Preparation and application of drug delivery system of targeted liver GSDMD

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By wrapping AQ-390 in PLGA-PEG-NH2 and modifying GalNAc-NHS, a drug delivery system targeting liver GSDMD was prepared, solving the problem that AQ-390 cannot achieve specific organ delivery and achieving effective treatment of liver diseases.

CN119679957APending Publication Date: 2025-03-25THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL UNIV

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Patent Information

Application Number: CN202411916512.2
Authority / Receiving Office: CN · China
Patent Type: Applications(China)
Current Assignee / Owner
Filing Date: 2024-12-24
Publication Date: 2025-03-25

Application Information

Patent Timeline

24 Dec 2024

Application

CN202411916512.2

25 Mar 2025

Publication

CN119679957A

IPC: A61K47/34; A61K47/26; A61K31/4152; A61P1/16; A61P29/00; A61P9/12

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Application Domain

Organic active ingredients Antipyretic

Technology Topics

Pharmaceutical Substances Targeted therapy

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AI Technical Summary

Technical Problem

The prior art small and medium-sized compound AQ-390 cannot achieve selective intracellular delivery of specific organs, resulting in the inaccurate evaluation of the role and effect in the treatment of liver disease.

Method used

AQ-390@PLGA-GalNAc NPs targeting liver GSDMD was prepared by wrapping AQ-390 in PLGA-PEG-NH2 and modifying with GalNAc-NHS.

Benefits of technology

The specific targeted delivery of AQ-390 to the liver is achieved, effectively inhibiting liver GSDMD and reducing the symptoms of metabolic-related fatty liver and related organ diseases.

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Abstract

The invention relates to preparation and application of a drug delivery system of a targeted liver GSDMD, and the preparation method comprises the following steps: completely dissolving a small-molecule inhibitor AQ-390 of a pyroptosis effect protein GSDMD with DMSO; slowly dissolving the PLGA-PEG-NH2 by using acetone; the preparation method comprises the following steps: adding completely dissolved AQ-390 into acetone dissolved with PLGA, ultrasonically dispersing, slowly adding into distilled water, magnetically stirring at room temperature, and volatilizing an organic reagent acetone overnight at room temperature in a fuming cupboard to obtain the AQ-390 (AQ-390 at PLGA) wrapped by PLGA-PEG-NH2 vesicles. The preparation process is simple and convenient, experimental conditions are easy to obtain, the liver can be well targeted, GSDMD is inhibited, and a theoretical basis and a new method are provided for development of novel clinical targeted therapy and diagnostic agents.

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