Andrographolide solubility is good? Is it water-soluble?

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What is Andrographolide?

You must care about the andrographolide solubility much as andrographolide has benefits in pharmaceutical, cosmeceutical, and nutraceutical.

Andrographolide, as an active compound of Andrographis extract, is used for common cold and flu, upper respiratory infections, osteoarthritis, fighting covid-19, and more.

Andrographolide is a constituent found in the herb Andrographis Paniculata, a yearly herb native to South Asia, which has a long medical history in China, India, Thailand, and other Asian countries. The main reason for the name King of Bitters of the herb is from Andrographolide, it is extremely bitter. 

Based on Andrographolide structure, the mechanism of Action is extensively studied, and the effects on cell signaling, immunomodulation, and stroke have already been studied. Is the active ingredient Andrographolide easily dissolved in different solvents?

Andrographolide crystal(purifed andrographis extract) with herb andrographis

Is there data on the solubility of andrographolide in various organic solvents?

Labdane diterpenoid Andrographolide is soluble in boiling ethanol, DMSO, and DMF, slightly soluble in methanol or ethanol, and very slightly soluble in chloroform, according to practices in past five decades.

The quality of andrographolide being soluble in DMSO and DMF.

In DMSO, andrographolide dissolves 25mg per ml(25mg/ml), this may rise up to 100mg/mL(285.35mM) by using Ultrosonic.

In Dimethyl formamide/DMF, 1ml DMF dissolves 14mg andrographolide.

Is andrographolide possible to be soluble in other organic solvents?

Chen Lingli(Ling-li,Chen. 1673-4610(2010)0100041-03) team compared the andrographolide solubility in solvents of n-Butanol, Ethyl Acetate, Glycerin, Chloroform, Methanol, and Absolute Ethanol.

🎯The first step for them was the preparation of three copies of the said solvents respectively.
🎯 The Second step was to add andrographolide, dissolving to supersaturated, shaking them to well mixed.
🎯Thirdly incubated the solutions in a water bath and kept the constant temperature at 37 ℃ for 12hrs to make them dissolve in equilibrium.
🎯The fourth step was to take the solutions out and kept 4 Hrs at room temperature. Then 4Hrs later, got appropriated amount and diluted with methanol to a fixed volume and filtered with 0.45 um microporous membrane.
🎯 Finally, the last step was to test the solubility with HPLC. They gained the results in
sheet 1.

Sheet 1 The Soluble quantity of Andrographolide in organic solvents(X Bar±s,n=3).

Solvents

Solubility(mg/ml)

Solvents

Solubility(mg/ml)

n-Butanol

8.079±0.365

Glycerin

0.677±0.183

Ethyl Acetate

2.483±0.380

Chloroform

0.213±0.241

Absolute Ethanol

7.925±0.561

Methanol

14.461±0.620

Will Andrographolide be soluble in Oil Phase?

We get this answer from Chen Linli team again. They developed research to find whether andrographolide is soluble in soybean oil and tea oil. And the following Sheet 2 shared the results.

Sheet 2   The dissolved quantity of  andrographolide in oil(X bar±s,n=3).

Oil

Soybean Oil

Tea Oil

Solubility(mg/ml)

3.827±0.011

3.287±0.023

Is Andrographolide soluble in water?

Research on the solubility of andrographolide was made under 5 different temperature conditions and got to understand the soluble possibility increased as the temperature increased as sheet3. As we see, the soluble quantity of Andrographolide in water is generally less than 0.1mg/mL. Therefore, the andrographolide is practically insoluble in water.

Sheet 3 Water solubility of Andrographolide at different temperatures (X bar±s, n=3).

Temperature

Room temperature(22℃)

30℃

37℃

40℃

45℃

Solubility(mg/ml)

0.069±0.010

0.059±0.007

0.072±0.007

0.082±0.009

0.103±0.012

We get to find out that the dissolved quantity of andrographolide  is relatively higher in Methanol than in other organic solvents, and the solubility in oil is 50 folds than that of water. These data shine light on andrographolide applications for formulations in skin care products and dietary supplements, and daily testing. Anyway, how to make andrographolide more soluble in water? Is there any solution to improve the solubility in water?

How to dissolved more andrographolide in water?

To have a better solubility of andrographolide in water or aqueous buffers. We should go two steps.

🎯Firstly, dissolving Andrographolide in DMF,
🎯Then diluted it with the water/aqueous buffers.
By this method, the dissolved andrographolide is promoted to approximately 0.5mg/ml in a 1:1 solution of DMF:PBS(pH 7.2). Do remember to use this aqueous andrographolide solution in one day.

OR try the water-soluble andrographolide, the andrographolide derivatives:
🎯Yanhuning  
🎯Andrographolide sulfote

Reference

1.     https://cdn.caymanchem.com/cdn/insert/11679.pdf

2.     https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7122281/

3.     https://www.medchemexpress.com/andrographolide.html

4.     Ling-li,Chen.1673-4610(2010)0100041-03

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