Supplement Delivery Systems - What's the deal?

VaughnTrue

VaughnTrue

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I have been talking a lot about delivery systems as of late, so I wanted to try and help explain what I've been talking about. The info below is something I put together this week to help explain the differences between what will undoubtedly become the two most popular ones out there. I want to make this thread as much about discussion of delivery systems as possible, and NOT discuss specific companies/manufacturers so we can have a legit discussion, and talk about the positives and negatives of delivery systems as a whole.

This discussion will be centered specifically around the 1-DHEA style products currently available, however I'd love to discuss any and all compounds being utilized.











Why use a delivery system?

Delivery system technologies are used primarily for two distinct purposes:

1. Blood hormone levels – The key to hormones is to getting them into your bloodstream where they can interact with androgen receptors. The higher you can get your blood hormone levels, the better results you can theoretically get while on cycle. To put this into perspective, imagine you are consuming a hormone at the rate of 100mg/day. If you can get 25% of this hormone into your blood stream, you will have 25mg of the compound able to produce its anabolic and muscle growing benefits for you. The remaining 75% will offer you no added benefit. This means that by increasing the rate at which the hormone can enter your blood stream, the higher the total amount of hormone you have to exert its power in your body.
2. Mitigating unwanted/undesirable effects – This issue encompasses two major issues.

The first issue is the same for all hormones. The higher the dose taken the more potential for side effects. For example, if the same compound is being used (as described above) at a rate of 100mg/day, it will yield 25mg of the active hormone. Now, the other 75mg will not be able to impact the body for anabolic purposes, but it still impacts the body in ways such as liver toxicity. This means that for every 100mg you ingest, 25% if going to its intended “good” purpose, and 75% is going to unwanted “bad” result.

The second issue is specific to DHEA and its various anabolic isomers. DHEA converts to numerous different hormones, some of which are beneficial (anabolic), and some of which are not (estrogenic). Studies have shown that when specific DHEA dosage thresholds are broken, virtually all DHEA taken beyond that amount converts to the negative/estrogenic hormones. This means that by utilizing a lower overall dose that offers a higher bioavailability you are able to reap much larger benefits, while reducing or completely eliminating unwanted estrogenic conversion.



No Delivery System

When 1-DHEA and 4-DHEA products first hit the market, they were sold by themselves without any delivery system, just the hormone in a capsule. Despite using no delivery system, it is worthy to note that users experienced significant results, as backed by clinical studies performed at West Texas A&M University.
The various forms of DHEA being discussed follow similar absorption and bioavailability of traditional DHEA. Studies which look to discern the potencies of DHEA have found it to be absorbed at a very low rate when taken orally. For example:



As this study shows, when you consume DHEA and its various isomers(like 1-DHEA or 4-DHEA) you’re left with around a 3%-6% rate of bioavailability(underlined in red above).
To put this into perspective, if you were taking the manufacturers recommended daily dosing of 330mg/day of 1-DHEA, your body would be absorbing only 9.9-19.8mg of the active hormone itself! And even at these low doses the results seen were impressive, including significant gains in lean mass, reductions in fat, and strength.
In addition to the low blood hormone levels which are offered from having no delivery system, this issue is also coupled with the fact that the small % of conversion to active hormones leaves a high % of the compound left over that has no pathway left to convert besides estrogenic hormones(unwanted). One example of these unwanted side effects can be seen in the lowering of LDL or “good cholesterol” in the Texas A&M study.

What does all of this mean? Simply put, if you’re consuming 1-DHEA or 4-DHEA without a delivery system included in its formulation, you can expect extremely low conversion of the compounds into their target hormones(1-testosterone and testosterone), and a highly level of conversion into unwanted estrogenic hormones. This means you can get solid cycle results, but must deal with some potential negatives.





SEDDS Delivery System

SEDDS or “Self-Emulsifying Drug Delivery Systems” is a new delivery system which is just about to hit the dietary supplement market. This method of delivery system claims to work as a result of: “SEDDS possess potential to improve oral bioavailability in poorly water soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro- or nano-emulsions containing the solubilized drug. Micro/non-emulsified drug can easily be absorbed through lymphatic pathways, bypassing the hepatic first-pass effect, owing to their miniscule globule size” (National Institute of Pharmaceutical Education and Research).
SEDDS delivery vastly improves the effects from 1-DHEA and 4-DHEA by increasing overall bioavailability up to 9x greater than non-delivery system administration. This claim can be seen below:



Source: https://www.docdroid.net/dnVJvPF/sedds-absorption-2.pdf.html

This study showed that when using a hormone (in this case progesterone) SEDDS offers up to 9x greater bioavailability when compared to no delivery system. This means that while no delivery system offers 3-6% bioavailability, SEDDS offers up to 9x that, or a 27-54% bioavailability. Keep in mind however that the higher end of this bioavailability spectrum is highly unlikely for the average user as it assumes perfect conversions in the body, something which never happens in vivo quite the same as it does in vitro. That being said, SEDDS offers a VAST improvement from traditional dosing of these compounds, and users can expect far greater results, fewer side effects, and less overall HPTA shutdown when using the SEDDS delivery method over no delivery method.
In short, SEDDS provides a much higher rate of bioavailability, lesser chance for estrogenic conversion, and a much more effective cycle.






Cyclosome™ Delivery System/Phytosome Delivery System
Cyclosome™ delivery system is the first completely pharmaceutical grade delivery system utilized in dietary supplements. Originally designed by Indena® under the name Phytosome®, Cyclosome™ utilizes identical technology to increase the bioavailability and intensity of 1-DHEA and 4-DHEA.
For quick reference, this video briefly explains how the technology works:

[video=youtube;extbuY3CvCk]https://www.youtube.com/watch?v=extbuY3CvCk[/video]​


Studies on humans (not rats, rabbits, pigs, dogs, or anything else), have shown Cyclosome™ technology to enhance bioavailability 29xhigher than non-delivery system methods, bringing with it a minimum of 90% bioavailability (Source: Phytosome®)

In a comparative study in humans(16), analyzing the absorption of curcumin Phytosome® (Meriva®) and curcumin the overall curcuminoid absorption was about 29-fold higher for Meriva® compared to the unformulated curcuminoid mixture, while a 50 to 60 fold higher absorption has been shown for demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC). Furthermore also the absorption was faster with Meriva® the with the unformulated curcumin.

This type of delivery system showcases what is currently known as the most effective way of increasing bioavailability for compounds such as 1-DHEA and 4-DHEA. This means much more potent and anabolic cycles, little to no estrogenic side effects, and minimal HPTA suppression.




How do the 3 types perform when compared using identical doses?​

To help you determine which delivery system (or lack thereof) is best for you in your search for the best cycle possible, here is a quick and easy guide. No delivery system will be abbreviated using “NDS”, SEDDS will be abbreviated as “SED”, and Cyclosome™ technology will be abbreviated as “CST”.
100mg/day dosing:
NDS x 100mg (3-6% bioavailability) = 3-6mg 1-DHEA/4-DHEA in the blood
SED x 100mg (3-6% bioavailability) x 9 = 27-54mg 1-DHEA/4-DHEA in the blood
CST x 100mg (3-6% bioavailability) x >90% bioavailability = greater than 90mg 1-DHEA/4-DHEA in the blood

To understand which delivery system is best for you, it’s crucial that you understand how the product you’re planning on purchasing is dosed, as this varies greatly from manufacturer to manufacturer. For example, if one product gives you 60srv of 50mg capsules, versus 60srv of 100mg capsules, this may play a role in how you decide which is the better overall value.
 

ma70

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Well, what's your opinion on Phytosomes vs Cyclodextrins? As far as I can tell for basics, one is putting something in a carb, and the other in a fat.
 
VaughnTrue

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Well, what's your opinion on Phytosomes vs Cyclodextrins? As far as I can tell for basics, one is putting something in a carb, and the other in a fat.
Great question.


The Phytosome technology from Idena utilizes the ability to offer both gastric/digestive protection, as well as first pass liver protection. A 1-2 combo punch in essence.

Cyclodextrins are still subjected to degradation in the gut, but those that remain are not subject to first pass liver implications. This means a great step up, but is still not as bioavailable as other delivery methods out there.
 

ma70

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Great question.


The Phytosome technology from Idena utilizes the ability to offer both gastric/digestive protection, as well as first pass liver protection. A 1-2 combo punch in essence.

Cyclodextrins are still subjected to degradation in the gut, but those that remain are not subject to first pass liver implications. This means a great step up, but is still not as bioavailable as other delivery methods out there.
Does this mean that Cyclodextrins are always inferior to Phytosomes? Sorry, I'm confused. This kind of technology/study is new and foreign to me.
 
VaughnTrue

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Does this mean that Cyclodextrins are always inferior to Phytosomes? Sorry, I'm confused. This kind of technology/study is new and foreign to me.
well there are two types of cyclodextrin "delivery systems" being sold today:

1. True cyclodextrin systems which encapsulate the target compound within itself

2. Cycodextrin being dry mixed with the specific ingredient, and being sold as a delivery system(IE - next to nothing)


In the true cyclodextrin system, you'll note much better bioavailability for many compounds, hwoever it will not offer the level of bioavailability when compared to a delivery system like that which Indena developed. From the research I have done, the top two best delivery systems available on the dietary supplement market today are SEDDS and Cyclosome.
 
Danes

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Good thread for sure.

Below, I have "short explained" some of delivery methods.

-SEDDS technology: (no need to explain more deeply since OP have posted info about SEDDS) is nothing new and has been used by Biotest some years now and it is definitely a very good delivery method.

-Complexing a compound with Cyclodextrin: will definitely increase bioavailability and absorption but you will NOT Protect the compound .

Same with:
-Bonding a compound to Phospholipids: such as PC (this is very similar to complexing with Cyclodextrins).
Bonding means linking two or more things together chemically. This is different than simply mixing things together.it means you cant just take lets say ecdysterone with soy lecithin granules and believe it will do anything. If you just bond compounds to phospholipids (PC is a phospholipid), you improve bioavailability by "sneaking" some of the compound into the intestinal track but you still have the issue of stomach acids damaging the compound so even though you get better bioavailability it's still not great (if your bioavailability is let us say 5%, you triple that and you're still only getting 15%, even if you make it 6x, that's still only 30% in the best case scenario).

-Liposomal delivery merhod:
Liposomes is basically a ball of fatty acids and inside the ball you have the compound you have encapsulated. Your body doesn't try to break down the liposome (depending on the type of liposome) until it gets into circulation where enzymes will break it down.

The liposome protects the compound from the stomach acids. You're body also allows liposomes to pass easily through the intestinal walls (to you body, it just sees the liposome, it doesn't see the compound inside yet, when the liposome gets into your system and is circulating, that's when you have the enzymatic actions freeing the compound from the liposome, since the liposome is already circulating in your blood, when the compound is freed, the compound in turn is also in your blood).

I have always said Liposomal delivery method is superior all those methods until i saw Cyclosome .
It is actually pretty cool and very effective idea and here is a short explanation why use cyclodexrin with liposomes:

-Cyclosome delivery method:
The liposomes contain the compound complexed with cyclic dexterins. The liposome protects the contents and then when it's in the system, the cyclic dexterin complex facilitates transport.

Here is a old ecdysterone study done on hunans using Liposomal Delivery method:

"Beneficial effect of liposome encapsulation on the healing of skin in vivo occured in ecdysterone. Ecdysterone liposomes reduced healing time of an experimental epidermal wound from 28 to only 11, whereas ecdysterone in a gel had no significant activity. Meybeck A, Bonté F. 1990*Ecdysteroid-containing liposomes for wound healing and skin regeneration. Demande FR 2,637,182."
 
VaughnTrue

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let me know if you have any questions...I am here to help as I understand with multiple delivery systems available it can be quite confusing
 
cheftepesh1

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Good info.
 

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