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    • 2. 发明授权
    • Nucleic acid complex and nucleic acid delivery composition
    • 核酸复合物和核酸递送组合物
    • US08338584B2
    • 2012-12-25
    • US12741457
    • 2008-11-06
    • Hirofumi TakeuchiYuichi TozukaYasuyuki HiraHidekazu Toyobuku
    • Hirofumi TakeuchiYuichi TozukaYasuyuki HiraHidekazu Toyobuku
    • C07H21/04C01H1/00A61K31/70
    • A61K47/40A61K9/1272A61K47/543A61K47/6951A61K48/005B82Y5/00C12N15/88
    • The present invention provides a nucleic acid complex with low toxicity and high safety that can persistently maintain a nucleic acid, such as siRNA or the like, in a cell; and a nucleic acid delivery composition that can efficiently deliver the nucleic acid complex into a cell. A nucleic acid complex with low toxicity and high safety that can persistently maintain a nucleic acid in a cell can be obtained by forming a complex using a nucleic acid to be introduced into a cell, and a highly branched cyclic dextrin. Moreover, when a carrier comprising (A) a diacylphosphatidylcholine, (B) cholesterol and/or a derivative thereof, and (C) an aliphatic primary amine is used as a nucleic acid delivery carrier to introduce the nucleic acid complex into a cell, the safety, the efficiency of intracellular delivery, and the persistence of the nucleic acid in the cell can be further improved.
    • 本发明提供了一种具有低毒性和高安全性的核酸复合物,其可以在细胞中持续保持核酸如siRNA等; 以及可以有效地将核酸复合物递送到细胞中的核酸递送组合物。 可以通过使用待引入细胞的核酸和高度支化的环糊精形成复合物来获得能够持续维持细胞中核酸的低毒性和高安全性的核酸复合物。 此外,当使用包含(A)二酰基磷脂酰胆碱,(B)胆固醇和/或其衍生物和(C)脂肪族伯胺的载体作为核酸递送载体以将核酸复合物引入细胞时, 可以进一步提高安全性,细胞内递送的效率和核酸在细胞中的持续性。