Methylated N-aryl chitosan derivative/DNA complex nanoparticles for gene delivery: Synthesis and structure–activity relationships

Biomedical Activity of Chitin/Chitosan Based Materials—Influence of Physicochemical Properties Apart from Molecular Weight and Degree of N-Acetylation

“…Apart from the influence of the chitosan concentration on its antimicrobial behavior, this parameter determines the properties of chitosan-based formulations for gene delivery systems [51,89,90]. It was established that the particle size of the chitosan/siRNA complex prepared by simple complexation increased when the concentration of chitosan was raised [51].…”

“…The comparative positive value of the surface charge (zeta potential) of chitosan-siRNA complexes also increased with the rising concentration of chitosan at a constant siRNA concentration. The transfection efficiency of the polyelectrolyte obtained depends on the mixing molar stoichiometry of DNA to chitosan (N/P ratio) [51,89,90]. Sajomsang et al reported that the highest gene transfection efficiencies of all N-aryl chitosan derivative/DNA complexes were observed at N/P ratios 5 due to the smallest particle size (95-124 nm) [89].…”

“…The transfection efficiency of the polyelectrolyte obtained depends on the mixing molar stoichiometry of DNA to chitosan (N/P ratio) [51,89,90]. Sajomsang et al reported that the highest gene transfection efficiencies of all N-aryl chitosan derivative/DNA complexes were observed at N/P ratios 5 due to the smallest particle size (95-124 nm) [89]. Zhu et al [91] investigated the aggregation behavior of O-carboxymethylchitosan in dilute solution to demonstrate its potential use in drug delivery systems.…”

“…Antimicrobial DQ ↑ at pH 7.2, no effect at acidic conditions [104] Adjuvanticity DQ no effect [106] Antithrombin DS ↑ [109] Acid-blinding capacity DS ↑ up to 25% [111] Immune enhancing effect pH < 4 or pH > 10 ↑ [76] Calcium/cobalt blinding capacity pH ↑ [82] Transfection efficiency C↓ [51,89,90] Gene knockdown efficiency C ↓ [90] ↑ directly proportion to property; ↓ inversely proportional to property…”

Influence of the Chemical Structure and Physicochemical Properties of Chitin- and Chitosan-Based Materials on Their Biomedical Activity

“…As a result the gene expression was improved in comparison with the chitosan-DNA complex both in vitro and in vivo. More recently, Sajomsang et al examined a methylated chitosan derivative/DNA complex containing different aromatic moieties (Sajomsang et al, 2009a). Of all the derivatives tested, N-(4-pyridinylmethyl) chitosan (MPyMeChX) exhibited the highest transfection efficiency in human hepatoma cells (Huh 7 cells).…”