Stable n-3 Diglyceride Emulsions for Ischemic Stroke Therapy
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Solution Overview
Problem
Current treatments for acute ischemic stroke, such as tissue plasminogen activator (t-PA), have limited effectiveness due to a narrow time window and do not effectively deliver neuroprotective agents like omega-3 fatty acids (n-3 FAs) to damaged brain tissue in a timely manner.
Innovation Solution
The development of stable n-3 diglyceride (DG) oil-in-water emulsions for acute therapy, which can be administered intravenously or intra-arterially, providing rapid delivery of n-3 FAs to injured tissues, including the brain, with a broader therapeutic window.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If stable n-3 diglyceride emulsions are developed for acute therapy, then the therapeutic window is expanded and neuroprotection is improved, but the emulsion stability and storage requirements become more complex
Solution Approach 1:
The patent applies parameter changes by optimizing emulsion composition parameters including using n-3 diglycerides with specific fatty acid profiles (DHA and/or EPA), controlling particle size distribution (mean diameter 10-500 nm), adjusting zeta potential (-30 to -60 mV), and selecting specific emulsifiers (phospholipids, proteins, or small molecules) to achieve both extended therapeutic window and storage stability
Solution Approach 2:
The patent employs composite materials by formulating complex emulsion systems combining n-3 diglyceride oil phase, aqueous phase, and multiple emulsifying agents (phospholipids like lecithin, proteins, or small molecule surfactants) to create a stable delivery system that maintains both therapeutic efficacy and storage stability
2Speed
If n-3 fatty acids are rapidly delivered to injured tissues, then neuroprotection effectiveness is improved, but the delivery system complexity increases
Solution Approach 1:
The patent uses emulsions as intermediary carriers that facilitate rapid delivery of n-3 fatty acids to injured tissues. The emulsion system acts as a mediator between the hydrophobic n-3 diglycerides and the aqueous bloodstream, enabling rapid transport and cellular uptake without requiring complex delivery devices or procedures
Solution Approach 2:
The patent leverages the hydraulic properties of intravenous infusion to achieve rapid delivery. The emulsion formulation is designed for IV administration, utilizing the body's existing fluid circulation system to rapidly distribute n-3 fatty acids to injured tissues throughout the body, including the brain
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
These emulsions effectively protect against cellular death, providing neuroprotection and organ protection in conditions such as ischemic stroke, myocardial infarction, and traumatic brain injury, even when administered outside the traditional time window for existing treatments.
Implementation Method 1
stable n-3 diglyceride (DG) oil-in-water emulsions for acute therapy
Data Source
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AI summary
The present invention provides compositions and methods involving stable omega-3 diglyceride oil-in-water emulsions for acute therapy to treat and/or prevent tissue or organ injury. The compositions provide protection from cellular death, and find use in patients in need of neuroprotection. For example, the compositions find use in treating ischemia reperfusion injuries, such as ischemic stroke. The compositions further find use for treatment of traumatic injuries, such as traumatic brain injury or spinal cord injury, among others. The compositions have a large time window by which they are effective after onset of traumatic or ischemic injury (e.g., after onset of stroke), and may be administered in conjunction with other therapies.