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Statements

Subject Item
n2:RIV%2F61389013%3A_____%2F13%3A00397906%21RIV14-MSM-61389013
rdf:type
skos:Concept n13:Vysledek
dcterms:description
In recent years, polymer drug carriers based on N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers with pH-triggered drug release have shown enhanced uptake in solid tumors and excellent antitumor activity. Here, the impact of the structure of the acid-labile spacer between the drug and the polymer carrier on the biodistribution of both the drug and the carrier was studied using in vivo noninvasive multispectral optical imaging of dual fluorescently labeled HPMAcopolymers. Five different spacers containing a pH-sensitive hydrazone bond were synthesized and used to combine a fluorescent model drug with a polymer backbone, conjugated with another non-releasable fluorescent dye. Two copolymers differing in polymer chain structure (linear and star-like) and molecular weight (30 and 200 kDa) were used to distinguish between carriers with molecular weights above and below the limit for renal filtration. The rate of model drug release from the conjugates was determined in vitro. The biodistributions of the six most promising conjugates were investigated in vivo in athymic nudemice inoculatedwith human colon carcinoma xenograft. The structure of the spacer in the vicinity of the hydrazone bond significantly influenced the release rate of the model drug. The slow release rate of a pyridyl group bearing spacer resulted in a greater amount of the model drug being transported to the tumor, whichwas independent of the carrier structure. The results of this study emphasize the importance of careful selection of the structure and appropriate spacer when designing polymer conjugates intended for passive tumor targeting. In recent years, polymer drug carriers based on N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers with pH-triggered drug release have shown enhanced uptake in solid tumors and excellent antitumor activity. Here, the impact of the structure of the acid-labile spacer between the drug and the polymer carrier on the biodistribution of both the drug and the carrier was studied using in vivo noninvasive multispectral optical imaging of dual fluorescently labeled HPMAcopolymers. Five different spacers containing a pH-sensitive hydrazone bond were synthesized and used to combine a fluorescent model drug with a polymer backbone, conjugated with another non-releasable fluorescent dye. Two copolymers differing in polymer chain structure (linear and star-like) and molecular weight (30 and 200 kDa) were used to distinguish between carriers with molecular weights above and below the limit for renal filtration. The rate of model drug release from the conjugates was determined in vitro. The biodistributions of the six most promising conjugates were investigated in vivo in athymic nudemice inoculatedwith human colon carcinoma xenograft. The structure of the spacer in the vicinity of the hydrazone bond significantly influenced the release rate of the model drug. The slow release rate of a pyridyl group bearing spacer resulted in a greater amount of the model drug being transported to the tumor, whichwas independent of the carrier structure. The results of this study emphasize the importance of careful selection of the structure and appropriate spacer when designing polymer conjugates intended for passive tumor targeting.
dcterms:title
Dual fluorescent HPMA copolymers for passive tumor targeting with pH-sensitive drug release II: impact of release rate on biodistribution Dual fluorescent HPMA copolymers for passive tumor targeting with pH-sensitive drug release II: impact of release rate on biodistribution
skos:prefLabel
Dual fluorescent HPMA copolymers for passive tumor targeting with pH-sensitive drug release II: impact of release rate on biodistribution Dual fluorescent HPMA copolymers for passive tumor targeting with pH-sensitive drug release II: impact of release rate on biodistribution
skos:notation
RIV/61389013:_____/13:00397906!RIV14-MSM-61389013
n13:predkladatel
n16:ico%3A61389013
n3:aktivita
n19:P n19:I
n3:aktivity
I, P(EE2.3.30.0029), P(GCP207/12/J030)
n3:cisloPeriodika
2
n3:dodaniDat
n15:2014
n3:domaciTvurceVysledku
n11:8890390 n11:9442286 n11:6390137 n11:9387501 n11:4763173
n3:druhVysledku
n5:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n14:predkladatel
n3:idSjednocenehoVysledku
70666
n3:idVysledku
RIV/61389013:_____/13:00397906
n3:jazykVysledku
n4:eng
n3:klicovaSlova
HPMA copolymers; pH-responsive drug release; tumor accumulation
n3:klicoveSlovo
n9:tumor%20accumulation n9:pH-responsive%20drug%20release n9:HPMA%20copolymers
n3:kodStatuVydavatele
NL - Nizozemsko
n3:kontrolniKodProRIV
[8FC423AA8E08]
n3:nazevZdroje
Journal of Controlled Release
n3:obor
n18:CD
n3:pocetDomacichTvurcuVysledku
5
n3:pocetTvurcuVysledku
9
n3:projekt
n10:GCP207%2F12%2FJ030 n10:EE2.3.30.0029
n3:rokUplatneniVysledku
n15:2013
n3:svazekPeriodika
172
n3:tvurceVysledku
Hoffmann, S. Kostka, Libor Mäder, K. Etrych, Tomáš Müller, T. Chytil, Petr Ulbrich, Karel Schindler, Lucie Caysa, H.
n3:wos
000327601700013
s:issn
0168-3659
s:numberOfPages
9
n6:doi
10.1016/j.jconrel.2013.05.008