Would Transdermal Rapamycin Cream be better than oral administration?

First I want to thank RapAdmin and all of the frequent contributors to this site. It is truly appreciated. I am strongly leaning towards purchasing Rapamycin and came across this transdermal product in the link below. Wondering if anyone has used the transdermal rapamycin, or for those who haven’t used it, what are your thoughts. Thank you in advance.

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As of a few minutes ago, the price was $135 for120mg rapa in 20ml transdermal gel. This is a very good price.

Hi Paula, welcome to the forum and thanks for posting.

I sat the rapamycin topical cream and the rapamycin oral tablets as two completely separate items, targeting different issues. The oral tablets are best for systemic administration of rapamycin, and gets to the blood and organs and brain relatively well it seems.

The topical cremes really only target the top layers of skin as I understand it - so it might help your skin (I made my own rapamycin skin cream according to the guidelines in the papers we reference in this discussion thread) and it worked OK, but nothing fantastic.

According to this paper - the topical rapamycin creme (at least the one they used) does not result in any significantly measurable amount of rapamycin in the blood stream. As they say here:

No blood samples collected contained detectable levels of rapamycin as assessed by LC/MS/MS analysis (limit of detection, 1 ng/ml)

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Rapamycin.store sells two creams. One is a cosmetic cream. The other is a transdermal cream meant for systemic absorption.

Interesting - I’ve never seen anything like that before, for rapamycin.

I would want to see some independent third party validation or clinical studies that this type of product is effective at raising blood sirolimus levels in a cost-effective manner before I’d consider purchasing it. I wouldn’t trust any vendor just “telling me” that it does this, given the many problems of bioavailability of rapamycin we’ve seen.

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They post lab results for the transdermal cream on this page.

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Lab reports shows 5 ng/L in blood.

“Apply the desired amount…once weekly”.

I wonder the cream, “amount” of rapamycin dosed, and how long after dosing was test taken to achieve this level? Surely, the peak level was higher.

Given the huge benefit of bypassing the first pass stomach/intestine loss, it could very well be extremely potent at small doses vs oral.

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Hormone replacement and many medications can be delivered transdermal. It depends on what delivery agent you use. It would be good to get Dr. Ross to weigh in @DrRoss. My concern is that we barely know what we are doing now with oral dosing, so at least some guard rails of common sense would help before everyone switching to transdermal. If we can at least agree on what systemic levels seem to be desirable and match those levels with transdermal, it would create some advantages over the oral dosing.

Indeed, there’s a lot of debate/discussion between DSMO, Transcutol, and likely many others, but clearly, there is a pathway to deliver rapamycin transdermal. Shouldn’t be a surprise, just pushing the envelope.

We have no idea, we are all guessing. Dr G and Dr B are all over the map. The transdermal matching is just trial/error experimenting.

Bypassing oral has HUGE advantages re availability and consistency. The issue is the pros/cons of the method of delivery. In many mice/rapamycin studies, ip injection was routinely used and demonstrably showed high efficacy vs NO response from oral gavage. If one is going to accept transdermal for systemic, then why not intramuscular*, routinely used for other hormonal deliveries in humans?

*not a health professional, not advocating

@mac. Agree with all your points. Sub cutaneous injection would even be easier. First pass effect can cause issues but can also be a benefit. The gut microbiome may help and or hinder Rapamycin. Love the thoughtful discussion though!

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We are in new territory. I am not aware of any studies that have evaluated and reported on rapamycin plasma levels in people who are taking rapamycin once weekly as opposed to daily. In some studies for unique medical conditions, the authors have aimed for plasma levels of 2-10 mg/mL. I’m interested to hear what other practitioners have to say on this topic.

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Something else to consider, and you mean post absorption and metabolization…do the metabolites interact with rapamycin for a BENEFIT? That’s another rabbit hole…I cannot keep up.

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There are literally hundreds of studies on cancer/transplant people taking rapamycin DAILY…unless you meant “healthy”, then yes. Therapeutic for these cohorts is 5-20 ng/mL.

Mac, you may have misread Dr Ross’ response. He’s saying there’s a paucity of published data on the pharmacokinetics of weekly administration of rapamycin versus daily administration.

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You are correct, my bad. But look through the posts for the seminal cancer/GFJ study, ALL weekly administration with almost 140 people, albeit cancer patients. Lots of data on side effects, we’ve already covered.

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Although it takes getting used to, I can attest that intramuscular injections (insulin, in my case) are no big deal. Show me a good product, and I’d do it (cautiously, as if starting over with rapa).

I take TRT IM, stay tuned….… :wink:

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Exactly! so many questions come to mind when I look at the lab test. How much cream was used, where was it placed, how long afterward administration/application was the lab test done, what does the AUC curve look like for this administration.

Seems like this method could be helpful, and it someone wanted to try it and do blood / sirolimus level tests it seems like it might be interesting - test 8 hours after applying, then daily for a week?

More opportunities for experimentation if you are interested in doing it.

Of all possible means of administration - this one seems the least researched, so people would be really flying blind here…

Someone should just ask these folks…I recall good technical discussions with them. I am one of those “some customers report poor oral bioavailability”

They seem like a very legitimate vendor just hopping on the Rapamycin bandwagon.

For Rapamycin yes, but as a general method of delivering drugs, vast precedence. These folks might already have some good clinical experience/data.

This is all good imho…more mainstream clinical experimentation.

Rapamycin IS a safe drug…you have to take a lot of it, you get side effects warning, and symptoms reverse when you stop. Thousands of people have been taking some mega doses in various trials, I don’t ever recall reading “death” as a DLT.

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So we are getting deep into the forrest, but to continue that theme further. Has anyone studied the Rapanuai people to see what blood levels of Rapamycin levels they have. I believe it was found in the soil. Did they have some in their food, get some injected through the skin by walking on the soil with bear feet and did they have any other “super powers” other than avoiding tetanus?

Delivery method is so interesting. Even more interesting is what other things may Rapamycin may be effecting other than just mTOR? The simplistic view of slowing aging by turning off mTOR seems to not give enough credit for more that Rapamycin may be doing and the journey of how it gets to the cells may play a part in that. Estrogen given orally has been found to increase clotting factors in the liver, but it also helps lower LDL. If you give estrogen transdermal in has minimal to no effect on clotting factors, but also no effect on LDL lowering. Looking at the whole process is almost like trying to solve a Rubik’s cube, each move can have an effect on multiple sides. For now, getting blood levels to some level that turns off mTOR1 and not mTOR2, seems to the less cluttered path. My reduction of basic pains and aches that I attributed to aging, is worth so much to me to take some risks.

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