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231224s2011 xx |||||o 00| ||eng c |
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|a 10.1021/la200002d
|2 doi
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|a pubmed24n0689.xml
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|a (DE-627)NLM206725221
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|a (NLM)21413743
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|a DE-627
|b ger
|c DE-627
|e rakwb
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|a eng
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| 100 |
1 |
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|a Ambike, Anshuman
|e verfasserin
|4 aut
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| 245 |
1 |
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|a Interaction of self-assembled squalenoyl gemcitabine nanoparticles with phospholipid-cholesterol monolayers mimicking a biomembrane
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|c 2011
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|a Text
|b txt
|2 rdacontent
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|a ƒaComputermedien
|b c
|2 rdamedia
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|a ƒa Online-Ressource
|b cr
|2 rdacarrier
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|a Date Completed 26.08.2011
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|a Date Revised 07.12.2022
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|a published: Print-Electronic
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|a Citation Status MEDLINE
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|a © 2011 American Chemical Society
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|a 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
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|a Journal Article
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|a Research Support, Non-U.S. Gov't
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|a Membranes, Artificial
|2 NLM
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|a Phosphatidylcholines
|2 NLM
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|a Phospholipids
|2 NLM
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|a Deoxycytidine
|2 NLM
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|a 0W860991D6
|2 NLM
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|a Squalene
|2 NLM
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|a 7QWM220FJH
|2 NLM
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| 650 |
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|a Cholesterol
|2 NLM
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| 650 |
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|a 97C5T2UQ7J
|2 NLM
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| 650 |
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|a 1,2-distearoyllecithin
|2 NLM
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| 650 |
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|a EAG959U971
|2 NLM
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| 650 |
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|a Gemcitabine
|2 NLM
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| 700 |
1 |
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|a Rosilio, Véronique
|e verfasserin
|4 aut
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| 700 |
1 |
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|a Stella, Barbara
|e verfasserin
|4 aut
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| 700 |
1 |
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|a Lepêtre-Mouelhi, Sinda
|e verfasserin
|4 aut
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| 700 |
1 |
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|a Couvreur, Patrick
|e verfasserin
|4 aut
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| 773 |
0 |
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|i Enthalten in
|t Langmuir : the ACS journal of surfaces and colloids
|d 1992
|g 27(2011), 8 vom: 19. Apr., Seite 4891-9
|w (DE-627)NLM098181009
|x 1520-5827
|7 nnns
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| 773 |
1 |
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|g volume:27
|g year:2011
|g number:8
|g day:19
|g month:04
|g pages:4891-9
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|u http://dx.doi.org/10.1021/la200002d
|3 Volltext
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|h 4891-9
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