title: Enhanced plasmid DNA transfer into tumor cells by nanoparticle composed of cholesteryl triamine and diamine.
abstract: Previously, we prepared cationic nanoparticles (NP and NP-N) composed of cholesteryl diamine (OH-Chol, (3S)-N-(2-(2-hydroxyethylamino)ethyl)cholesteryl-3-carboxamide) and cholesteryl triamine (OH-N-Chol, (3S)-N-(2-(2-(2-hydroxyethylamino)ethylamino)ethyl)cholesteryl-3-carboxamide), respectively, with Tween 80 for small interfering RNA (siRNA) delivery into tumor cells. In this study, we prepared NP-0.25 N composed of OH-Chol and OH-N-Chol at a molar ratio of 3/1 with Tween 80, and evaluated the transfection efficiency of plasmid DNA (pDNA) into tumor cells. NP-N exhibited lower transfection activity than NP; however, NP-0.25 N showed higher transfection activity than both NP and NP-N in various tumor cells. NP-0.25 N increased the amount of internalized pDNA by increased cellular association, and improved the escape from endosomes after clathrin-mediated endocytosis. The results of the experiments suggested that cholesteryl triamine may have potential as a helper lipid to increase the transfection for pDNA delivery by cationic cholesterol-based nanoparticles.
authors: Institute of Medicinal Chemistry, Hoshi University, Tokyo 142–8501, Japan. yhattori@hoshi.ac.jp
authors: Yoshiyuki
authors: Y
authors: Hattori
authors: Tsukasa
authors: T
authors: Nakamura
authors: Hiroaki
authors: H
authors: Ohno
authors: Nobutaka
authors: N
authors: Fujii
authors: Yoshie
authors: Y
authors: Maitani
mesh_terms: D045744:Cell Line, Tumor; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000737:chemistry; D004247:DNA / Q000008:administration & dosage* / Q000737:chemistry; D004983:Ethanolamines / Q000737:chemistry*; D006801:Humans; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010957:Plasmids; D011136:Polysorbates / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D014162:Transfection / Q000379:methods*
chemical_list: D004983:Ethanolamines; C582849:N-(2-(2-(2-hydroxyethylamino)ethylamino)ethyl)cholesteryl-3-carboxamide; D011136:Polysorbates; D013501:Surface-Active Agents; C551595:cholesteryl-3beta-carbosyamidoethylene-N-hydroxyethylamine; D004247:DNA; D002784:Cholesterol