About: Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin     Goto   Sponge   NotDistinct   Permalink

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  • A physically entrapped anticancer drug (paclitaxel) was previously shown to be rapidly eliminated from the circulation, likely because the drug was insufficiently retained in the micelles. To fully exploit the EPR effect for drug targeting, a DOX methacrylamide derivative (DOX-MA) was covalently incorporated into the micellar core by free radical polymerization. The structure of the doxorubicin derivative is susceptible to pH-sensitive hydrolysis, enabling controlled release of the drug in acidic conditions (in either the intratumoral environment and/or the endosomal vesicles). The entire drug payload was released within 24 h incubation at pH 5 and 37 °C, whereas only around 5% release was observed at pH 7.4. DOX micelles showed higher cytotoxicity in B16F10 and OVCAR-3 cells compared to DOX-MA, likely due to cellular uptake of the micelles via endocytosis and intracellular drug release in the acidic organelles.
  • A physically entrapped anticancer drug (paclitaxel) was previously shown to be rapidly eliminated from the circulation, likely because the drug was insufficiently retained in the micelles. To fully exploit the EPR effect for drug targeting, a DOX methacrylamide derivative (DOX-MA) was covalently incorporated into the micellar core by free radical polymerization. The structure of the doxorubicin derivative is susceptible to pH-sensitive hydrolysis, enabling controlled release of the drug in acidic conditions (in either the intratumoral environment and/or the endosomal vesicles). The entire drug payload was released within 24 h incubation at pH 5 and 37 °C, whereas only around 5% release was observed at pH 7.4. DOX micelles showed higher cytotoxicity in B16F10 and OVCAR-3 cells compared to DOX-MA, likely due to cellular uptake of the micelles via endocytosis and intracellular drug release in the acidic organelles. (en)
Title
  • Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin
  • Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin (en)
skos:prefLabel
  • Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin
  • Core-crosslinked polymeric micelles with controlled release of covalently entrapped doxorubicin (en)
skos:notation
  • RIV/61389013:_____/10:00346588!RIV11-AV0-61389013
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(IAA400500806), P(KAN200200651), Z(AV0Z40500505)
http://linked.open...iv/cisloPeriodika
  • 30
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 252167
http://linked.open...ai/riv/idVysledku
  • RIV/61389013:_____/10:00346588
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • doxorubicin; cancer therapy; polymeric micelle (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [3FAA5BDC8344]
http://linked.open...i/riv/nazevZdroje
  • Biomaterials
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 31
http://linked.open...iv/tvurceVysledku
  • Etrych, Tomáš
  • Ulbrich, Karel
  • Lammers, T.
  • Storm, G.
  • Hennink, W. E.
  • Rijcken, C. J. F.
  • Talelli, M.
  • Iman, M.
  • Schiffelers, R. M.
  • Varkouhi, A. K.
  • van Nostrum, C. F.
http://linked.open...ain/vavai/riv/wos
  • 000281498600021
http://linked.open...n/vavai/riv/zamer
issn
  • 0142-9612
number of pages
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