Dextran Mannose Carrier Targeting CD206 Macrophages

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Solution Overview

Problem

Current methods lack effective solutions for diagnosing and treating macrophage-related disorders, as existing technologies do not specifically target CD206 expressing cells, which are involved in various diseases including immune-mediated and inflammatory conditions.

Innovation Solution

Development of synthetic macromolecular carrier molecules, such as tilmanocept, that bind exclusively to the mannose receptor protein CD206 on macrophages and other CD206 expressing cells, allowing for targeted delivery of therapeutic or diagnostic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional diagnostic and therapeutic agents are used, then general delivery to tissues is achieved, but specific targeting of CD206 expressing macrophages is not realized

Engineering Contradiction:

Improvediagnostic detection precisionVSAvoidtarget cell specificity

Core Design Contradiction:

Measurement precisionVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by modifying specific regions of the dextran molecule to contain mannose moieties at controlled densities and configurations. This creates localized binding sites that specifically recognize CD206 receptors on macrophages, while other portions of the molecule maintain properties for circulation and stability. The differential structure allows simultaneous optimization of targeting precision and delivery versatility.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying the molecular weight, mannose content, and structural configuration of dextran derivatives. These parameter adjustments optimize the balance between renal clearance, blood circulation time, and receptor binding affinity. By tuning these parameters, the agents achieve both specific macrophage targeting and adaptable delivery to different tissue contexts.

Inventive Principle:

Principle #35Parameter changes

2Productivity

If non-specific delivery systems are used, then broad tissue distribution is achieved, but targeted therapeutic delivery to macrophages is not accomplished

Engineering Contradiction:

Improvetherapeutic delivery efficiencyVSAvoidoff-target effects

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses mannose moieties as intermediary structures that mediate between the dextran carrier and CD206 receptors on macrophages. This intermediary binding mechanism enables selective recognition and uptake by target cells, while non-target cells lack the appropriate receptors and thus do not accumulate the therapeutic agent. This intermediary step eliminates off-target effects while maintaining high delivery efficiency to macrophages.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If existing carrier molecules are used, then general pharmacokinetic properties are achieved, but macrophage-specific uptake and retention are not optimized

Engineering Contradiction:

Improvetherapeutic agent retentionVSAvoidmacrophage targeting capability

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent creates composite structures by combining dextran backbone with mannose moieties and potentially other functional groups. This composite design integrates the stability and circulation properties of dextran with the specific macrophage-targeting capability of mannose-CD206 interactions. The composite structure achieves both reliable retention through stable circulation and effective targeting through receptor-mediated uptake.

Inventive Principle:

Principle #40Composite materials

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 carrier molecules effectively target and internalize into CD206 expressing cells, enabling precise diagnostic imaging and therapeutic intervention for macrophage-related disorders, improving diagnostic detection and therapeutic delivery.

Implementation Method 1

bind exclusively to the mannose receptor protein CD206 on macrophages and other CD206 expressing cells

Methodology Applied

Scientific EffectReceptor-ligand binding:

Implementation Method 2

The carrier molecules effectively target and internalize into CD206 expressing cells

Methodology Applied

Scientific EffectEndocytosis:

Data Source

PatentUS20220016272A1Compositions, methods and kits for diagnosing and treating CD206 expressing cell-related disorders

Publication Date: 2022.01.20 CARDINAL HEALTH 414 LLC

AI summary

A method of diagnosing a CD206 expressing cell-related disorder by administering a pharmaceutical composition to a subject, the composition including a carrier molecule having a detectable moiety attached thereto. The carrier molecule has a dextran backbone, and at least one receptor substrate conjugated, directly or indirectly, to the dextran backbone, wherein the receptor substrate is chosen so as to specifically bind to CD206. A method of treating a CD206 expressing cell-related disorder is also provided, as well as an ex vivo method and kit for quantitating the number of cells expressing CD206 in a bodily fluid.