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CHAPTER 11
Multicompartment Lipid Nanocarriers
for Targeting of Cells Expressing
Brain Receptors
CLAIRE GÉRAL, ANGELINA ANGELOVA, and SYLVIANE LESIEUR
CNRS, University of Paris Sud, Châtenay-Malabry, France
BORISLAV ANGELOV
Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic,
Prague, Czech Republic
VALÉRIE NICOLAS
Cell Imaging Platform, University of Paris Sud, Châtenay-Malabry, France
Abstract
Neurotrophic factors, such as the brain-derived neurotrophic factor (BDNF), are essen-
tial for the development and survival of human neurons. Their encapsulation in carrier
lipid systems is anticipated to overcome the problems resulting from the pharmacoki-
netics of peptides in the cerebral circulation. Lipid nanocarriers containing an omega-3
polyunsaturated fatty acid [eicosapentaenoic acid] (EPA), showing neuroprotective
effects, should trigger the BDNF activity. The purpose of this study is to design and
characterize self-assembled lipid systems suitable for encapsulation and potentiation
of neurotrophic peptide activity and study of multicompartment liquid crystalline
formulations in vitro on a human neuronal cell line expressing BDNF receptors. Steri-
cally stabilized nanodispersed lipid systems are prepared from a PEGylated (polyeth-
ylene glycol) liquid crystalline phase in excess water. Such lipid nanovectors, derived
by self-assembly, are of ongoing interest thanks to their biocompatible compositions
and the relatively low energy input required for their manufacture. The latter is an
essential factor for the encapsulation of fragile and temperature-sensitive peptide
molecules. Having induced the differentiation of a human neuroblastoma cell line SH-
SY5Y, as a model of neurodegeneration, we examine in vitro the expression of the
TrkB brain receptor of neurotrophins and the cytotoxicity of the designed multicom-
partment lipid nanocarriers to neuronal cells.
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