Creatine Fatty Ester Composition for Nasal Brain Delivery
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Solution Overview
Problem
Current treatments for Creatine Transporter Deficiency (CTD) are ineffective due to the inability of creatine and its derivatives to cross the blood-brain barrier and degrade in biological fluids, leading to insufficient brain creatine levels and impaired energy metabolism.
Innovation Solution
A composition comprising creatine fatty esters, omega-3 fatty acids, and glycerides is administered nasally, bypassing the blood-brain barrier and protecting the esters from plasma esterases, allowing for stable delivery and conversion to creatine in brain cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If creatine is administered orally, then muscle mass and performance are improved, but brain creatine levels remain insufficient due to blood-brain barrier saturation
Solution Approach 1:
The patent changes the chemical form of creatine from free creatine to creatine fatty esters (prodrugs). This parameter change allows the compound to bypass the saturated creatine transporter at the blood-brain barrier through alternative pathways, thereby increasing brain creatine levels in CTD patients without relying on the saturated transporter system.
Solution Approach 2:
The patent uses creatine fatty esters as intermediary compounds that can cross the blood-brain barrier and are then converted to free creatine within the brain. These intermediary prodrugs serve as carriers that deliver creatine to the brain without being subject to the same transporter saturation limitations as free creatine.
2Quantity of substance
If creatine derivatives are used to cross the blood-brain barrier, then brain delivery is improved, but stability in biological fluids deteriorates due to degradation by plasma esterases
Solution Approach 1:
The patent employs nasal administration as a preliminary action that delivers creatine fatty esters directly to the brain, bypassing the bloodstream where plasma esterases would degrade the prodrugs. This preliminary direct delivery prevents the stability problem by avoiding exposure to degrading enzymes in biological fluids.
Solution Approach 2:
The patent extracts the creatine fatty esters from the bloodstream environment (where plasma esterases cause degradation) and delivers them directly to the brain through nasal administration. This extraction from the harmful environment preserves the stability of the prodrugs until they reach the target tissue.
3Ease of operation
If oral creatine supplementation is used, then general creatine availability is improved, but brain penetration is insufficient due to transporter saturation
Solution Approach 1:
The patent changes the administration route from oral to nasal and modifies the chemical form to creatine fatty esters. This dual parameter change maintains ease of non-invasive administration while dramatically improving brain creatine concentration by bypassing the saturated oral absorption and blood-brain barrier transporter system.
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 composition significantly increases brain creatine levels, improving cognitive function and brain performance in CTD patients by delivering creatine fatty esters effectively.
Implementation Method 1
conversion to creatine in brain cells
Data Source
AI summary
A composition comprising at least one creatine fatty ester or salt thereof, at least one omega 3 fatty acid or salt thereof and at least one glyceride for use in medicine, the composition being free of non ionic surfactants and in particular said composition for use in treating the brain creatine transporter deficiency disease.