Ecdy and Liposomal Encapsulation

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aron7awol
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Ecdy and Liposomal Encapsulation

Post by aron7awol »

I had an idea recently to greatly improve bioavailability of ecdysterone, given its hydrophobic and lipophilic properties. I have used similar processes in order to improve bioavailability of cannabinoids, which share those properties, with great results.

The general idea is to mix the extract with oil in order to get the fat-soluble compounds (ecdysteroids, cannabinoids) to bind with the fat, then add lecithin (I prefer sunflower, but soy also works) and agitate the mixture. Lecithin contains phospholipids, which are a very special type of molecule that is hydrophilic on one end and hydrophobic on the other end. This property causes them to form liposomes. You can see a visual example of how this looks here: https://www.uspharmacist.com/CMSImagesCo ... liv-F1.gif

Liposomal encapsulation has been shown to increase bioavailability by as much as an order of magnitude in many cases. This could be a huge boost for us to get more of the precious ecdysterone inside of us! I don't currently own an ultrasonic cleaner, but they use ultrasonic energy in order to perform liposomal encapsulations in the pharmaceutical industry, so I think I'll have to buy one to experiment with.

Here's a link I found which details liposomal encapsulation of Vitamin C using lecithin and ultrasonic energy:
https://curezone.com/forums/fm.asp?i=1556982

I also found a patent related to liposomal encapsulation of ecdysteroids, which tells me I'm on to something here!:
https://www.google.com/patents/US5198225
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RobRegish
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Post by RobRegish »

FANTASTIC work brother!

One caveat though: Ecdysterone is water soluble (not fat), due to its multiple OH groups. I learned this through conversations with Pat Arnold, so need to correct some of my past articles.

Having said that, there may be other compounds in RCE (tannins, resins etc.) that are fat soluble, so this experiment certainly is worthy.

Please keep us posted!!!
aron7awol
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Post by aron7awol »

Ahh thanks for that correction! I had assumed it was fat-soluble because every other steroid/sterol I knew of was fat-soluble. That's great to know!

Luckily, I think liposomal encapsulation may still be able to help us, since vitamin C is also water-soluble and it massively increases its bioavailability. I will proceed with my experiment and keep you posted on the results.
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thicketman
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Post by thicketman »

It's interesting that you brought this subject up. I have been mulling over the question in my mind about how to combine phospholipids with fish oil. The reason for this is that phospholipids supposedly increase the bioavailability of the Omega 3s in krill oil. Krill oil has some interesting studies (including one on inhibiting fat gain on a bulk) but if I recall correctly, the dose is pretty high (not cost effective).

I realize that it's much more complex than just having a phospholipid carrier, particularly since it wouldn't be in its natural form. In any case, I am curious if there would be any discernible effects (dry skin, dry eyes, brain chemistry, mitigation of fat gain, etc.).
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askmass
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Post by askmass »

Very interesting, because we considered doing a Liposomal format for Kre-Anabolyn when it was first in development many years ago.

We did not go in that direction for several good reasons, however have always made the following recommendation and it absolutely renders increased benefits in real life use-

"Smart MUSCLE MASS nutrition TIP: For peak results, take each Kre-Anabolyn dose with a tablespoon of Ultimate Omega, coconut, flax or olive oil to ensure your meal contains optimum EFA's. Research has shown doing this extends the anabolic effects of Kre-Anabolyn capsules for up to two additional hours!"

From https://bodybuildingsupplements.com/leuzea_ecdy.html
BrainSquirt
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Post by BrainSquirt »

hey guys just some (almost) random thoughts:

Effective ‘liposomes’ must be specialized in structure and ‘activity’ and targeted to cell type it’s being delivered to

AND/or/ie
……the typical DIY utoob sonification techniques would likely compromise some of the ‘good stuff’ in KA

Going a little off topic here but …
??? any gains from enterically coating KA (or a portion of the dose) ???







fwiw, if one were after the resins in a product the best way to get at those is via alcohol solution.
...and, for the most part, any beneficial 'tannins' you’re after in a product can most readilty be ‘got at’ via warm distilled water solution
just takes small amounts of each solvent and proper soak time...
... for the fat soluable parts, my thinking is it's important to match the lipid to the 'herb'. ... so... I don't doubt the effectiveness but I am curious if MCT's are the best 'solution' for KA... etc

...
thicketman,
have you looked at
https://suppversity.blogspot.com/2012/06 ... ts-in.html
?
moving / tweaking DHA ratio can really get some traction in some individuals

(and barely related… )
btw, moving / increasing GLA ratio can REALLY grab some ‘health and fitness’ traction in some individuals!!!

later...
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askmass
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Post by askmass »

We considered what could best be described as the Gaia liquid phyto caps delivery system for Kre-Anabolyn.

I remember this being appealing on paper, but ultimately it would have meant eliminating very important co-ingredients, crimped freshness longevity, and then all we were guaranteed to gain was to insure some EFA's were present come dosage time.

We like to push compliance of things which increase results, so a simple recommendation to take a full tablespoon of EFA's sufficed - while allowing the full, vibrant formula to remain intact (and that is the trump card).

In my experience, the more complex the herb, the more it's a mixture of fat and water soluble actives, the less likely a liquid extract of any sort can deliver all that.

Leuzea Rhaponticum Carthamoides is an incredibly complex little shrub, and the whole 'ActivECDY' bit even more so!

Alternatively, if you have one or cluster of very similar actives, then liquid is very often the most efficient and effective extraction and delivery system. You can refine it extensively, hone it (Yohimbe Supreme).

Not trying to take this too far off topic from the initial lipo encapsulation discussion. But, it's interesting to note those who have experimented with oil pulling invariably find the same oil(s) they have affinity for also clearly work best to give them top results from KA.

We all tend to need to supplement different parts of the EFA spectrum, just don't forget that the EFA's are ESSENTIAL for a reason.
aron7awol
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Post by aron7awol »

BrainSquirt:
Are you saying that you think sonification techniques would actually damage some of the compounds, or are you saying that you think liposomal encapsulation would actually prevent bioabsorption of certain compounds?

John:
Which ingredients would the Gaia caps have prevented you from using? I did assume shelf life would be a big reason not to do liposomal encapsulation in Kre-Anabolyn and sell it that way.



I guess my logic was that if taking a KA cap and eating a tablespoon of EFAs enhances absorption, then actually mixing the powder inside the cap with the fat directly would enhance it even more rather than relying on it happening randomly in the stomach. If that interferes with absorption of the water-soluble compounds, however, then it becomes a question of is there a way to maximize absorption of both? I feel like lecithin should be involved in any case since it has been shown to improve absorption of both types of compounds.

I completely agree with the point that herbs with complex mixes of fat and water soluble actives are difficult to find a perfect delivery system for. However, I don't simply accept that letting it mix with water and fat in my stomach is optimal, either. I'm a scientist at heart and I'm always looking to optimize everything in my life.

So here are my current questions in case one of you already know the answer or feel like discussing:
1. Does mixing directly with a fat interfere with absorption of the water-soluble compounds?
2. Does mixing with lecithin interfere with absorption of either water or fat soluble compounds?
3. Would a water soak, followed with an oil soak, then an emulsification of both using lecithin, be ideal?
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askmass
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Post by askmass »

aron7awol wrote:John:
Which ingredients would the Gaia caps have prevented you from using? I did assume shelf life would be a big reason not to do liposomal encapsulation in Kre-Anabolyn and sell it that way.



I guess my logic was that if taking a KA cap and eating a tablespoon of EFAs enhances absorption, then actually mixing the powder inside the cap with the fat directly would enhance it even more rather than relying on it happening randomly in the stomach. If that interferes with absorption of the water-soluble compounds, however, then it becomes a question of is there a way to maximize absorption of both? I feel like lecithin should be involved in any case since it has been shown to improve absorption of both types of compounds.

I completely agree with the point that herbs with complex mixes of fat and water soluble actives are difficult to find a perfect delivery system for. However, I don't simply accept that letting it mix with water and fat in my stomach is optimal, either. I'm a scientist at heart and I'm always looking to optimize everything in my life.



Tip of the hat to you, aron.

Critical Thinking is something too many people are surely missing these days, but here on the BP forum we see it in abundance!

I'll elaborate more in a follow up, perhaps, by on the Lecithin point I'll state right out that it's what the PS in Burn It Up is derived from and a key to that formula's success for MULTIPLE reasons, and that we have very liberal amounts infused into MASS PRO Whey.

On the point about having a mix in the cap- Once it hits stomach acid, either way it's scattered randomly. The digestive system is good at sorting it all out, but yes, we can improve the odds a lot.

Bioperine was chosen, along with the "take it with a tablespoon of EFA's" recommendation to maximize Kre-Anabolyn uptake.

That said, for those where malabsorption in general is an issue, here's an unabashed plug for Alkaplex (digestive enzymes, pH/alkaline optimization) and Pearls (legit, patented pro-biotic) available on the MASS site.

Even if you are using a quality EFA and think you are near optimum absorption, 30 days on the above additional might prove otherwise to you.

Re longevity- An oil base limited the shelf life test results to where it was barely scraping one year with natural oils... Flax was the worst of all, something like 3 months and it would have gone rancid. I guess we could have used a fake fat, maybe MCT, but for what better purpose?

It came down to fresh, quality EFA consumption on the spot being the best honest recommendation - Plus it kept the entire Kre-Anabolyn formula intact and insured it's 100% full potency, perfect pH of the Kre-Alkalyn, etc. long term.
BrainSquirt
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Post by BrainSquirt »

aron7awol wrote:BrainSquirt:
Are you saying that you think sonification techniques would actually damage some of the compounds...?
I don’t know for sure it would 'damage' KA. I do know that many properties / constituents of herbs can be compromised by the silverware sonic cleaner techniques shown on the DIY utoobs.
aron7awol wrote:BrainSquirt:
...are you saying that you think liposomal encapsulation would actually prevent bioabsorption of certain compounds?
Yes. bcse... All liposomal encapsulation methods are not created equal… if the vehicle can’t make a landing in the target cells, it really doesn’t matter how good the payload is. I continue to research and experiment and it is not my intention is not to discourage you here at all …thx for the topic!
...just the more I learn about liposomal encapsulation, the more I realize how specialized the relationship of the vehicle to the payload it is.
As AskMass asserted, a healthy biome may be the real key to optimal 'uptake and utilitization' ...
My thinking is that the 'lipid(s and AA's)' you choose for the body to create it's own loading the payload on the vehicle for optimal delivery is also very important. for example, across time, I've gotten good results from berries and cream plus MCTs for early / mid day dosing, but I have been experimenting with rice bran oil if I dose KA later in the afternoon... etc etc.

All the best

BrainSquirt
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Post by BrainSquirt »

re: "I completely agree with the point that herbs with complex mixes of fat and water soluble actives are difficult to find a perfect delivery system for. However, I don't simply accept that letting it mix with water and fat in my stomach is optimal, either." I concur with your optimization theme... and at the same time acknowledge that the digestive system does some elaborate packaging with proteins etc of nutrients before and as it passes them through the walls. For whole herbs, I guess I'm leaning a little bit toward give the body all the right stuffs and it's far better at putting them together than a laboratory can do it.
aron7awol wrote:So here are my current questions in case one of you already know the answer or feel like discussing:
1. Does mixing directly with a fat interfere with absorption of the water-soluble compounds?
2. Does mixing with lecithin interfere with absorption of either water or fat soluble compounds?
3. Would a water soak, followed with an oil soak, then an emulsification of both using lecithin, be ideal?
my off the cuff, quick opinions.
1 not very much
2 not for most things
3 i actually think that might be worth trying.
:D :shock: ... what about a water soak for one portion of the dose and an oil soak for another portion and then wrapping them both in lecithin and proteins, etc ?
?
BrainSquirt
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Post by BrainSquirt »

AskMass, Thank you very much for your answers and comments.

:) Completely Off topic question: Got an estimated in stock date for Berries n Cream cases?
BrainSquirt
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Post by BrainSquirt »

I know i keep posting ‘low tech’ replies to what are intended to be more ‘up tech’ questions … but here’s one more idea.

:idea: One possible high quality ‘folk solution’ dietary medium / accompaniment for KA might be pasture fed eggs *
They got all the ‘solvents we’ve been discussing above – the lipids, the lecithin, the proteins, the water, (and the vitamins and minerals, etc) … I personally will be trying this with any late afternoon /early evening dosing of KA

* pasture fed = sunlight, free range, hard shells, deep yellow orange yolk, viscous whites... cheap (well not anymore :evil: ,but) grocery store eggs don't make the cut for me

Ps are quail eggs and roe good options too?

Thoughts?

Ya'll have a good one.
aron7awol
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Post by aron7awol »

I appreciate the replies, gentlemen.

Ideally, I'd like to test and compare each of the following approaches, all consumed with a big meal:
- Water soak, oil soak, water & oil soak
- The 3 above, with and without lecithin added
- With and without ultrasonic encapsulation, for each of the lecithin tests
- Mix with a whole, raw egg (I love this one, BrainSquirt)

Unfortunately, I'm looking at 10 different tests, with no method of testing levels in the blood of anything, no control group, and probably no easy way to compare anecdotally either.

Does anyone have any ideas as far as measuring the effects somewhat scientifically? Rob, I know you've done quite a bit of ecdy testing on yourself. Any suggestions?[/list][/list]
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