ROS-responsive cationic liposome-loaded tryptanthrin as well as preparation method and application thereof

By using ROS-responsive cationic liposomes to deliver tryptophan ketone in a local high ROS environment in the intestine, the problem of poor solubility and insufficient targeting of tryptophan ketone during ECLS is solved, thus achieving effective protection against intestinal damage and reducing systemic side effects.

CN121846031APending Publication Date: 2026-04-14THE FIRST MEDICAL CENT CHINESE PLA GENERAL HOSPITAL
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Patent Information

Application Number
CN202610284746.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-03-10
Publication Date
2026-04-14

AI Technical Summary

Technical Problem

In existing technologies, tryptophan has problems such as poor solubility, low bioavailability, and insufficient targeting during in vitro life support, which leads to severe intestinal damage and adverse reactions when administered systemically.

Method used

ROS-responsive cationic liposomes carrying tryptophan were used. By encapsulating tryptophan in liposomes, the ROS-responsive properties of DSPE-TK-PEG and the cationic properties of DOTAP were utilized to achieve targeted release in the high ROS environment of the intestine, thereby enhancing the therapeutic effect and reducing systemic exposure.

Benefits of technology

In ECLS-related intestinal injury, ROS-responsive cationic liposome ketone significantly reduced ADAMTS4 expression and VCAN degradation, improved intestinal barrier integrity, reduced inflammatory factor expression, and decreased intestinal tissue damage scores, while liver and kidney function remained largely normal, demonstrating good efficacy and safety.

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Abstract

The invention provides ROS (reactive oxygen species)-responsive cationic liposome-loaded tryptanthrin as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The ROS response cationic liposome loaded tryptanthrin disclosed by the invention comprises an ROS response cationic liposome and tryptanthrin which is entrapped in the ROS response cationic liposome; the ROS response cationic liposome is prepared from the following raw materials: egg yolk lecithin, cholesterol, DSPE-TK-PEG (distearoyl phosphatidylcholine) and DOTAP (dioctyl phthalate). In view of significant increase of intestinal local active oxygen under the ECLS condition, the ROS-responsive cationic liposome is adopted to wrap tryptanthrin, so that tryptanthrin is selectively released in an intestinal injury area, whole body exposure is reduced, and meanwhile, the protection effect on the intestinal tract is enhanced.
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