Krill Oil Solubilization of Poorly Water-Soluble Active Agents
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Solution Overview
Problem
Existing methods for solubilizing poorly water-soluble dietary supplements and pharmaceutically active agents face challenges such as high production costs, health risks from solubilizers like polysorbates, adverse side effects, variable absorption rates, and high equipment requirements, limiting their widespread use and effectiveness.
Innovation Solution
A method using krill oil extract as a solubilizer, combined with controlled temperature increments, to create a clear solubilisate solution of these agents without polysorbates, ensuring stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If polysorbate-based solubilization methods are used, then solubility of poorly water-soluble agents is improved, but health risks and adverse side effects increase
Solution Approach 1:
The patent replaces expensive and harmful polysorbate solubilizers with krill oil, which contains natural phospholipids that form micelles. This substitution eliminates the need for potentially carcinogenic substances while maintaining solubilization effectiveness through a safer, naturally occurring alternative.
Solution Approach 2:
Krill oil acts as an intermediary substance that mediates between the poorly water-soluble active agent and the aqueous environment. The phospholipids in krill oil form micellar structures that encapsulate lipophilic compounds, enabling their solubilization in water-based formulations without requiring harmful solubilizers.
2Reliability
If conventional solubilization techniques are used, then bioavailability is improved, but production costs and equipment requirements increase
Solution Approach 1:
The patent employs a self-emulsification process where krill oil automatically forms micelles and emulsifies the active agent upon contact with water, without requiring high-pressure homogenizers or complex equipment. This self-service mechanism dramatically simplifies manufacturing while maintaining high bioavailability through natural micelle formation.
Solution Approach 2:
The invention changes the physical-chemical parameters of the formulation by using krill oil's natural phospholipid content to create micelles at physiological concentrations. This parameter change eliminates the need for expensive high-pressure processing equipment while achieving superior solubilization and bioavailability compared to conventional methods.
3Quantity of substance
If micelle and liposome application technologies are used, then solubility is improved, but device complexity and production difficulty increase
Solution Approach 1:
The patent extracts and utilizes the natural micelle-forming capability of phospholipids from krill oil, eliminating the need for complex liposome fabrication equipment. By focusing on the essential micelle-forming function rather than creating complete liposome structures, the process is dramatically simplified while maintaining solubilization effectiveness.
Solution Approach 2:
Instead of using complex external devices to create micelles or liposomes, the invention inverts the approach by allowing the krill oil phospholipids to self-assemble into micellar structures spontaneously upon contact with water. This inversion from device-driven to material-driven micelle formation eliminates complex production equipment.
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 method achieves complete solubilization with stable, cost-effective, and health-friendly solutions suitable for a broad range of agents, allowing easy production and distribution in consumer-friendly units.
Implementation Method 1
A third solubilization mechanism are micelle and liposome application technologies. Herein the substance to be delivered is enclosed in a spherical aggregate of surfactant molecules. These molecules are characterized by a polar head group and a long nonpolar chain ('tail'). When given into an aqueous medium these molecules tend to associate by aggregating to spherical structures by orienting the polar head group towards the surrounding medium and the nonpolar chain towards the interior of the spheres.
Implementation Method 2
There is a variety of approaches for improving the solubility of such agents and in many cases also their bioavailability by using solubilization techniques. Herein the solubility of an agent in a medium is augmented by adding a third substance. These third substances are referred to as solubilizers (solubilizing agents), substances that may for example build a complex with the substance to be solubilized.
Implementation Method 3
Another mechanism of action of solubilizers is the augmentation of the dissolving capacity of the solvent, for example by disturbing the cluster structure of water. Examples for such structure breakers are glycerol (glycerin) and macrogols (polyethylene glycol, PEG).
Data Source
AI summary
The present invention relates to a method for solubilizing poorly water-soluble dietary supplements and pharmaceutically active agents by means of hill oil extract, to the solubilisate produced by this method and respective uses as a dietary supplement or pharmaceutical dosage form.