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• W2320798631 abstract "Gemcitabine (dFdC or Gem) is a water-soluble cytotoxic drug, with poor cellular uptake in the absence of a nucleoside transporter. To improve its diffusion through membranes, it was modified by grafting of a squalenoyl moiety. In water, this derivative is able to form stable and monodispersed nanoparticles made of inverse hexagonal phases. The formation and interfacial properties of the squalenoyl gemcitabine (SQ-Gem) nanoparticles, and their ability to interact with phospholipid and cholesterol monolayers modeling a biomembrane, was assessed from surface tension measurements and Brewster angle microscopy. To get a better insight into the mechanisms of SQ-Gem interaction with the various lipids, the interfacial behavior of SQ-Gem and squalene was also studied by surface pressure and surface potential measurements, in the absence and in the presence of phospholipids and cholesterol. The results showed that SQ-Gem nanoparticles adsorbed at the free air/water interface and disrupted to form a monolayer. SQ-Gem molecules released from the adsorbed nanoparticles were also able to penetrate into condensed phospholipid-cholesterol mixed monolayers. The kinetics of this penetration was apparently controlled by intermolecular interactions between the drug and the adsorbed lipids. Whereas distearoylphosphatidylcholine (DSPC) hindered SQ-Gem penetration, cholesterol favored it, which could have important implications in the therapeutic field since cholesterol targeting could alter lipid raft composition and cancer cell survival." @default.
• W2320798631 created "2016-06-24" @default.
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• W2320798631 date "2011-03-17" @default.
• W2320798631 modified "2023-10-04" @default.
• W2320798631 title "Interaction of Self-Assembled Squalenoyl Gemcitabine Nanoparticles with Phospholipid−Cholesterol Monolayers Mimicking a Biomembrane" @default.
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• W2320798631 doi "https://doi.org/10.1021/la200002d" @default.
• W2320798631 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21413743" @default.
• W2320798631 hasPublicationYear "2011" @default.
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