Curcumin Nanococrystal Composition for Injectable Water Solubility

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Solution Overview

Problem

Existing methods for enhancing the solubility and stability of highly lipophilic drugs like carvedilol and curcumin are inadequate, limiting their use in injectable forms due to insufficient solubility and stability, especially for intravenous administration.

Innovation Solution

The development of nanococrystal formulations comprising curcumin, a coformer, and a stabilizer, with particle sizes less than 10 nm, which are synthesized using solvent-diffusion and solvent-evaporation techniques, and stabilized with lyoprotectants to enhance solubility and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If salt formation is used to increase solubility, then solubility is improved, but it is restricted to ionizable relatively weak acids and bases

Engineering Contradiction:

ImprovesolubilityVSAvoidapplicability to drug types

Core Design Contradiction:

Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical form of the drug from crystalline to amorphous state, and forms inclusion complexes with cyclodextrins, fundamentally altering the physical and chemical parameters to achieve solubility enhancement without being restricted to ionizable drugs

Inventive Principle:

Principle #35Parameter changes

2Speed

If micronization is used to improve dissolution rate, then dissolution rate is improved, but equilibrium dissolution remains unchanged

Engineering Contradiction:

Improvedissolution rateVSAvoidequilibrium dissolution

Core Design Contradiction:

SpeedVSQuantity of substance

Solution Approach 1:

The patent transforms the drug from crystalline to amorphous form, which has higher energy state and solubility, and creates nanosized particles with significantly increased surface area, thereby improving both dissolution rate and equilibrium dissolution simultaneously

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If complex formation by cyclodextrins is used to increase solubility, then solubility is improved, but permeability of drugs decreases

Engineering Contradiction:

ImprovesolubilityVSAvoidpermeability

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent segments the drug into nanosized particles (1-100 nm), which provides such a high surface area to volume ratio that the permeability issue caused by cyclodextrin complexation is overcome, allowing both high solubility and maintained permeability

Inventive Principle:

Principle #1Segmentation

4Stability of the object's composition

If crystalline forms are used, then stability is improved, but solubility is low

Engineering Contradiction:

Improvephysical stabilityVSAvoidwater solubility

Core Design Contradiction:

Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The patent changes the physical state from crystalline to amorphous, which has higher solubility due to higher energy state, while using spray drying and freeze drying techniques along with stabilizers to maintain physical stability of the amorphous form during storage

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 nanococrystal compositions significantly increase the water solubility of drugs like carvedilol by 1500 times and curcumin by 16000 times, providing stable formulations suitable for intravenous administration.

Implementation Method 1

pharmaceutical nanocrystals (NCs) are colloidal dispersions of sizes less than 1000 nm

Methodology Applied

Scientific EffectNanocrystal formation: Nanocomposite

Implementation Method 2

cocrystals (CCs) have shown great capabilities to modify drugs' physicochemical properties

Methodology Applied

Scientific EffectCocrystal formation: Crystallisation

Implementation Method 3

synthesized using solvent-diffusion and solvent-evaporation techniques

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 4

synthesized using solvent-diffusion and solvent-evaporation techniques

Methodology Applied

Scientific EffectEvaporation: Evaporation

Implementation Method 5

forming a nanococrystal dispersion by mixing the first solution with a second solution

Methodology Applied

Scientific EffectPrecipitation: Precipitation

Implementation Method 6

stabilized with lyoprotectants to enhance solubility and stability

Methodology Applied

Scientific EffectFreeze-drying: Freeze Drying

Implementation Method 7

stabilized with lyoprotectants to enhance solubility and stability

Methodology Applied

Scientific EffectLyoprotection: Preservative

Data Source

PatentUS12533326B2Preparation of soluble form of curcumin

Publication Date: 2026.01.27 SALAMAT PAJOOHAN PARSIAN PHARMED

AI summary

A curcumin nanococrystal composition including curcumin, a coformer, and a stabilizer. The coformer may include at least one of 3,5-dinitrobenzoicacid, gentisic acid, phloroglucinol, 4,4-bipyridine, tartaric acid, citric acid, and gallic acid. The curcumin nanococrystal composition has a particle size less than 10 nm, and the curcumin has a water-solubility between 5 mg/ml and 20 mg/ml.