@article{oai:nagasaki-u.repo.nii.ac.jp:00006210, author = {Kodama, Yukinobu and Harauchi, Satoe and Kawanabe, Saki and Ichikawa, Nobuhiro and Nakagawa, Hiroo and Muro, Takahiro and Higuchi, Norihide and Nakamura, Tadahiro and Kitahara, Takashi and Sasaki, Hitoshi}, issue = {6}, journal = {Biological and Pharmaceutical Bulletin}, month = {Jun}, note = {We developed binary and ternary complexes based on polymers and liposomes for safe and effective delivery of small interfering RNA (siRNA). Anti-luciferase siRNA was used as a model of nucleic acid medicine. The binary complexes of siRNA were prepared with cationic polymers and cationic liposomes such as polyethylenimine (PEI), polyamidoamine (PAMAM) dendrimer, poly-L-arginine (PLA), trimethyl[2,3-(dioleoxy)-propyl]ammonium chloride (DOTMA), and cholesteryl 3β-N-(dimetylaminnoethyl)carbamate hydrochloride (DC-Chol). The ternary complexes were constructed by the addition of γ-polyglutamic acid (γ-PGA) to the binary complexes. The complexes were approximately 54-153 nm in particle size. The binary complexes showed a cationic surface charge although an anionic surface charge was observed in the ternary complexes. The polymer-based complexes did not show a silencing effect in the mouse colon carcinoma cell line expressing luciferase regularly (Colon26/Luc cells). The binary complexes based on liposomes and their ternary complexes coated by γ-PGA showed a significant silencing effect. The binary complexes showed significant cytotoxicity although the ternary complexes coated by γ-PGA did not show significant cytotoxicity. The ternary complexes coated by γ-PGA suppressed luciferase activity in the tumor after their direct injection into the tumors of mice bearing Colon26/Luc cells. Thus, we have newly identified safe and efficient ternary complexes of siRNA for clinical use., Biological and Pharmaceutical Bulletin, 36(6), pp.995-1001; 2013}, pages = {995--1001}, title = {Safe and Effective Delivery of Small Interfering RNA with Polymer- and Liposomes-Based Complexes}, volume = {36}, year = {2013} }