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Would Transdermal Rapamycin Cream be better than oral administration?

Posted on June 23, 2022 By admin No Comments on Would Transdermal Rapamycin Cream be better than oral administration?


Paula


June 23, 2022, 3:06 pm


# 1

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 have not used it, what are your thoughts. Thank you in advance.

Rapamycin Buyers Group

Transdermal Rapamycin Cream – Rapamycin Buyers Group

Our custom formulated low dose transdermal Rapamycin cream containing 120mg Rapamycin. Transdermal delivery is a perfect way to deliver Rapamycin into the body as it bypasses the digestive system which can breakdown rapamycin. This type of delivery …

Est. reading time: 1 minute


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 creams 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 cream (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)


Vlasko


June 23, 2022, 5:51 pm


# 4

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.

I would like 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 would not trust any vendor just “telling me” that it does this, given the many problems of bioavailability of rapamycin we’ve seen.


Vlasko


June 23, 2022, 6:26 pm


# 6

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


MAC


June 23, 2022, 7:05 pm


# 7

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.


David


June 23, 2022, 7:16 pm


# 8

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 oral dosing.


MAC


June 23, 2022, 7:41 pm


# 9

David:

It depends on what delivery agent you use

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.

David:

If we can at least agree on what systemic levels seem to be desirable and match those levels with transdermal

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.

David:

it would create some advantages over the oral dosing.

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


David


June 23, 2022, 8:19 pm


# 10

@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 hinder Rapamycin. Love the thoughtful discussion though!


DrRoss


June 23, 2022, 8:24 pm


# 11

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.


MAC


June 23, 2022, 8:27 pm


# 12

David:

The gut microbiome may help and hinder Rapamycin

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 can not keep up.


MAC


June 23, 2022, 8:29 pm


# 13

DrRoss:

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

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.

Beauty

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