Coordination Complex for Synergistic Drug Delivery

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Solution Overview

Problem

Current combination drug therapies often face challenges in ensuring effective synergistic delivery of multiple pharmaceutical agents, as seen in cases where one agent can interfere with the binding of another, leading to reduced efficacy or toxicity, and there is a lack of methods using metals to combine different pharmacophore fragments effectively.

Innovation Solution

The development of coordination complexes comprising a first and second biologically active moiety bound to a metal, forming a single molecular entity that enhances pharmacodynamic properties and allows for synergistic delivery to target tissues, leveraging metal coordination chemistry to stabilize the complex while maintaining biological activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple pharmaceutical agents are combined in a single molecular entity, then synergistic delivery and pharmacodynamic properties are enhanced, but the complexity of designing and manufacturing the complex increases

Engineering Contradiction:
Improvesynergistic delivery efficacyVSAvoidcomplex design and manufacturing
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

A metal ion serves as an intermediary to coordinate and hold multiple pharmacophore fragments in a stable complex structure, enabling synergistic delivery while simplifying the overall design compared to covalent conjugation approaches

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite molecular entity combining multiple pharmacophore fragments with a metal ion, leveraging the stabilizing properties of metal coordination chemistry to achieve both synergistic efficacy and structural stability

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If biologically active moieties are bound to a metal in a coordination complex, then stability and pharmacokinetic properties are improved, but the loss of free pharmacophore fragments may occur

Engineering Contradiction:
Improvecomplex stabilityVSAvoidpharmacophore fragment release
Core Design Contradiction:
Stability of the object's compositionVSLoss of substance

Solution Approach 1:

The coordination complex is designed with dynamic binding characteristics, allowing the metal-pharmacophore bonds to remain stable during circulation while enabling controlled release at target sites through ligand exchange mechanisms

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The patent utilizes changes in the coordination environment of the metal ion (such as ligand exchange with biological molecules) to control the release of pharmacophore fragments at the appropriate time and location

Inventive Principle:
Principle #35Parameter changes

3Reliability

If combination drug therapy is used to treat disease states, then treatment efficacy and quality of life are improved, but the risk of interference between agents and toxicity increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidagent interference and toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the combination therapy into distinct pharmacophore fragments that are spatially separated around a central metal ion, preventing direct interference between agents while maintaining their synergistic therapeutic effects

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The metal ion acts as a mediator that holds potentially interfering pharmacophore fragments in a controlled arrangement, allowing them to function synergistically while preventing harmful interactions between the agents

Inventive Principle:
Principle #24Intermediary (Mediator)

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

This approach enables kinetically synergistic delivery of biologically active agents, improving their pharmacokinetic properties, stability, and efficacy by forming a single molecular entity that retains therapeutic effects while minimizing interference, thus enhancing treatment outcomes for various disease states.

Implementation Method 1

The development of coordination complexes comprising a first and second biologically active moiety bound to a metal, forming a single molecular entity that enhances pharmacodynamic properties

Methodology Applied
Scientific EffectMetal coordination chemistry: Chemical Bonding

Data Source

PatentEP2373171B1Frequency modulated drug delivery (FMDD)
Publication Date: 2017.11.01 SYNTHONICS INC
  • EP2373171B1 patent drawingFigure 1
  • EP2373171B1 patent drawingFigure 2
  • EP2373171B1 patent drawingFigure 3

AI summary

Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.