Soluble Polyelectrolyte Complexes for Delayed Biguanide Release
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Solution Overview
Problem
Existing formulations of biguanide antimicrobial polyelectrolytes do not allow for controlled or delayed release forms, which are desirable for applications requiring sustained antibacterial action and tissue repair properties.
Innovation Solution
The formation of soluble polyelectrolyte complexes between glycosaminoglycans (GAGs) and cationic antimicrobial biguanide polymers (ABPs) at specific stoichiometric ratios greater than 10:1, enabling controlled, gradual, and delayed release of ABPs, synergizing antimicrobial action with wound-healing properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyelectrolyte complexes are formed with stoichiometric ratio approximating 1, then complex formation is maximized, but solubility is lost and insoluble complexes are obtained
Solution Approach 1:
The patent changes the stoichiometric ratio parameter from approximately 1:1 to greater than 10:1 (GAG:ABP), which fundamentally alters the complex properties from insoluble to soluble while maintaining complex formation. This parameter change enables the complex to remain in solution and be suitable for pharmaceutical formulations.
Solution Approach 2:
The patent uses an excessive amount of anionic polyelectrolyte (GAG) relative to the cationic polyelectrolyte (ABP), with the GAG:ABP ratio exceeding 10 in terms of equivalents. This excessive action of the anionic component prevents precipitation and maintains solubility while still forming effective complexes.
2Speed
If conventional formulations are used, then immediate antimicrobial action is achieved, but controlled or delayed release is not possible
Solution Approach 1:
The patent creates a pre-formed complex structure where the ABP is associated with GAG through electrostatic interactions. This preliminary complexation allows the antimicrobial agent to be released in a controlled manner over time, providing both immediate and sustained action rather than just immediate release.
Solution Approach 2:
The patent introduces dynamic release characteristics where the ABP can be progressively released from the GAG/ABP complex over time. The system transitions from a static formulation to a dynamic release system, enabling controlled, gradual, and/or delayed release of the antimicrobial agent.
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 soluble complexes provide sustained antimicrobial activity and tissue repair benefits, suitable for various pharmaceutical compositions and medical devices, optimizing rheology and efficacy through controlled release mechanisms.
Implementation Method 1
enabling controlled, gradual, and delayed release of ABPs
Implementation Method 2
the interaction between ABPs and GAGs forms polyelectrolyte complexes whose characteristics depend on the stoichiometry
Implementation Method 3
ABP is released from GAG/ABP due to competition on the surface of the GAG by other cations present at the site of application
Implementation Method 4
competition on the surface of the GAG by other cations
Implementation Method 5
synergising the antimicrobial action of ABP with the wound-healing and tissue-repair properties typical of GAG
Data Source
AI summary
Disclosed are soluble polyelectrolyte complexes of polymeric biguanidine antimicrobial, such as polyhexamethylene biguanide or polyaminopropyl biguanide, with glycosaminoglycans, such as hyaluronic acid, chondroitin or chondroitin sulphate and derivatives thereof, and their use as active ingredients of pharmaceutical compositions or medical devices.