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 1-Sq-mono, 2-Sq-bis and 3-Be-mono. The conjugates were assembled to produce the corresponding nano-assemblies (NAs) Sq-NA1, Sq-NA2 and Be-NA3. 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.
Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers / Colombo, Eleonora; Biocotino, Michele; Frapporti, Giulia; Randazzo, Pietro; Christodoulou, Michael S; Piccoli, Giovanni; Polito, Laura; Seneci, Pierfausto; Passarella, Daniele. - In: PHARMACEUTICS. - ISSN 1999-4923. - 11:8(2019), p. 422. [10.3390/pharmaceutics11080422]
Nanolipid-Trehalose Conjugates and Nano-Assemblies as Putative Autophagy Inducers
Frapporti, Giulia;Piccoli, Giovanni;Seneci, Pierfausto;
2019-01-01
Abstract
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 1-Sq-mono, 2-Sq-bis and 3-Be-mono. The conjugates were assembled to produce the corresponding nano-assemblies (NAs) Sq-NA1, Sq-NA2 and Be-NA3. 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione
