How to improve the solubility of Andrographolide in water?
Andrographolide is a diterpene lactone found in the medicinal herb Andrographis Paniculata (Burm.f.) Nees, a medicinal plant that has been used for centuries in South Asia. Andrographolide is the main bioactive constituent of the Andrographis extract, it dissolves in boiling ethanol, slightly soluble in methanol or ethanol, but the solubility of andrographolide is not so good as it in methanol, it is almost insoluble in water.
The experimental aqueous solubility is 3.29ug/mL(SD0.73), while water is the most convenient and best price solvent, we need to figure out some methods to increase the dissolved quantity of andrographolide in water.
How about increasing the temperature of the solution?
Research on the solubility of andrographolide in water was made under 5 different temperature conditions and showed that the soluble possibility increased as the temperature increased, the highest solubility at 45℃ is at 0.103±0.012mg/mL. This does not change the rule in water not as in boiled ethanol, this changes.
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.
Will the solubility change when an ultrasonic wave is applied?
Ultrasonic does help to mix the substances in the solvents and get the balanced solution, it does not help to dissolve the andrographolide in water.
Is it workable to improve the dissolving quantity in water with other solvents?
Yes, it is practically workable to increase the andrographolide solubility in water with other solvents. An easy one is to promote solubility with DMF by two steps, this increases approximately 0.5mg/ml in a 1:1 solution of DMF: PBS(pH 7.2). The steps are as follows：
🎯Firstly, dissolving Andrographolide in DMF,
🎯then diluted it with the water/aqueous buffers.
If the former one is not satisfactory to you, you may try the water-soluble andrographolide derivatives.
Andrographolide derivatives are also NF-κB inhibitors, the same as andrographolide. They are developed to solve the water solution by adding different salts to andrographolide. They are mainly applied as injections to treat upper respiratory tract infections, pneumonia, bacillary dysentery, and other syndromes.
The available water-soluble andrographolide derivatives are Yanhuning, Chuanhuning, Lianbizhi, and Xiyanping, and Yanhuning(intermediate/API) is the one with the most commercial batch and easy to access.
🎯Yanhuning originates from andrographolide and is generally composed of 4-Dehydroxy-11,12-Didehydroandrographolide-3,19-Disuccinic acid half ester potassium sodium salt monohydrate.
🎯While Chuanhuning is the semi-products during the semi-synthesis of Yanhuning, it is primarily composed of 14-dehydroxy-11,12-didehydroandrographolide-3,19-disuccinic acid half ester monopotassium salt. It (intermediate/API) is commercially supplied in China.
🎯Xiyangping is the trade name of the Andrographolide Sulfonate. The Xiyangping is one of the official treatments for severe covid-19 in China.
🎯Lianbizhi is also a trading name for an injection of Sodium bisulfate andrographolide. This injection has also been used clinically to treat pneumonia and yielded better results than those achieved with azithromycin. Meanwhile, Sodium bisulfate andrographolide is one of the metabolites in Studies of andrographolide metabolites in rats. And this derivative (intermediate/API)) is accessible in China
Another thing that may relate to the water solubility of andrographolide is getting a clear andrographolide solution for in vivo research.
This can be achieved by applying DMSO, and adding each solvent one by one, the solubility shall be at least 2.5mg/mL.
🎯10% DMSO 40% PEG300 5% Tween-80 45% saline
🎯 10% DMSO 90% (20% SBE-β-CD in saline)
🎯 10% DMSO 90% corn oil
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