Interaction of surfactant coated PLGA nanoparticles with in vitro human brain-like endothelial cells

[Display omitted] Treatment for CNS related diseases are limited by the difficulty of the drugs to cross the blood–brain barrier (BBB). The functionalization of polymeric nanoparticles (NPs) coated with the surfactants polysorbate 80 (PS80) and poloxamer 188 (P188), have shown promising results as d...

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Veröffentlicht in:International journal of pharmaceutics 2022-06, Vol.621, p.121780-121780, Article 121780
Hauptverfasser: Moya, Elisa L.J., Lombardo, Sonia M., Vandenhaute, Elodie, Schneider, Marc, Mysiorek, Caroline, Türeli, Akif E., Kanda, Takashi, Shimizu, Fumitaka, Sano, Yasuteru, Maubon, Nathalie, Gosselet, Fabien, Günday-Türeli, Nazende, Dehouck, Marie-Pierre
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container_title International journal of pharmaceutics
container_volume 621
creator Moya, Elisa L.J.
Lombardo, Sonia M.
Vandenhaute, Elodie
Schneider, Marc
Mysiorek, Caroline
Türeli, Akif E.
Kanda, Takashi
Shimizu, Fumitaka
Sano, Yasuteru
Maubon, Nathalie
Gosselet, Fabien
Günday-Türeli, Nazende
Dehouck, Marie-Pierre
description [Display omitted] Treatment for CNS related diseases are limited by the difficulty of the drugs to cross the blood–brain barrier (BBB). The functionalization of polymeric nanoparticles (NPs) coated with the surfactants polysorbate 80 (PS80) and poloxamer 188 (P188), have shown promising results as drugs carriers are able to cross the BBB on animal models. In this study, poly(lactide-co-glycolide) (PLGA) NPs coated with PS80 and P188, labelled with a fluorescent dye were tested on human pre-clinical in vitro model to evaluate and compare their uptake profiles, mechanisms of transport and crossing over human brain-like endothelial cells (BLECs) mimicking the human BBB. In addition, these NPs were produced using a method facilitating their reproducible production at high scale, the MicroJet reactor® technology. Results showed that both formulations were biocompatible and able to be internalized within the BLECs in different uptake profiles depending on their coating: P188 NP showed higher internalization capacity than PS80 NP. Both NPs uptakes were ATP-dependent, following more than one endocytosis pathway with colocalization in the early endosomes, ending with a NPs release in the brain compartment. Thus, both surfactant-coated PLGA NPs are interesting formulations for delivery to the brain through the BBB, presenting different uptake profiles.
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identifier ISSN: 0378-5173
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source Elsevier ScienceDirect Journals
subjects Animals
BBB in vitro models
Blood-Brain Barrier (BBB)
Blood-Brain Barrier / metabolism
Brain / metabolism
Drug Carriers / metabolism
Endothelial Cells / metabolism
Excipients / metabolism
Humans Nanoparticles
Life Sciences
Nanocarriers
Poloxamer / metabolism
Poloxamer 188
Poly(lactide-co-glycolide) nanoparticles
Polysorbate 80
Polysorbates Pulmonary Surfactants / metabolism
Surface-Active Agents / metabolism
title Interaction of surfactant coated PLGA nanoparticles with in vitro human brain-like endothelial cells
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