Curcumin Phospholipid Complexes for Bioavailability

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Solution Overview

Problem

Curcumin's low bioavailability due to extensive metabolism limits its effectiveness as a cancer chemopreventive agent, as plasma and tissue concentrations remain low despite high oral doses, making it impractical to increase dosages further.

Innovation Solution

Phospholipid complexes of curcumin are formed by dissolving curcumin in a protic solvent, such as ethanol, with phospholipids like soy phosphatidyl choline, under reflux and concentration, enhancing curcumin's bioavailability by forming complexes that increase systemic levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If the oral dose of curcumin is increased to achieve higher plasma concentrations, then the bioavailability may be improved, but it becomes impractical and undesirable due to the already high doses investigated

Engineering Contradiction:
Improveplasma concentration of curcuminVSAvoidpracticality of dosing
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

Phospholipids serve as an intermediary substance that forms complexes with curcumin, facilitating its absorption and transport in the bloodstream. This mediator enables curcumin to achieve higher plasma concentrations without requiring impractically high oral doses, as the phospholipid complex protects curcumin from metabolism and enhances its bioavailability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite material by combining curcumin with phospholipids in specific ratios (1:1 to 1:10 w/w). This composite curcumin-phospholipid complex exhibits improved pharmacokinetic properties compared to pure curcumin, allowing effective plasma concentrations to be achieved with practical oral dosing

Inventive Principle:
Principle #40Composite materials

2Reliability

If curcumin is administered orally to achieve cancer chemopreventive effects, then the therapeutic benefit may be obtained, but the extensive metabolism by conjugation and reduction pathways limits the plasma and tissue concentrations achieved

Engineering Contradiction:
Improvecancer chemopreventive efficacyVSAvoidplasma and tissue concentrations
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The phospholipid complex is formed before curcumin administration, creating a protective structure that prevents extensive metabolism by conjugation and reduction pathways. This preliminary complexation action ensures that curcumin reaches plasma and target tissues in its active form, maintaining both efficacy and adequate concentrations

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention changes the physical-chemical parameters of curcumin by forming complexes with phospholipids. This complexation alters curcumin's solubility, stability, and resistance to metabolic degradation, enabling it to maintain higher concentrations in plasma and target tissues while retaining its chemopreventive activity

Inventive Principle:
Principle #35Parameter changes

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 phospholipid complexes of curcumin achieve five-fold higher peak plasma levels and area under the plasma concentration time curve compared to uncomplexed curcumin, significantly improving bioavailability and potential chemopreventive efficacy.

Implementation Method 1

dissolving curcumin in a protic solvent, such as ethanol, with phospholipids like soy phosphatidyl choline

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 2

phospholipid complexes of curcumin are formed by dissolving curcumin in a protic solvent

Methodology Applied
Scientific EffectComplex formation:

Implementation Method 3

under reflux and with stirring

Methodology Applied
Scientific EffectReflux:

Implementation Method 4

The resulting suspension is concentrated under reduced pressure to a residue

Methodology Applied
Scientific EffectEvaporation under reduced pressure: Vacuum Distillation

Data Source

PatentUS10603329B2Phospholipid complexes of curcumin having improved bioavailability
Publication Date: 2020.03.31 INDENA SPA

AI summary

The present invention relates to novel phospholipids complexes of curcumin or extracts containing it having improved bioavailability.