If it doesn’t have alcohol or propylene glycol, then I would dissolve it first in transcutol, then mix it with the rest of your formulation. The transcutol is a better solvent/exipient for the rapamycin and would help it penetrate the skin.
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I’m not sure - I think it was the alcohol, or maybe the propylene glycol. It was many years ago I tried it. I just want to avoid both of those, so I’m going to make my own formulation based on tablets of minoxidil and the other compounds.
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Found the full-text of the article.
http://sci-hub.wf/10.1111/ics.12620#
or
Downloaded it. AVG antivirus says no malware.
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Hey @RapAdmin in the original paper, minoxidil strength is 0.5% but in the screenshot of tweets which you have shared, it says 5% minoxidil.
Which one is correct ?
Also there is a correction in original paper regarding the dosage of tacrolimus. It is 24 micrograms per ml, which comes around 2.4 mg per 100 ml. Is that right ?
Quote from original paper says 5mg/ml minoxidil.
The composition of RT1640 is cyclosporin A (1.2 mg/ml; Medisca
NDC # 38779-0660-01), minoxidil (5 mg/ml; Medisca NDC
38779-0574-05), and RT175 (120 ng/ml; manufactured for
RiverTown Therapeutics, Inc. by Hovione FarmaCiencia SA) diluted
in 50:30:20 propylene glycol:ethanol:H2O. The composition
of CsA is cyclosporin A (1.2 mg/ml) diluted in 50:30:20 propylene
glycol:ethanol:H2O.
Link to full text of article is below.
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I would totally pay a pharmacist or biologist to mix this for me to make sure it’s done the correctly LOL
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Hi there. First off, wanted to say thank you to the author for citing my articles on RiverTown Therapeutics. It’s very interesting to read this discussion and see the topics of CsA and FK506 being revisited for hair repigmentation. I’ve actually just published a new article on a company based in Korea who has developed a safer analog of FK506, I imagine it may be of notable interest to this community. I won’t post the link, but the admin is welcome to share it if they like to. Cheers
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Thank you so much for posting! Your instincts are correct. We would love to read that article.
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From what i have read the risk of topical tacrolimus is very low for people out of childhood.
Here is the follicle thought article
https://folliclethought.com/molgenbio-fk506-derivative-hair-growth-drug/
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Yes I prescribe tacrolimus all the time for eczema and other inflammatory skin conditions and consider it very safe. Its main disadvantage is that it only comes in a greasy ointment and not a cream, but there’s a compounded version we can order that comes in a cream formulation, has free 2-day shipping and only costs the patient 50 bucks. There’s also another calcineurin inhibitor (Elidel/pimecrolimus) that only comes in a cream form, but I don’t know if anyone’s done studies with it involving androgenetic hair loss.
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Tacrolimus powder is not dissolving in transcutol.
I have kept 1.4 mg tacrolimus powder in 3ml of transcutol, stirred it multiple times and its just lying there at the bottom like a lump from last 24 hours
Any ideas ? @RapAdmin
Perhaps we need to use ethanol for tacrolimus.
Tacrolimus is soluble in methanol, ethanol, acetone, ethyl acetate, and ether, and it is practically insoluble in water.
https://www.uspharmacist.com/article/tacrolimus-01-topical-microemulsion-43011
Also:
Solubility Soluble in DMSO (20 mg/ml), ethanol (30 mg/ml), acetone, ethyl acetate, diethyl ether or chloroform.
Source:
Water Solubility: Freely soluble in DMSO or ethanol. Poorly soluble in water. Soluble in dimethyl sulfoxide, ethanol, water, acetone, chloroform, ethyl acetate, ether, methanol and dimethyl formamide.
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I know little about compounding pharmaceuticals… but have been searching around and reading. I’ve found this information on Tacrolimus compounding (albeit for an oral solution, but perhaps there is some useful information in here. While ethanol is typically used in many of the scalp serums (as is typical with minoxidil formulations), I want to minimize the ethanol in my own preparations due to its negative effect on my scalp (causing itching and sores).
I will continue to look for more info on this issue. Here is what I’ve found so far - a short excerpt from a compounding pharmacy book:
Tacrolimus Formulations.pdf (326.4 KB)
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And for people who want to learn more about making ointments and pastes for skin and scalp:
Ointments and Pastes Compounding.pdf (7.8 MB)
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Thanks for sharing the info @RapAdmin. Unfortunately i have zero knowledge about chemistry and i am not sure if adding ethanol ( just 1ml in 60ml water base minoxidil) into the formulation would cause scalp irritation.
I’m pretty much in the same position as you. Lets hope someone with more knowledge than us can help and contribute in this effort to develop a low scalp irritation formulation of this hair tonic…
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I was about to order the pills for this and took a look at the paper. It looks like the quantities in the paper were:
*1.2 mg/ml cyclosporin
*5 mg/ml minoxidil
*120 ng/ml RT175
The unit for RT175 is in nanograms rather than milligrams, so this would correspond to 0.00012 mg/ml, or a total of 0.012 mg in your 100 gram or 3.5 oz mix.
This seems like a tiny amount and I wonder how it could make a big difference. Is it possible that the RT175 is more effective/potent than standard tacrolimus? I’m not sure how we could find this out since RT175 was formulated for the study. They seem to attribute the color regeneration to the RT175 in the paper.
Did you arrive at the 100 mg of tacrolimus in your mix using a different method? Am I reading the quantities in the paper correctly?
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Sorry - I may have made a mistake in my calculations - go with the paper data, but I also believe that there is a pretty wide range of dosing cited in the patent application made by RiverTown (see patent above). I’m just embarking on my effort to create this formulation and have yet to order the ingredients. Hope to move on this over the next week or two and will update the info when I have time. Nobody has done any work at figuring out the optimal doses of these different factors used in the formula - so at this early stage its still a lot of trial and error, and hopefully people will report their results and dosing protocols, concentrations used, etc.
RT175 is a derivative of Tacrolimus - when I spoke with David from Rivertown he didn’t say anything about RT175 being more effective/potent than tacrolimus, his pitch was more on the safety side (tacrolimus has slightly increased risk of cancer when used in young people, not a concern in this type of application though - so I suspect David is hyping the risk factor to make the RiverTown formulation have more perceived value).
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Maybe Melissa L. Harris can help you out?
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Since the quantity is so small, it would probably make sense to order the 0.25 mg tacrolimus capsules, which are the smallest I see for sale on Indiamart. In a 100 ml solution, this would still be about 20x the amount used in the paper. A single strip of 10 tacrolimus tablets would be a ~10+ month supply and cost less than a few dollars.
Has anyone talked about a minimum dollar amount when ordering from Indiamart? Perhaps you’d have to by something like $20 or $50 of tacrolimus to make it worth their time, even though it’s orders of magnitude more than you’d need based on the paper quantities.
