Self-emulsifying bioactive concentrate for retinoid delivery
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing methods for reducing skin aging using retinoids often cause deleterious skin effects such as flaking, peeling, and visible redness due to required high concentrations and dosing regimens.
Innovation Solution
The use of novel bioactive lysophospholipid emulsifiers produced by combining de-oiled lecithin with Phospholipase A enzyme activity and retinyl esters in self-emulsifying bioactive concentrates, which optimize epidermal thickening without harming the skin barrier or causing adverse effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If retinoids are administered at high concentrations to achieve epidermal thickening, then skin aging signs are reduced, but deleterious skin effects such as flaking, peeling, and redness occur
Solution Approach 1:
The invention changes the chemical parameters of the retinoid by converting it into a retinyl ester prodrug form. This modification alters the molecular structure to reduce irritation while maintaining the ability to produce epidermal thickening and reduce aging signs when metabolized in the skin.
Solution Approach 2:
The retinyl ester acts as an intermediary substance that is less irritating than the active retinoid. It serves as a prodrug that gets metabolized in the skin to release the active retinoid, thereby mediating between the need for effective anti-aging action and the need to minimize harmful side effects.
2Stability of the object's composition
If conventional emulsifiers are used in retinoid formulations, then skin barrier function is compromised, but product stability and delivery are improved
Solution Approach 1:
The invention uses a composite emulsifier system comprising both synthetic and natural emulsifiers. This composite approach combines the stability-providing properties of synthetic emulsifiers with the skin-friendly characteristics of natural emulsifiers, achieving both formulation stability and skin barrier preservation.
Solution Approach 2:
The emulsifier system is segmented into multiple components with different functions. Synthetic emulsifiers provide structural stability and emulsion maintenance, while natural emulsifiers provide skin compatibility and barrier protection. This segmentation allows each component to optimize its specific function without compromising the other.
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 bioactive concentrates effectively reduce signs of skin aging with increased epidermal thickness, minimizing skin redness and flaking, while maintaining skin health, and enhancing retinyl ester proliferative properties.
Implementation Method 1
combining (i) a de-oiled lecithin and (ii) from about 0.1 to about 10% of an enzyme with Phospholipase A ('PLA') Activity
Implementation Method 2
an enzyme with Phospholipase A ('PLA') Activity
Implementation Method 3
enhancing retinyl ester proliferative properties
Data Source
AI summary
A self-emulsifying bioactive concentrate produced by a process comprising the steps of (a) creating a lysophospholipid concentrate comprised of a de-oiled lecithin source and 0.1% to 10% of an enzyme with having phospholipase A activity, wherein the lysophospholipid concentrate contains greater than 20% lysophosphatidyl-choline; and (b) combining the lysophospholipid concentrate from step (a) with a retinyl ester formed by the reaction of retinol and one or a mixture of unsaturated fatty acid(s).