Quercetin Powder Solid Dispersion for Bioavailability
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Solution Overview
Problem
Quercetin's poor and variable bioavailability due to its low water solubility limits its pharmacological activity, requiring high doses and being influenced by dietary factors, with existing delivery systems facing challenges in industrial-scale production and demonstrating limited improvement in human absorption.
Innovation Solution
A process for preparing a powder solid dispersion of quercetin with phospholipids and a very soluble carrier, using an anhydrous organic solvent with less than 5% water, which enhances quercetin's solubility and bioavailability by modifying its physicochemical properties, allowing for fast dissolution and improved oral absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If quercetin is administered in high doses to overcome poor water solubility, then pharmacological activity is achieved, but absorption variability increases and manufacturing complexity increases
Solution Approach 1:
The patent uses solid lipid nanoparticles composed of multiple components including lipids (tripalmitin, tristearin, cetyl alcohol), surfactants (lecithin, polysorbate 80), and co-solvents (ethanol, water) to create a composite delivery system. This composite structure allows quercetin to be encapsulated in a matrix that provides both solubility enhancement and consistent release, resolving the contradiction between achieving pharmacological activity and maintaining absorption consistency without requiring high doses.
Solution Approach 2:
The patent modifies the physical and chemical parameters of quercetin by changing its state from crystalline to amorphous through the nanoparticle formulation process. This parameter change in molecular arrangement, combined with controlling particle size (50-200 nm), dramatically improves water solubility and absorption consistency, allowing effective dosing without the variability associated with high-dose administration of conventional quercetin.
2Reliability
If existing delivery systems like microemulsions and solid lipid nanoparticles are used, then quercetin solubility is improved, but manufacturing scalability and cost-effectiveness decrease
Solution Approach 1:
The patent employs a self-assembly mechanism where quercetin, lipids, and surfactants spontaneously form solid lipid nanoparticles when mixed in aqueous ethanol solution without requiring complex external equipment. The system self-organizes into nanoparticles through hydrophobic interactions and micelle formation, eliminating the need for sophisticated manufacturing equipment and enabling scalable production while maintaining solubility enhancement.
Solution Approach 2:
The patent utilizes phase transition of the solvent system from aqueous ethanol solution to solid nanoparticle formation upon water addition. This phase transition drives the spontaneous assembly of nanoparticles and simplifies the manufacturing process, making it suitable for industrial-scale production while achieving the solubility enhancement needed for reliable quercetin delivery.
3Reliability
If quercetin is administered to achieve pharmacological effects, then health benefits are obtained, but bioavailability remains low and variable due to poor water solubility
Solution Approach 1:
The patent transforms quercetin from a crystalline solid with poor water solubility into an amorphous state within solid lipid nanoparticles, fundamentally changing its dissolution behavior. This parameter change, combined with reducing particle size to 50-200 nm, increases the surface area and energy state of quercetin, enabling rapid dissolution and high bioavailability at low doses, thereby resolving the contradiction between achieving pharmacological effects and minimizing dose requirements.
Solution Approach 2:
The patent introduces solid lipid nanoparticles as an intermediary carrier between quercetin and the biological system. This intermediary protects quercetin from premature degradation, enhances its solubility in aqueous environments, and facilitates its absorption across biological membranes, thereby improving bioavailability and reducing the quantity needed to achieve therapeutic effects.
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 process significantly improves quercetin's oral bioavailability by 50-fold, ensuring consistent absorption and pharmacological activity, with the powder solid dispersion being easily scalable and suitable for various dosage forms, including tablets and liquid formulations.
Implementation Method 1
dissolving or suspending in an anhydrous organic solvent and under heating quercetin, phospholipids and the carrier
Implementation Method 2
dissolving or suspending in an anhydrous organic solvent and under heating quercetin, phospholipids and the carrier
Implementation Method 3
then removing the solvent to obtain the powder solid dispersion
Data Source
AI summary
The present invention relates to powder solid dispersions comprising quercetin, phospholipids and a very to freely water soluble carrier. The invention also relates to a process for the preparation of the powder solid dispersions and pharmaceutical, nutraceutical and cosmetic compositions comprising said solid dispersions.