#456

Thank you so much for that, i will get that scale.

We keep in touch about out Sirolimus creams!! :wink:

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#457

Thanks for your gentle course correction for me, @Brett_Miller ā€” I never claimed I was smart, only educated.

Well, hopefully this will help someone who was considering it. Itā€™s exactly what I would have done if I trusted powder.

Iā€™m looking forward to hearing more on the cream.

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#458

Apologies if this has been addressed somewhere regarding the impact on coating. The coating of the tablets I take are sugar, Pfizer variety. Is this an issue for making?

#459

Not sure what you mean. What brand of rapamcyin / sirolimus are you using - Pfizer rapamune? The Pfizer brand product uses a special nanocrystal technology - see this thread: Rapamycin and NanoCrystal Formulations

I suspect that using Pfizer rapamune may not be the best option for creating the topical cream (it would also be un-necessarily expensive). Iā€™m not sure how the nanocrystal pills break up when you crush them, and how that might absorb into the skin, even with transcutol or DSMO.

I personally use either the sirolimus powder, or the Zydus or Biocon brand rapamycin tablets.

#460

Iā€™m taking Pfizer from Australia and it clearly says they are sugar coating Sucrose and Lactose monohydrate.

#461

Yes - The Rapamune ingredients are:

RAPAMUNE Tablets: sucrose, lactose, polyethylene glycol 8000, calcium sulfate, microcrystalline cellulose, pharmaceutical glaze, talc, titanium dioxide, magnesium stearate, povidone, poloxamer 188, polyethylene glycol 20,000, glyceryl monooleate, carnauba wax, dl-alpha tocopherol, and other ingredients. The 0.5 mg and 2 mg dosage strengths also contain yellow iron (ferric) oxide and brown iron (ferric) oxide.

from here: https://labeling.pfizer.com/ShowLabeling.aspx?id=139§ion=MedGuide#:~:text=Inactive%20ingredients%3A%20RAPAMUNE%20Tablets%3A%20sucrose,dl-alpha%20tocopherol%2C%20and%20other

So you are right - but I donā€™t think that coating matters in the formulation of a topical mixture.

If youā€™re using this to create cream youā€™ll be crushing the tablets, and then disolving the mixture in transcutol or DSMO or something similar.

The key issue is how the nanocrystal technology works when the pills are crushed and powder dissolved. Thats beyond my pharmacokinetic knowledge.

Try it and see if it helps your skin. Thats probably the easiest way to move forward.

2 Likes
#462

I have the liquid version has any one tried to apply the liquid directly to the face with good result ? I cannot swallow pills

#463

Itā€™s not that easy to calculate because the weight of 500 ml depends on the substanceā€™s density. If the substance has a density of 1 g/mL (which is often the case for water), then 500 ml would be 500 grams. But we are not using water here. For other substances, like Rapa mixed with transcutol, the weight may differ. We need a pharmacist to help with calculation :blush:

#464

I used a nail drill and sandered the yellow coating off, with not too much loss. Worked well.

2 Likes
#465

What do you guys think? Any reason why I should not get them? It is from my local pharmacy.

Sirolimus 1.0% Cream/Ointment:15g $69.95, 30g $109.95, 60g $189.95 (AUD). Divide by 1.5 to get USD.

From what I can see I canā€™t make the 60g bottle without at least $180usd of rapamycin tablets.

Any disadvantage for using cream or ointment? I should ask for cream isnā€™t? I get more with cream because of the lighter density.

Is there a shelf life?

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#466

So I finally thought I may want to make a Rapa cream - just couldnā€™t find the motivation to do so the past years. Then I read this post of Rapadmin. Has this ever been discussed, as it seems like a decent concern to me? I havenā€™t been able to find more research on this, but admittedly thus far Iā€™ve only done a quick search. I wouldnā€™t look forward to wasting time making such a cream, only to break down the ECM.

Source: Rapadmin.
ā€œBut there is also research that suggests rapamycin may not be that good for the skin, increasing inflammatory markers (which is not a good sign), and triggering a breakdown of the extracellular matrix:ā€

"Rapamycin is a long studied molecule affecting mTOR/nutrient signaling and has recently been shown to decrease P16 levels of aging skin21, therefore it was chosen as a positive control of senotherapeutic effect in aging skin models. " ā€¦ ā€œRapamycin induced a significant increase in P16 expression, a trend towards increased expression of inflammatory markers (IL6 and IL8), and a significant decrease in Keratin 1 gene expression levels (Fig. 3B). In the dermis, peptide 14 treatment promoted a significant reduction in B2M gene expression, a pro-aging factor, as well as in the expression ofIL8. Rapamycin treatment induced no significant changes in these markers and increased Matrix Metalloproteinase-1 (MMP1) gene expression, indicative of breakdown of the extracellular matrix (Fig. 3C).ā€

Source:
https://www.biorxiv.org/ā€¦/10.1101/2020.10.30.362822v2.full

#467

Yes - I still wonder about that statement from the OneSkin team. The caveats are that they only tested a single dose level of rapamycin (and were making no attempts to optimize the performance of rapamycin in skin aging), they were only using it as a ā€œcontrolā€ to compare their own compound against. But never-the-less, some pros and cons given what weā€™ve seen in the research.

My approach is still to use pulsed rapamycin cream - 3 or 4 months on, then off for a few months. If anything is going south (a negative impact on my skin) I should notice it.

We donā€™t know how important these specific Interleukins are in skin aging. Perhaps P16 is more important than the IL6 and IL8).

We also know that IL-17 seems to be important: A proteĆ­na IL-17 desempenha um papel importante no envelhecimento da pele, terapias aprovadas pela FDA disponĆ­veis

4 Likes
#468

Thanks! Have you, or any other members, observed any changes in your skin at all, after using Rapamycin cream? Do you add a preservative, on another note, in your transcutol-Rapamycin cream?

#469

So, Iā€™ve been using the Rapa cream nearly 6 weeks 1-2 times per day, and I find it very drying. Up to the point that it is causing redness that is lasting days. I had to stop using it for a few days.

I assume itā€™s the transcutol causing that, after going over some studies that suggest it may increase transepidermal water loss. I only use 5% transcutol. (And 0.2% Rapa). (A company apparently selling Rapa cream mentions dryness can sometimes occur but that it will disappear after 1 week. Thatā€™s definitely not the case for me Topical Rapamycin - #15 by BandolsMom - Rapamycin - Healthspan)

Has anyone else been running into such issues with dryness? Iā€™d reduce the transcutol as I still think thatā€™s probably the culprit, but at 5% itā€™s already a low concentration. And Iā€™d think I canā€™t get the rapa to dissolve well enough if I reduce it even further.

Edit: reading through this thread again Iā€™m now wondering if it is the Rapamycin causing the dryness. As others donā€™t seem to be having any issues with Transcutol in apparently much higher dosesā€¦ Thatā€™s surprising to read. I did use generous amounts of the Rapa cream twice per day, perhaps that is a problem. And Iā€™ve been using an oil base to simplify the process. Perhaps the Cerave cream Rapadmin uses to mix in the Rapa/Transcutol-mixture has ingredients that counteract TEWL more effectively.

#470

What did you mix the rapamycin/transcutol formula with? I have no issues with my CeraVe based cream.

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#471

Thanks Rapadmin, I use a simple oil as base cream (sweet almond oil). I felt keeping the base cream simple, increases the chances that the Rapa doesnā€™t oxidise affecting its stability and efficacy. I also donā€™t doubt the efficacy of the Rapa, but the dryness makes it far from ideal. Iā€™ll need to use it (far) less often, and probably use an occlusive cream or something on top.

I was using a rather thick ā€˜layerā€™ of it twice per day - going to tone that down also. Iā€™ll let the Rapa cream sink in for 30mins, then use an occlusive to seal. Iā€™ll see if that avoids this dryness/redness.

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#472

Much higher proportion of transcutol here (~30%) and no cream/oil. I havenā€™t noticed drying in particular in the areas I use it.

3 Likes
#473

Thanks so much for sharing, Sol. If you donā€™t mind me asking: how long have you been using Rapa cream, and have you noticed any effects at all?
The transcutol may indeed not be the culprit after all.

#474

This sounds like an attempt to sell their product. I would love to see long term study of rapamycin skin cream optimized for absorption and performance. For 2+ years, Iā€™ve used my own rapamycin skin cream based on recipes discussed in this forum, with no ill effects and probably some minor good effects.

#475

A year. Alas, no clear results, not for pigmentation, skin quality, nor toenail fungus. These things take time, so Iā€™ll continue, but I was hoping for faster and clearer outcomes.

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