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Article Dans Une Revue Journal of Drug Delivery Science and Technology Année : 2021

Correlation between the composition of PLA-based folate targeted micelles and release of phosphonate derivative of betulin

Katarzyna Jelonek
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Bożena Kaczmarczyk
  • Fonction : Auteur
Arkadiusz Orchel
  • Fonction : Auteur
Ewa Chodurek
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Marzena Jaworska – Kik
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Piotr Paduszyński
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Ewa Bębenek
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Elwira Chrobak
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Monika Musiał-Kulik
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Aleksander Foryś
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Stanisław Boryczka
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Janusz Kasperczyk
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Résumé

There are increasing numbers of developed nanocarriers for anticancer drug delivery in the aim to avoid side effects of the conventional chemotherapy. Filomicelles with folic acid (FA) as a targeting moiety are a novel approach that can potentially maximize therapeutic efficacy while minimizing side effects. The aim of this study was to analyze the influence of composition of PLA-based micelles functionalized with folic acid on their drug encapsulation and release properties as well as cytotoxic activity against cancer cells. Micelles were obtained from combination of poly (L-lactide)-Jeffamine-folic acid (PLA-Jeff-FA) and poly (L-lactide)-poly (ethylene glycol) (PLA-PEG) or poly (L-lactide)-poly (ethylene glycol)-folic acid and PLA-PEG. E− 29-diethoxyphosphoryl-28-O-propynoylbetulin as an anticancer agent was encapsulated into micelles. The in vitro biocompatibility of drugfree micelles was confirmed as well as cytotoxicity of E− 29-diethoxyphosphoryl-28-O-propynoylbetulin loaded micelles against FR-positive SK-BR-3 cells. The micelles provided a release of an active agent for over 260 h. However, the micelles characterized differences in morphology, drug loading and release properties. The hydrophobic block length has been identified as a factor that may be used to control inter-and intramolecular interactions and, in consequence, micelle's properties, e.g. drug encapsulation efficiency and release rate.

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Chimie
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Dates et versions

hal-03369693 , version 1 (07-10-2021)

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Katarzyna Jelonek, Bożena Kaczmarczyk, Arkadiusz Orchel, Ewa Chodurek, Marzena Jaworska – Kik, et al.. Correlation between the composition of PLA-based folate targeted micelles and release of phosphonate derivative of betulin. Journal of Drug Delivery Science and Technology, 2021, 65, ⟨10.1016/j.jddst.2021.102717⟩. ⟨hal-03369693⟩
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