Nature as a source of inspiration for cationic lipid synthesis

Abstract

Synthetic gene delivery systems represent an attractive alternative to viral vectors for DNA transfection. Cationic lipids are one of the most widely used non-viral vectors for the delivery of DNA into cultured cells and are easily synthesized, leading to a large variety of well-characterized molecules. This review discusses strategies for the design of efficient cationic lipids that overcome the critical barriers of in vitro transfection. A particular focus is placed on natural hydrophilic headgroups and lipophilic tails that have been used to synthesize biocompatible and non-toxic cationic lipids. We also present chemical features that have been investigated to enhance the transfection efficiency of cationic lipids by promoting the escape of lipoplexes from the endosomal compartment and DNA release from DNA-liposome complexes. Transfection efficiency studies using these strategies are likely to improve the understanding of the mechanism of cationic lipid-mediated gene delivery and to help the rational design of novel cationic lipids.

Assessment of new biocompatible Poly(N-(morpholino)ethyl methacrylate)-based copolymers by transfection of immortalized keratinocytes

“…Various modifications have been attempted to further improve the transfection efficiency. Among those, modifications aiming at the enhancement of the endosomal escape of the polyplexes were reported (26). Indeed, the endosomal escape is necessary to avoid the lysosomal degradation of the DNA (27).…”

Delivering the goods: viral and non-viral gene therapy systems and the inherent limits on cargo DNA and internal sequences

“…Chemical transfection reagents are improving year-on-year and, under ideal conditions, now rival the efficiency of retrovirus vectors, achieving almost 100% efficiency for some types of cultured cells e.g. (Montier et al 2008;Labas et al 2010).…”

siRNA transfection by dendritic core–shell nanocarriers

“…[130,[143][144][145] Cationic lipid-based transfection reagents were first introduced by Felgner et al in 1987. [146] Since they are non immunogenic and can be easily prepared in large quantities, lipids are used as gene delivery agents.…”