Alkylammonium EDTA Lipid Formulations for Oxidation Stability
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Solution Overview
Problem
Lipid-based formulations are susceptible to oxidation during storage and in vivo, especially when metal ions like iron are present, leading to reduced efficacy and shelf-life, and conventional antioxidants are not soluble in non-aqueous environments.
Innovation Solution
Incorporation of alkylammonium EDTA salts into lipid formulations, which are soluble in non-aqueous environments, to prevent oxidative degradation of lipids and active agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional antioxidants are used in lipid formulations, then oxidation protection is provided, but the antioxidants are not soluble in non-aqueous environments
Solution Approach 1:
The patent changes the chemical parameter of the antioxidant by converting it from its conventional form to an alkylammonium salt form. This parameter change enables the antioxidant to dissolve in non-aqueous lipid environments while retaining its oxidation protection capability through metal ion chelation
Solution Approach 2:
The alkylammonium group acts as an intermediary that bridges the incompatibility between conventional antioxidants and non-aqueous lipid environments. This intermediary structure provides both the solubility needed for lipid formulation incorporation and the chelating functionality for oxidation protection
2Duration of action of moving object
If lipid formulations are stored for extended periods, then controlled release functionality is maintained, but oxidation and chemical degradation occur
Solution Approach 1:
The alkylammonium EDTA salt is incorporated into the lipid formulation during manufacturing, performing preliminary protection against oxidation before the formulation is stored or administered. This advance protection prevents degradation during the extended storage period required for controlled release applications
Solution Approach 2:
The patent converts the harmful effect of metal ions that catalyze oxidation into a beneficial effect by using these same metal ions as targets for chelation. The alkylammonium EDTA salt specifically binds metal ions, transforming the oxidation catalyst into a stabilized complex that protects the lipid formulation during long-term storage
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
Significantly reduces oxidation and chemical degradation, maintaining the stability and efficacy of lipid-based formulations, thereby extending shelf-life and ensuring controlled release of active agents.
Implementation Method 1
Incorporation of alkylammonium EDTA salts into lipid formulations, which are soluble in non-aqueous environments, to prevent oxidative degradation of lipids and active agents
Implementation Method 2
Both the lipid components, particularly unsaturated lipids, and any active agent contained in the pre-formulation or sustained release composition are susceptible to oxidation... it is thought that equipment used for the manufacture of lipid formulations commonly includes stainless steel which can leach small amounts of metal ions (particularly Fe) into the mixture. It is therefore common to include an antioxidant in lipid formulations. These generally function by chelating any metal ions, thereby hindering their participation in oxidation processes
Data Source
AI summary
The present invention relates to mixtures comprising at least one lipid and/or at least one oil; and an alkyl ammonium EDTA salt; wherein the mixture has a water content in the range of 0 to 1.0 wt %. The invention further relates to mixtures which are pre-formulations, methods of treatment comprising administration of such pre-formulations, to pre-filled administration devices and kits containing the formulations, to the use of an alkylammonium EDTA salt to reduce the decomposition of the lipid components and/or any active agent contained within the pre-formulation, and to alkyl ammonium EDTA salts as described herein.