Method for coupling dialkylamine and polypeptide
The chemical coupling method was used to prepare compound (I) A-[B-]bC-D, which solved the problem of coupling P/A- and PAS- peptides with lipids. The prepared lipid nanoparticles were stable and turbid, prolonging the circulation time of lipid particles in the blood and improving RNA encapsulation efficiency and LNP shielding ability.
Patent Information
- Application Number
- CN202480068574.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-10-27
- Filing Date
- 2024-10-25
- Publication Date
- 2026-05-26
AI Technical Summary
Existing technologies have failed to provide an effective method for convenient and reliable coupling of P/A- and/or PAS- peptides to lipids, resulting in turbidity and precipitation problems in liposome formulations and failing to effectively prolong the circulation time of lipid particles in the blood.
Lipid nanoparticles were prepared by chemically coupling di(alkyl)amines with P/A- and/or PAS- peptides using compound (I), where A is a di(alkyl)amino, B is a linker, b is 1 or 0, C is a polypeptide capable of forming a random coil conformation, and D is an N-terminal protecting group. Lipid nanoparticles were then prepared by mixing ethanol solution with aqueous solution.
Efficient and stable coupling of P/A- and/or PAS- peptides with lipids was achieved. The prepared lipid nanoparticles were free of turbidity and precipitation, and the circulation time of lipid particles in the blood was significantly prolonged, improving RNA encapsulation efficiency and LNP shielding ability.