Cerasome as an infusible, cell-friendly, and serum-compatible transfection agent in a viral size.

Abstract

Alanine-based cationic lipid 1 having a (EtO)3SiCH2CH2CH2 group on the quaternized ammonium nitrogen forms a liposome which self-rigidifies via in situ sol-gel processes (Si-OEt + H2O --> Si-OH + EtOH followed by 2Si-OH --> Si-O-Si + H2O) on the surface. The resulting cerasome (partially ceramic- or silica-coated liposome) (60-70 nm) retains the integrity of such in the complexation with lucifarase-encoding plasmid DNA pGL3. The resultant pGL3 complex of infusible or monomeric cerasome in a viral size ( approximately 70 nm) exhibits a remarkable transfection performance toward HeLa and HepG2 cells with a 102-3-fold higher efficiency (relative to that of the nonsilylated reference lipid 2), minimized cytotoxicity, and serum compatibility. Reference lipid 2, i.e., alanine-based lipid having a simple quaternized ammonium headgroup, forms liposome (60-70 nm) which is less self-confined and more mobile undergoes DNA-induced fusion to give endocytosis-irrelevant and more toxic bigger (100-300 nm) particles. The silicon strategy thus provides a simple and widely applicable tool to overcome general problems associated with current technology of artificial gene delivery.

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@article{Matsui2006CerasomeAA, title={Cerasome as an infusible, cell-friendly, and serum-compatible transfection agent in a viral size.}, author={Kazuki Matsui and Shinsuke Sando and Takashi Sera and Yasuhiro Aoyama and Yoshihiro Sasaki and Takayoshi Komatsu and Takashi Terashima and Jun-ichi Kikuchi}, journal={Journal of the American Chemical Society}, year={2006}, volume={128 10}, pages={3114-5} }