Home Cosmetic Science Talk Formulating Help on formulating this hair-loss serum? 2 possible actives

  • Help on formulating this hair-loss serum? 2 possible actives

    Posted by ETcellphone on November 23, 2020 at 3:31 am

    So I want to formulate this hair loss serum. The active ingredients called for are azelaic acid or zinc sulphate (I could also combine the two in a serum if I wanted). I will link the study I reference right below here. It is an in vitro study. 

    https://pubmed.ncbi.nlm.nih.gov/3207614/

    The study says:

    “When added at concentrations of 3 or 9 mmol/l, zinc was a potent inhibitor of 5 alpha-reductase activity. At high concentrations, zinc could completely inhibit the enzyme activity. Azelaic acid was also a potent inhibitor of 5 alpha-reductase; inhibition was detectable at concentrations as low as 0.2 mmol/l and was complete at 3 mmol/l”

    Anyhow, I don’t understand how to convert the measurements of the actives. 
    I don’t know how to convert mmol/l to grams, or even know if that is possible. Do you know how to convert this? 

    Their solubility:
    - Online it says azelaic acid is soluble in glycerin and glycol at a concentration of 0.5-1.5%
    - zinc sulfate I cannot find information on concerning solubility. 

    Do you think in a formula using the Azelaic acid, I would need to use an alcohol to enable the azelaic acid to penetrate the scalp? I’m unsure of how many grams of propylene glycol I would need to dissolve the azelaic acid in as well. I’m more interested in using Azelaic acid I guess, since it in general is a great skincare ingredient. 

    Leo replied 4 years ago 4 Members · 3 Replies
  • 3 Replies
  • suswang8

    Member
    November 24, 2020 at 4:02 am

    Friendly note that these tests were done in vitro, not in vivo, so no one has any idea how this would align to the concentration you should use on the skin.  We know that azelaic acid is currently in use at 15-20% in prescription formulations, so consider that as one data point to consider.  Perhaps you could experiment with 5% or so?  Topical zinc sulfate has been used at 5% concentration in at least one study.  These are just guesstimates as to what you could consider using, not taking into account other actives you might want to use.  Keep in mind that hair loss/growth is an extremely complicated science, hence the reason the FDA has approved literally one topical treatment during the last 30 years.  

    The others can advise you about formulation, but keep in mind that the more alcohol/propylene glycol that you use, the more irritating the formulation will tend to be.

  • chemicalmatt

    Member
    November 24, 2020 at 9:18 pm

    Azelaic acid average mass = 188 Da = 188g/L, so 1 mmol = 0.188g/L or ~ 0.02% w/w, so 5 mmol ~ 0.10% w/w. Should be soluble in butylene glycol, but add a little ethoxydiglycol to co-solvate and for dermal penetration. Leave the ethanol in the vodka bottle. Hope this helps. 

  • Leo

    Member
    November 25, 2020 at 4:48 am

    A key issue related to this invitro study is the same key issue that applies to all ingredients that are tested in vitro—-as per the authors, “if this inhibition is confirmed in vivo.” 

    Even if confirmed in vivo and given that over 99.99% of in vitro ingredient claims are NOT confirmed in vivo, you are NOT legally able to use any hair claims that are associated with growth or functional hair loss unless the FDA approves. 

    Please also note that the authors published this work over 30 years ago and they make NO reference to hair.

    I am not saying that the information is incorrect but why proceed with this venture.

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