Rapamycin in lecithin-based formulations to increase bioavailability

[rasotis]

Hi, I recently acquired a quantity of rapamycin powder. Rapamycin has good solubility in lecithin so I’ve tried dissolving 10 mg of rapamycin powder into 0.5 mL liquid lecithin for a weekly dose. It appears to completely dissolve after a few minutes. Judging from the literature, rapamycin becomes more bioavailable when dissolved in lecithin-based formulations. I wonder if there are others in this group who have tried this approach and if they can share any thoughts about how this works for them. Thanks.

[AustraliaLongevity]

I’ve never heard of this. You should do a sirolimus blood test after ingesting it to see how effective it is.

[Joseph]

FWIW

Take a dose of your compound, then do a blood test{to measure the rapamycin level] within 2 hours of taking.

You will have an idea of how much is absorbed.

@rasotis

“Rapamycin has good solubility in lecithin”

Liposomal rapamycin!

Liposomal aggregates sustain the release of rapamycin and protect cartilage from friction

Abstract “Fibrosis, low-grade inflammation, and increased friction are together with degradation of cartilage key culprits for debilitating pain in osteoarthritis (OA), which is one of the most common chronic diseases of today’s aging population. Intraarticular administration of bio-lubricants loaded with a pharmaceutically active component recently showed promise to improve therapy. Liposomes have emerged as exceptional lubricant biomaterial, but their small size leads to rapid clearance from the synovium, causing a need for more frequent administration. We recently developed a liposomal drug delivery system based on aggregation of negatively charged liposomes with physiologically present divalent cations. Here, we expanded our platform by replacing calcium with zinc, reported to exert anti-inflammatory action. The liposomal aggregates extend the release of rapamycin (RAPA) beyond the free liposomes and have a diameter of nearly 100 μm, which was previously established to improve ret…

[Alpha]

• Rapamycin Instability: Rapamycin is highly susceptible to rapid degradation in highly acidic environments, such as the stomach (pH 1.2), with studies showing almost complete degradation (below 2%) within 30 minutes in simulated gastric fluid when unformulated.

• Lecithin’s Role: While lecithin is a common pharmaceutical carrier that can help with drug solubility and absorption, and a component of some protective nanoparticle formulations, dissolving rapamycin powder in lecithin alone does not provide a sufficient barrier to the harsh acidic conditions of the stomach.

Even a liposomal rapamycin would experience very significant degradation by stomach acid.

Possible alternative to enteric encapsulation:

New nanoformulation of rapamycin Rapatar extends lifespan in homozygous p53−/− mice by delaying carcinogenesis - PMC.

Rapamycin powder has DIY uses in:

• Skin cream or treatments
• Hair restoration
• Tooth and flossing paste

[desertshores]

@Alpha

Possible alternative to enteric encapsulation:

Why is this a problem? Enteric-coated capsules are readily available in the US. That’s what I use. I insert already coated Rapacan tablets into enteric-coated capsules and take them with olive oil. Maybe overkill, but that is what I do.

[sol]

I’m intrigued. What’s your reasoning for double-encapsulation?

[desertshores]

What’s your reasoning for double-encapsulation?
Because I did some experiments with the Rapacan and Zydus tablets, which I posted on another thread a long time ago.
When the Rapacan and Zydus tablets were dropped into a beaker filled with water and a little hydrochloric acid to make a solution with a pH of average stomach acids, they dissolved in ~ 5 minutes.
So, I now put my tablets in enteric-coated capsules to help bypass the stomach and get into the lower digestive tract.
Here is a clip of the experiment. I have shortened it to show just from the time it was mostly disintegrated (5 minutes) until the time they were completely dissolved( ~10 min.) The cloudiness is from the excipients.