Cationic lipid, liposome containing a cationic lipid, and nucleic acid pharmaceutical composition containing liposome, and formulation and application thereof

ES3072950T3Undetermined Publication Date: 2026-07-07

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Patent Information

Authority / Receiving Office: ES · ES
Patent Type: Patents
Filing Date: 2022-04-01
Publication Date: 2026-07-07

Application Information

Patent Timeline

01 Apr 2022

Application

07 Jul 2026

Publication

ES3072950T3

IPC: C07C219/06; C07C219/16; C07C229/12; C07C229/16; C07C229/26; C07C233/18; A61K9/127; A61P35/00; C08G65/332; C08G65/333; C08G65/337

CPC: A61K45/06; A61K47/18; A61P31/00; A61P35/00; A61K31/713; A61K9/1271; A61K9/1272; A61K9/5123

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AI Technical Summary

Technical Problem

Existing cationic lipids for drug delivery systems are not optimized for efficient transport and stability of nucleic acid drugs, leading to suboptimal therapeutic effects.

Method used

Development of novel cationic lipids branched via nitrogen, which can be protonated under physiological pH to enhance binding with nucleic acids, improve serum stability, and facilitate efficient cellular uptake through endocytosis, forming neutral ion pairs within endosomes to release drugs into the cytoplasm.

Benefits of technology

The novel cationic lipids enhance the loading, stability, and transfection efficiency of nucleic acid drugs, offering improved therapeutic outcomes with potential fluorescence or targeting capabilities.

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Abstract

The present invention provides a novel cationic lipid with the structure shown in the general formula (1), specifically a nitrogen-branched cationic lipid, a liposome containing said cationic lipid, a liposomal nucleic acid pharmaceutical composition also containing said cationic lipid, and its preparation and application. The definition of each symbol in the formula is defined herein. The cationic liposome containing the cationic lipid of formula (1), according to the present invention, can improve the loading rate and release rate of nucleic acid drugs. The preparation of the cationic liposomal nucleic acid pharmaceutical composition described in the present invention exhibits good cellular biocompatibility and enhanced gene transfection capacity, thereby improving the therapeutic and / or preventive effects of nucleic acid drugs.

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