Enhanced Plasmid DNA Transfer into Tumor Cells by Nanoparticle Composed of Cholesteryl Triamine and Diamine

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概要

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• 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-0.25N 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-0.25N showed higher transfection activity than both NP and NP-N in various tumor cells. NP-0.25N 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.

著者

• Maitani Yoshie

  Institute Of Medicinal Chemistry Hoshi University

• Ohno Hiroaki

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Fujii Nobutaka

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Hattori Yoshiyuki

  Institute Of Medicinal Chemistry Hoshi University

• Ohno Hiroaki

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Nakamura Tsukasa

  Institute of Medicinal Chemistry, Hoshi University

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