Water-Soluble Curcumin via Co-Crystal and Phospholipid Micelles

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Solution Overview

Problem

Curcumin's poor water solubility and low bioavailability limit its practical applications, despite its pharmacological benefits, due to its insolubility in water and reliance on organic solvents or synthetic emulsifiers that pose safety risks and flavor impacts.

Innovation Solution

A solvent-free method involving the formation of a curcumin-vitamin C-ascorbyl palmitate co-crystal, followed by high-speed emulsification and microencapsulation with a wall material, significantly enhancing water solubility and bioavailability without using synthetic emulsifiers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If curcumin is dissolved in organic solvents (n-hexane, ethanol, ethyl acetate) to improve solubility, then water solubility increases, but safety risks increase and solvent residues remain in products

Engineering Contradiction:
Improvewater solubilityVSAvoidsafety risk and solvent residues
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses phospholipids (such as soybean lecithin) as intermediary substances to form mixed micelles with curcumin. This mediator enables curcumin to be dispersed in water without requiring toxic organic solvents, thus improving water solubility while eliminating safety risks and solvent residues. The phospholipid acts as a bridge between the hydrophobic curcumin and hydrophilic water environment.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If synthetic emulsifiers (Tween, polyglycerol esters) are used to improve water solubility, then solubility increases, but product flavor is affected and usage is restricted by GB2760 standards

Engineering Contradiction:
Improvewater solubilityVSAvoidflavor impact
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent replaces synthetic emulsifiers with natural phospholipids that are safer and have fewer restrictions. The phospholipid-based mixed micelle system provides the necessary emulsification function without the flavor impacts and strict usage limits associated with synthetic emulsifiers like Tween, making it more suitable for food and pharmaceutical applications.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Reliability

If curcumin is used directly without modification, then the product is simple and safe, but water solubility remains poor and bioavailability is low

Engineering Contradiction:
Improvesafety and simplicityVSAvoidwater solubility and bioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent creates a composite material system consisting of curcumin-phospholipid mixed micelles. This composite structure combines the hydrophobic curcumin core with the hydrophilic phospholipid shell, enabling the material to maintain safety while achieving improved water solubility and bioavailability. The composite micelle structure allows curcumin to be delivered effectively in aqueous environments.

Inventive Principle:
Principle #40Composite materials

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 a 10 to 18-fold increase in bioavailability and excellent water solubility, verified through animal experiments, while being safer and more industrially viable than previous methods.

Implementation Method 1

dissolving curcumin, vitamin C and ascorbyl palmitate in an ethanol aqueous solution, evaporating ethanol under reduced pressure, and vacuum drying to obtain a curcumin-vitamin C-ascorbyl palmitate co-crystal

Methodology Applied
Scientific EffectCo-crystal formation: Crystallisation

Implementation Method 2

high-speed emulsifying the curcumin-vitamin C-ascorbyl palmitate co-crystal and a wall material colloidal solution under vacuum, sequentially conducting a two-stage wet grinding, a homogenization and a potential adjustment to obtain an emulsified body

Methodology Applied
Scientific EffectEmulsification: Emulsion

Implementation Method 3

evaporating ethanol under reduced pressure

Methodology Applied
Scientific EffectEvaporation under reduced pressure: Evaporation

Implementation Method 4

subjecting the emulsified body to microencapsulation with a wall material twice and drying to obtain the water-soluble curcumin mixture

Methodology Applied
Scientific EffectMicroencapsulation: Absorption (physical)

Data Source

PatentUS11642316B2Water-soluble curcumin mixture with high bioavailability and preparation method and application thereof
Publication Date: 2023.05.09 HENAN ZHONGDA HENGYUAN BIOTECH CO LTD
  • US11642316B2 patent drawing
  • US11642316B2 patent drawing

AI summary

A method for preparing a water-soluble curcumin mixture with high bioavailability includes the following steps: A) dissolving curcumin, vitamin C and ascorbyl palmitate in an ethanol aqueous solution, evaporating ethanol under reduced pressure, and vacuum drying to obtain a curcumin-vitamin C-ascorbyl palmitate co-crystal; B) high-speed emulsifying the curcumin-vitamin C-ascorbyl palmitate co-crystal and a wall material colloidal solution under vacuum, sequentially conducting a two-stage wet grinding, a homogenization and a potential adjustment to obtain an emulsified body; and C) subjecting the emulsified body to microencapsulation with a wall material twice and drying to obtain the water-soluble curcumin.