SATO YUSUKE,佐藤 悠介,HARASHIMA HIDEYOSHI,原島 秀吉,OKABE NANA,岡部 奈々
申请号：
JP2018038082
公开号：
JP2019151589A
申请日:
2018.03.02
申请国别(地区):
JP
年份:
2019
代理人:
摘要：
PROBLEM TO BE SOLVED: To provide lipid nanoparticles useful as a carrier for drug active ingredients such as siRNA and having excellent delivery efficiency even if the particle diameter has become small.SOLUTION: Provided is a lipid nanoparticle containing a cationic lipid represented by the following general formula (I) [a is an integer from 3 to 5； b is 0 or 1； R1 and R2 are each independently a group having 20 or more carbon atoms represented by the following general formula (A) (q represents an integer from 1 to 9, r represents 0 or 1, s represents an integer from 1 to 3, t represents 0 or 1, u represents an integer from 1 to 8, c represents 0 or 1, v represents an integer from 4 to 12)； X represents a group represented by the following general formula (B) (d is an integer of 0 to 3, R3 and R4 are each independently a C1-4 alkyl group or a C2-4 alkenyl group) or a 5- to 7-membered non-aromatic heterocyclic group]； and a neutral lipid with a hydrophilic group having 2 or more carbon atoms and a linear hydrophobic group.SELECTED DRAWING: NoneCOPYRIGHT: (C)2019,JPO&INPIT【課題】本発明は、ｓｉＲＮＡ等の薬効成分のキャリアとして有用であり、粒子径が小さくなっても送達効率の優れた脂質ナノ粒子を提供することを課題とする。【解決手段】下記一般式（Ｉ）〔ａは３～５の整数；ｂは０又は１；Ｒ１及びＲ２はそれぞれ独立に下記一般式（Ａ）（ｑは１～９の整数、ｒは０又は１、ｓは１～３の整数、ｔは０又は１、ｕは１～８の整数、ｃは０又は１、ｖは４～１２の整数を示す。）で表される炭素数２０以上の基；Ｘは下記一般式（Ｂ）（ｄは０～３の整数、Ｒ３及びＲ４はそれぞれ独立にＣ１－４アルキル基又はＣ２－４アルケニル基である。）で表される基又は５～７員非芳香族ヘテロ環基を示す〕で表されるカチオン性脂質と、炭素数２以上の親水性基と直鎖状の疎水性基を備える中性脂質とを含有する、脂質ナノ粒子。［化１］【選択図】なし
