)</s1></fA11><fA14 i1="01"><s1>Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University</s1><s2>Osaka</s2><s3>JPN</s3><sZ>1 aut.</sZ><sZ>3 aut.</sZ><sZ>5 aut.</sZ></fA14><fA14 i1="02"><s1>Molecular Imaging Program, Center for Cancer Research, National Cancer Institute, NIH</s1><s2>MD</s2><s3>USA</s3><sZ>2 aut.</sZ><sZ>4 aut.</sZ></fA14><fA20><s1>293-296</s1></fA20><fA21><s1>2010</s1></fA21><fA23 i1="01"><s0>ENG</s0></fA23><fA43 i1="01"><s1>INIST</s1><s2>16510</s2><s5>354000189944010390</s5></fA43><fA44><s0>0000</s0><s1>© 2010 INIST-CNRS. 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Bifunctional diethylenetriaminepentaacetic acid (pSCN-benzyl-DTPA) was bound to the epsilon -amino group of lysine in a dendrimer, to be labeled with radioactive indium-111. These PEGylayed dendrimers showed longer blood retention and lower accumulation in other normal organs such as the kidneys than the non-PEGylated dendrimer. 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