I have to prepare a 5mg/kg drug solution for animal study in rats. I have tried to dissolve berberine in DMSO and maintained it with PBS but failed to dissolve in a clear solution. Kindly suggest me. Thanks in advance.
Dear Vikas,
many thanks for sharing this interesting technical problem with the RG community. According to data sheets which are freely available on the general internet (e.g. Cayman Chemical), berberine hydrochloride is soluble in ethanol and DMF at ca. 500 μg/ml and ca. 25 mg/ml in DMSO. The solubility of berberine hydrochloride aqueous buffers such as PBS is much lower. In order to achieve the highest solubility in aqueous buffers, berberine hydrochloride should be first dissolved in DMSO to give a clear solution. This can then be diluted with the appropriate aqueous buffer (e.g. PBS). The solubility of berberine hydrochloride chloride) in a 1:4 solution of DMSO:PBS at pH = 7.2 has been reported to be 0.2 mg/ml. If necessary, minor insoluble particles can be removed by filtration, and the resulting clear solution should be used for subsequent studies on the same day.
I hope this helps. Good luck and best wishes, Frank Edelmann
Hi Dr Vikas Shukla . I hope the following link could help you:
Article Preparation and in vitro-in vivo evaluation of intestinal re...
Frank T. Edelmann Thanks for the response. I have to take 10mg in 1 mL solution (DMSO: PBS) for in vivo intravenous administration of berberine chloride. The maximum solubility of berberine chloride in DMSO is 25mg/mL but we can not use pure DMSO solution to dissolve the drug for animal work as far as toxicity concern. I have tried to dissolve but the solution has become suspended. Kindly suggest to me could I use the suspended solution for intravenous injection?
Aref Wazwaz Thanks for the response. I have to take 10mg in 1 mL solution (DMSO: PBS) for in vivo intravenous administration of berberine chloride. The maximum solubility of berberine chloride in DMSO is 25mg/mL but we can not use pure DMSO solution to dissolve the drug for animal work as far as toxicity concern. I have tried to dissolve but the solution has become suspended. Kindly suggest to me could I use the suspended solution for intravenous injection?
Dear Vikas, many thanks for your kind response and explanation. Berberine chloride is well known (imfamous?) for its low solubility and bioavailability. My suggestion would be to go just ahead and try intravenous injection of the suspension in DMSO / water provided that the particles are finely divided and evenly suspended. I assume that in this case an experiment is worth more than any further speculation.
Good luck and best wishes!
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