Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers

The disaccharide trehalose is an autophagy inducer, but its pharmacological application is severely limited by its poor pharmacokinetics properties. Thus, trehalose was coupled via suitable spacers with squalene (in 1:2 and 1:1 stoichiometry) and with betulinic acid (1:2 stoichiometry), in order to...

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Bibliographic Details
Published in:Pharmaceutics 2019-08, Vol.11 (8), p.422
Main Authors: Colombo, Eleonora, Biocotino, Michele, Frapporti, Giulia, Randazzo, Pietro, Christodoulou, Michael S, Piccoli, Giovanni, Polito, Laura, Seneci, Pierfausto, Passarella, Daniele
Format: Article
Language:English
Subjects:
Acids
Autophagy
autophagy induction
betulinic acid
Chromatography
Disease
nano-assemblies
Solvents
squalene
trehalose
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Summary:The disaccharide trehalose is an autophagy inducer, but its pharmacological application is severely limited by its poor pharmacokinetics properties. Thus, trehalose was coupled via suitable spacers with squalene (in 1:2 and 1:1 stoichiometry) and with betulinic acid (1:2 stoichiometry), in order to yield the corresponding nanolipid-trehalose conjugates , and . The conjugates were assembled to produce the corresponding nano-assemblies (NAs) , and . The synthetic and assembly protocols are described in detail. The resulting NAs were characterized in terms of loading and structure, and tested in vitro for their capability to induce autophagy. Our results are presented and thoroughly commented upon.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11080422