Siglec-Binding Nanoparticle Composition for Stable Targeted Delivery
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Solution Overview
Problem
Existing therapeutic agents face challenges in targeting Siglec receptors on cell surfaces due to hydrolysis and degradation, leading to reduced efficacy and high production costs, and there is a need for compositions that can deliver Siglec-binding ligands and therapeutic agents via receptor-mediated endocytosis.
Innovation Solution
A pharmaceutical composition comprising a non-covalent complex of a Siglec-binding agent, such as sialic acid or its derivatives, with a counterion, forming nanoparticles that can be insoluble and stable, encapsulating active pharmaceutical ingredients, using cationic lipids or polymers for delivery to specific cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antibodies are used to target Siglec receptors, then specific binding to cell surfaces is achieved, but hydrolysis and degradation occur leading to reduced efficacy
Solution Approach 1:
The patent uses short-chain sialic acid derivatives (oligosaccharides with 2-10 sugar units) instead of long-lived antibodies. These short-chain molecules are more resistant to hydrolysis and degradation, maintaining binding activity longer despite their smaller size and shorter half-life in circulation.
Solution Approach 2:
The patent modifies the chemical structure of sialic acid by creating derivatives with specific sugar unit lengths (2-10 units) and attaching them to carrier molecules. This parameter change optimizes the balance between binding affinity to Siglec receptors and resistance to degradation, improving both reliability and duration of action.
2Reliability
If antibodies are used for targeted delivery, then specific cell binding is achieved, but production costs increase
Solution Approach 1:
The patent replaces expensive antibody production with cheaper sialic acid derivative synthesis. The short-chain oligosaccharides can be produced through standardized chemical synthesis methods, significantly reducing manufacturing costs while maintaining targeted delivery capability to Siglec-expressing cells.
Solution Approach 2:
The patent uses simplified molecular copies of sialic acid structures (short-chain derivatives) instead of full-length antibodies. These copies retain the essential binding function at a fraction of the cost, achieving the same targeting accuracy through a more economical molecular model.
3Adaptability or versatility
If sialic acid-containing agents are used to bind Siglec, then immune modulation is achieved, but delivery stability is reduced
Solution Approach 1:
The patent creates composite structures by conjugating sialic acid oligosaccharide derivatives to carrier molecules (such as proteins, lipids, or polymers). This composite approach enhances delivery stability by protecting the sialic acid moieties from degradation while maintaining their immune modulation capability through Siglec binding.
Solution Approach 2:
The patent optimizes the length of sialic acid chains (2-10 sugar units) and modifies their chemical structure to improve stability. This parameter optimization allows the agents to maintain both delivery stability and immune modulation capability, as the modified structures resist degradation better while retaining Siglec binding affinity.
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 composition effectively binds Siglec receptors, facilitating immune modulation and targeted delivery of therapeutic agents to cells, enhancing stability and reducing production costs.
Implementation Method 1
a non-covalent complex formed by a Siglec-binding agent and a counterion
Implementation Method 2
a non-covalent complex formed by a Siglec-binding agent and a counterion
Data Source
AI summary
This invention provides a pharmaceutical composition comprising an agent that can bind Siglec receptors on cell surface. This invention also provides the method of preparing said pharmaceutical composition and the use thereof.