Modified Krill Oil Parenteral Emulsion for Oxidative Stability
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Solution Overview
Problem
Current parenteral lipid emulsions containing omega-3 fatty acids, primarily from fish oil triglycerides, face challenges such as oxidative degradation and adverse effects due to high polyunsaturated fatty acid content, and the high phospholipid content of krill oil makes it unsuitable for use as a major source in injectable emulsions due to potential interference with plasma clearance and adverse reactions.
Innovation Solution
A composition comprising krill oil with a modified fatty acid profile, where omega-3 fatty acids are predominantly attached to the phospholipid backbone, particularly in the second position, and a mixture with fish oil is used to create a stable and effective parenteral formulation, potentially replacing or supplementing egg phospholipids as surfactants, and incorporating astaxanthin for antioxidant properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If krill oil with high phospholipid content is used as a major source in injectable emulsions, then the antioxidant protection and omega-3 fatty acid delivery are improved, but plasma clearance interference and adverse reactions occur
Solution Approach 1:
The patent extracts and removes phospholipids from krill oil to create a triglyceride-based formulation. This extraction eliminates the harmful high phospholipid content while retaining the beneficial omega-3 fatty acids (EPA and DHA) and astaxanthin antioxidant, thereby resolving the contradiction between antioxidant protection and plasma clearance interference
Solution Approach 2:
The patent changes the compositional parameters of krill oil by reducing phospholipid content to less than 10% w/w (preferably less than 5% w/w, more preferably less than 1% w/w) while maintaining or enhancing omega-3 fatty acid content. This parameter modification allows the oil to provide antioxidant protection without causing plasma clearance interference
2Stability of the object's composition
If omega-3 fatty acids are positioned at position-2 on the glyceride backbone, then oxidation resistance and bioavailability are improved, but manufacturing complexity increases
Solution Approach 1:
The patent specifies that omega-3 fatty acids should be predominantly at position-2 on the glyceride backbone (at least 70%, preferably at least 80%, more preferably at least 90%). This positional parameter change enhances oxidation resistance and bioavailability while the patent acknowledges this may require specialized manufacturing processes
3Quantity of substance
If vegetable or marine-based polyunsaturated fatty acids are used in injectable lipid emulsions, then nutritional support is improved, but oxidative degradation occurs
Solution Approach 1:
The patent converts the harmful susceptibility to oxidation into a benefit by incorporating astaxanthin, a potent natural antioxidant, at concentrations of at least 0.01 mg/L (preferably at least 0.1 mg/L, more preferably at least 1.0 mg/L). The astaxanthin protects the polyunsaturated fatty acids from oxidative degradation while maintaining their nutritional value
Solution Approach 2:
The patent modifies the fatty acid composition parameters by ensuring omega-3 fatty acids comprise at least 20% w/w (preferably at least 30% w/w, more preferably at least 40% w/w) of total fatty acids, with EPA and DHA specifically targeted. This compositional change provides nutritional support while the associated astaxanthin content prevents oxidative degradation
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 modified krill oil composition enhances the stability and bioavailability of omega-3 fatty acids, reduces oxidative degradation, and improves the safety and efficacy of parenteral administration by stabilizing emulsions and mitigating adverse effects, offering a safer treatment for conditions like sepsis and endotoxicosis.
Implementation Method 1
krill oil possesses another unique attribute, in that it contains the naturally occurring antioxidant, astaxanthin, but in amounts 10x to 100x higher than the antioxidants naturally found in commonly used polyunsaturated triglyceride oil-in-water parenteral emulsions
Implementation Method 2
a parenteral oil-in-water emulsion comprising a phospholipid obtained from a marine crustacean
Implementation Method 3
replacing or supplementing egg phospholipids as surfactants
Data Source
AI summary
A method of parenterally administering a composition, the method including parenterally administering to a person a composition including krill oil in an oil-in-water emulsion. A parenterally applicable pharmaceutical composition, including an oil-in-water emulsion including a phospholipid obtained from a marine crustacean.