Lipid particles, nucleic acid drugs containing the lipid particles, and compositions for nucleic acid delivery

By using lipid particles prepared by using specific compounds or their salts, the problems of low nucleic acid encapsulation rate and delivery efficiency in the prior art are solved, and efficient nucleic acid delivery effect is achieved.

CN116172975BActive Publication Date: 2025-03-28FUJIFILM CORP
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Patent Information

Application Number
CN202310246921.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2018-06-08
Filing Date
2019-06-07
Publication Date
2025-03-28
Estimated Expiration
2039-06-07

AI Technical Summary

Technical Problem

The prior art is difficult to achieve high nucleic acid encapsulation rates and excellent nucleic acid delivery, especially when lipid particles are used as carriers.

Method used

Lipid particles with high nucleic acid encapsulation rate and excellent nucleic acid delivery ability are prepared using specific compounds or their salts. The compound is represented by formula (1), and the encapsulation efficiency and delivery effect of the nucleic acid are improved by the optimization of specific linking groups and hydrocarbon chain lengths.

Benefits of technology

High nucleic acid encapsulation rate and excellent nucleic acid delivery effect are achieved, and the problem of low nucleic acid delivery efficiency in the prior art is solved.

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Abstract

The subject of the present invention is to provide a lipid particle capable of achieving high nucleic acid encapsulation rate and excellent nucleic acid delivery, a nucleic acid drug comprising the lipid particle, and a composition for nucleic acid delivery. According to the present invention, a compound represented by the following formula (1) or a salt thereof can be provided. In the formula, X represents -NR 1 ‑or‑O‑, R 1 represents a hydrogen atom, a hydrocarbon group, etc., R 2 and R 3 Each independently represents a hydrogen atom, a hydrocarbon group, etc., and R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 Each independently represents a hydrogen atom or an alkyl group, and R 4 With R 5 , R 10 With R 5 , R 5 With R 12 , R 4 With R 6 , R 5 With R 6 , R 6 With R 7 , R 6 With R 10 , R 12 With R 7 , and R 7 With R 8 Any one or more of the groups may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, and a, b, c and d each independently represent an integer of 0 to 3, wherein a+b is 1 or more, and c+d is 1 or more.
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