Thiol-Functionalized Polyglycerol Mucolytics for Viscous Mucus
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Solution Overview
Problem
Existing treatments for conditions characterized by excessive mucus production and increased mucus viscosity, such as cystic fibrosis and chronic obstructive pulmonary disease, are inadequate in effectively decomposing disulfide bridges in mucus, leading to respiratory issues and inflammation.
Innovation Solution
The use of thiol-functionalized polyglycerol derivatives, which can penetrate mucus gels and break disulfide bridges, thereby reducing mucus viscosity and providing anti-inflammatory effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing mucolytic treatments (NAC, dithiol compounds) are used, then disulfide bridges in mucus are targeted for decomposition, but the effectiveness is insufficient and mucus viscosity remains high
Solution Approach 1:
The patent changes the chemical parameters of existing mucolytic compounds by introducing polyglycerol backbones with multiple thiol groups, transforming simple dithiol compounds into multi-thiol polymeric structures. This parameter change increases the number of active sites per molecule, thereby improving the reliability of disulfide bridge decomposition and reducing mucus viscosity more effectively.
Solution Approach 2:
The patent creates composite mucolytic agents by combining polyglycerol backbones with multiple thiol-functionalized side chains. This composite structure integrates the flexibility and solubility of polyglycerol with the high reactivity of multiple thiol groups, achieving superior effectiveness in decomposing disulfide bridges compared to simple dithiol compounds.
2Stability of the object's composition
If mucus concentration increases in diseases like CF and COPD, then mucus forms disulfide bridges and viscoelastic properties increase, but this leads to life-threatening respiratory issues
Solution Approach 1:
The patent introduces thiol-functionalized polyglycerol derivatives as intermediary agents that mediate between the excessive mucus production and the respiratory system. These compounds act as reducing agents that selectively break disulfide bridges in mucus without disrupting the overall mucus gel structure, thereby maintaining protective functions while eliminating respiratory obstruction.
Solution Approach 2:
The patent changes the redox parameters of the mucus environment by introducing compounds with multiple thiol groups that can reduce disulfide bonds. This parameter change transforms the oxidized, cross-linked mucus state into a reduced, more fluid state, preventing respiratory obstruction while preserving the mucus barrier function.
3Productivity
If simple dithiol compounds are used for mucolysis, then some disulfide bridges are reduced, but the overall mucus viscosity reduction is limited
Solution Approach 1:
The patent segments the mucolytic function into multiple independent thiol groups attached to a polyglycerol backbone. Each thiol group acts as an independent active site for disulfide bridge decomposition, increasing the overall productivity of the mucolytic agent compared to simple dithiol compounds with only two reactive groups.
Solution Approach 2:
The patent creates multi-functional mucolytic agents where each polyglycerol molecule performs multiple disulfide bridge reduction reactions simultaneously. The multiple thiol groups provide universal reactivity toward various disulfide bonds in different mucus regions, significantly enhancing the rate of decomposition and viscosity reduction.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The thiol-functionalized polyglycerol derivatives effectively reduce mucus viscosity and alleviate respiratory and gastrointestinal conditions by facilitating mucus decomposition and discharge, while also offering anti-inflammatory properties.
Implementation Method 1
The basic strategy for relieving mucus-induced shortness of breath is to decompose the mucus by reducing the disulfide bridges
Implementation Method 2
Mucus consists of highly glycosylated mucin monomers (up to 80% sugar content), which allows hydrogels to form in the presence of water
Data Source
AI summary
It is provided a method of treatment of a human or animal patient in need thereof to achieve a reduction of the viscosity of mucus of the patient which is carried out by administering a polyglycerol derivative having a linear or dendritic polyglycerol backbone and carrying at least one thiol group covalently bound to the polyglycerol backbone. It is further provided a method of treatment of a human or animal patient suffering from chronic sinusitis, asthma, chronic bronchitis, cystic fibrosis, chronic obstructive pulmonary disease, emphysema, bronchiectasis, chronic inflammatory bowel diseases, constipation, gastrointestinal malabsorption syndrome, irritable bowel syndrome, steatorrhea or diarrhea by administering a polyglycerol derivative. Further specific thiol-functionalized polyglycerol derivatives and a corresponding manufacturing method are provided.