Abstract
In this study a multifunctional carrier (MFC), 1,4,7-triazanonylimino-bis[ N-(oleicyl-cysteinyl-histinyl)-1-aminoethyl)propionamide] (THCO), containing protonatable amines of different p K as, polymerizable cysteine residues and hydrophobic groups, was designed, synthesized and evaluated for efficient small interfering RNAs (siRNA) delivery. THCO showed pH-sensitive cellular membrane disruption at the endosomal–lysosomal pH to facilitate intracellular siRNA delivery. THCO formed stable and compact nanoparticles with siRNA through charge complexation, hydrophobic condensation and reversible polymerization. The THCO/siRNA nanoparticles were readily modified with PEG-Mal by reacting with remaining thiol groups at the surface. The siRNA delivery efficiency of THCO was comparable to that of Transfast™, much higher than that of N-(2,3-dioleoyloxy-1-propyl)trimethylammonium methyl sulphate (DOTAP) in serum-free medium. PEGylated THCO/siRNA nanoparticles resulted in higher transfection efficiency than those of Transfast™ and DOTAP in the presence of serum. This study demonstrated that the MFC-THCO is promising for efficient siRNA delivery.
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