In the world of supplementation, Andros reign supreme as today's legal prohormones of choice. For those who are unaware of these compounds, the term Andro specifically pertains to the naturally occurring DHEA metabolites known as Epiandrosterone, 1-Androsterone and 4-Androsterone. There are a wide variety of Andros available utilizing different delivery methods, each with claims regarding their bioavailability, compound half-life, and so on. It can be confusing, even overwhelming, when trying to choose a product that meets your needs. So let's try to clear up some of that confusion by reviewing the different delivery methods currently available.
Let's begin with Cyclodextrins. Cyclodextrins use a carbohydrate-enveloping effect with compounds. The idea is that they are complexed in a structure which makes them water soluble. And they are in general designed to be taken sublingually (placed under the tongue to dissolve) with the intention to bypass first pass metabolism (liver breakdown). In 2002 a paper published in the Journal of Applied Physiology showed that a cyclodextrin complex of 4-Androstenediol did indeed result in increases in serum testosterone levels. However 4-Androstenediol, commonly referred to as 4-AD, converts directly to testosterone (1-step conversion) and since been banned in the United States. Now the legal prohormone 4-Androsterone, which converts to 4-Androstenedione and 4-Androstenediol and then convert to Testosterone (2-step conversion), is being seen released in the same manner of delivery along with 1-Androsterone and Epiandrosterone. But there's an issue, they are completely different compounds. The difference between 1-step and 2-step conversion prohormones is significant enough that we cannot assume that the results of a study done on a 1-step conversion prohormone will translate to a 2-step conversion prohormone. There are also claims that because of the limited surface area, the amount of prohormone that can be absorbed at one time sublingually appears to be 25mg or less, which is an extremely low dosage. As of 2015, there are still no studies proving the effectiveness of Cyclodextrins in delivering Andros and causing real-world results in body composition or performance.
So, let's move on to Liposomes. Liposomes act in a similar manner to Cyclodextrins, but instead of using a carbohydrate-enveloping effect it uses a fat-enveloping effect, they fold upon themselves, giving a shell with a water-soluble exterior and an oil soluble interior (somewhat similarly to cyclodextrins). When a liposome is ingested, it passes through the stomach and into the small intestine where it comes into contact with the non-polar intestinal cell lining, merging with it. When this happens, the compound trapped in the interior of the liposome is transferred into the intestinal lining and from there it travels into the portal circulation to the liver. Liposomes and Cyclodextrins work very similarly; you put the compound in a water-soluble shell, and then deposit it in the lipid-like surface of the oral or intestinal mucosa. However, the flux between the cavity of the cyclodextrin molecule and the mucosa is far more efficient and faster than liposomes. A liposome must first merge and dissolve into the mucosal cell membrane before its contents are delivered. In contrast, the cyclodextrin molecule undergoes no such interaction at the mucosal membrane, and does not disintegrate; it simply instantaneously delivers its payload. An industry expert has commented in the past that that single-layered liposomes are great oral products, and may also be effective sublingually (under the tongue) but likely don't work as well as cyclodextrin-complexed products. As of 2015, there are still no studies proving the effectiveness of Liposomes in delivering Andros and causing real-world results in body composition or performance.
Now let's discuss Esters. Adding an ester group to a compound makes it less soluble in water and more soluble in fat. The main claimed benefit of adding such an ester is potential lymphatic delivery (through the small intestine into the lymphatic system and thus bypassing the liver) for overall improved bioavailability. Whether or not this works for Andros has yet to be proven. There are a number of different esters, for example the enanthate ester, which you may see hidden in a compounds nomenclature as "enanthoxy" if the enanthate ester is attached to an oxygen atom. Now it’s worth pointing out that esters varying in their length, and due to this, take up a varying percentage of the compounds weight that is essentially inactive, resulting in less active hormone milligram for milligram. A good way of illustrating how different esters result in different amounts of active compounds is by looking at various esterified testosterone preparations. In this instance, the esters Enanthate, Caprylate and Undecanoate:
-100mg Testosterone Enanthate = 71.99mg Testosterone (28.01mg Enanthate)
-100mg Testosterone Caprylate = 69.56mg Testosterone (30.44mg Caprylate)
-100mg Testosterone Undecanoate = 65.15mg Testosterone (34.85mg Undecanoate)
As you can see around 1/3rd of the compound is inactive, and though these numbers don't necessarily reflect those of esterified Andros the principal is the same, less Andros by weight. There is also a misconception that orally ingested esterified compounds will match intramuscularly injected esterified compounds in the ability to provide a sustained release, but this is simply not the case. For example, an intramuscular injection of Testosterone Undecanoate provides a sustained release of Testosterone into the bloodstream for up to 10 weeks, but if orally administered it is eliminated from the body in just 3 to 4 hours. To what extent, if any, esterification improves bioavailability or half-life has yet to be proven, while increasing cost and providing lower doses of the active hormone by weight. Just as with Cyclodextrins and Liposomes, as of 2015, there are still no studies proving the effectiveness of Esterification in delivering Andros and causing real-world results in body composition or performance.
And finally, let's talk about free-form Andros. Free-form Andros are unmodified, no cyclodextrin, no liposome, and no ester, not delivered sublingually (under the tongue) but taken orally (swallowed). A paper published by West Texas A&M University, the California Baptist University and the University of Texas at Austin looked at the effects of 330mg free-form 1-Androsterone given daily for 4 weeks to 9 males with an average of 5 years of experience in resistance training and an average body fat of 13%. During the following 4 weeks, the subjects participated in 16 sessions of structured resistance-training. The results showed that the 9 males had gained an average of 10.4lbs (4.7kg) lean mass, lost over 4.4lbs (2kg) fat, and had a total load strength increase of 161lbs (73.2kg). No conflicts of interest, financial or otherwise, were declared by the author(s), and the research was supported by the West Texas A&M University Kilgore Research Center. Thus it can be extrapolated that this unbiased paper shows free-form 1-Androsterone to be a highly effective precursor to its target hormone 1-Testosterone, and is capable of eliciting highly favorable changes in body composition. As of 2015, it is still the only study proving the effectiveness of Andros in causing real-world results in body composition and performance, and this study specifically used high dosage Free-Form in delivering Andros, thus being the most logical choice when choosing a method of delivery.
So when choosing an Andro product to help you reach your goals, ask yourself, do you want a product that is backed my theories and hypotheticals, or by science? Does it look good on paper, with no real-world proof to convince you one way or another, or is it scientifically backed to give you the results you're looking for?
Let's begin with Cyclodextrins. Cyclodextrins use a carbohydrate-enveloping effect with compounds. The idea is that they are complexed in a structure which makes them water soluble. And they are in general designed to be taken sublingually (placed under the tongue to dissolve) with the intention to bypass first pass metabolism (liver breakdown). In 2002 a paper published in the Journal of Applied Physiology showed that a cyclodextrin complex of 4-Androstenediol did indeed result in increases in serum testosterone levels. However 4-Androstenediol, commonly referred to as 4-AD, converts directly to testosterone (1-step conversion) and since been banned in the United States. Now the legal prohormone 4-Androsterone, which converts to 4-Androstenedione and 4-Androstenediol and then convert to Testosterone (2-step conversion), is being seen released in the same manner of delivery along with 1-Androsterone and Epiandrosterone. But there's an issue, they are completely different compounds. The difference between 1-step and 2-step conversion prohormones is significant enough that we cannot assume that the results of a study done on a 1-step conversion prohormone will translate to a 2-step conversion prohormone. There are also claims that because of the limited surface area, the amount of prohormone that can be absorbed at one time sublingually appears to be 25mg or less, which is an extremely low dosage. As of 2015, there are still no studies proving the effectiveness of Cyclodextrins in delivering Andros and causing real-world results in body composition or performance.
So, let's move on to Liposomes. Liposomes act in a similar manner to Cyclodextrins, but instead of using a carbohydrate-enveloping effect it uses a fat-enveloping effect, they fold upon themselves, giving a shell with a water-soluble exterior and an oil soluble interior (somewhat similarly to cyclodextrins). When a liposome is ingested, it passes through the stomach and into the small intestine where it comes into contact with the non-polar intestinal cell lining, merging with it. When this happens, the compound trapped in the interior of the liposome is transferred into the intestinal lining and from there it travels into the portal circulation to the liver. Liposomes and Cyclodextrins work very similarly; you put the compound in a water-soluble shell, and then deposit it in the lipid-like surface of the oral or intestinal mucosa. However, the flux between the cavity of the cyclodextrin molecule and the mucosa is far more efficient and faster than liposomes. A liposome must first merge and dissolve into the mucosal cell membrane before its contents are delivered. In contrast, the cyclodextrin molecule undergoes no such interaction at the mucosal membrane, and does not disintegrate; it simply instantaneously delivers its payload. An industry expert has commented in the past that that single-layered liposomes are great oral products, and may also be effective sublingually (under the tongue) but likely don't work as well as cyclodextrin-complexed products. As of 2015, there are still no studies proving the effectiveness of Liposomes in delivering Andros and causing real-world results in body composition or performance.
Now let's discuss Esters. Adding an ester group to a compound makes it less soluble in water and more soluble in fat. The main claimed benefit of adding such an ester is potential lymphatic delivery (through the small intestine into the lymphatic system and thus bypassing the liver) for overall improved bioavailability. Whether or not this works for Andros has yet to be proven. There are a number of different esters, for example the enanthate ester, which you may see hidden in a compounds nomenclature as "enanthoxy" if the enanthate ester is attached to an oxygen atom. Now it’s worth pointing out that esters varying in their length, and due to this, take up a varying percentage of the compounds weight that is essentially inactive, resulting in less active hormone milligram for milligram. A good way of illustrating how different esters result in different amounts of active compounds is by looking at various esterified testosterone preparations. In this instance, the esters Enanthate, Caprylate and Undecanoate:
-100mg Testosterone Enanthate = 71.99mg Testosterone (28.01mg Enanthate)
-100mg Testosterone Caprylate = 69.56mg Testosterone (30.44mg Caprylate)
-100mg Testosterone Undecanoate = 65.15mg Testosterone (34.85mg Undecanoate)
As you can see around 1/3rd of the compound is inactive, and though these numbers don't necessarily reflect those of esterified Andros the principal is the same, less Andros by weight. There is also a misconception that orally ingested esterified compounds will match intramuscularly injected esterified compounds in the ability to provide a sustained release, but this is simply not the case. For example, an intramuscular injection of Testosterone Undecanoate provides a sustained release of Testosterone into the bloodstream for up to 10 weeks, but if orally administered it is eliminated from the body in just 3 to 4 hours. To what extent, if any, esterification improves bioavailability or half-life has yet to be proven, while increasing cost and providing lower doses of the active hormone by weight. Just as with Cyclodextrins and Liposomes, as of 2015, there are still no studies proving the effectiveness of Esterification in delivering Andros and causing real-world results in body composition or performance.
And finally, let's talk about free-form Andros. Free-form Andros are unmodified, no cyclodextrin, no liposome, and no ester, not delivered sublingually (under the tongue) but taken orally (swallowed). A paper published by West Texas A&M University, the California Baptist University and the University of Texas at Austin looked at the effects of 330mg free-form 1-Androsterone given daily for 4 weeks to 9 males with an average of 5 years of experience in resistance training and an average body fat of 13%. During the following 4 weeks, the subjects participated in 16 sessions of structured resistance-training. The results showed that the 9 males had gained an average of 10.4lbs (4.7kg) lean mass, lost over 4.4lbs (2kg) fat, and had a total load strength increase of 161lbs (73.2kg). No conflicts of interest, financial or otherwise, were declared by the author(s), and the research was supported by the West Texas A&M University Kilgore Research Center. Thus it can be extrapolated that this unbiased paper shows free-form 1-Androsterone to be a highly effective precursor to its target hormone 1-Testosterone, and is capable of eliciting highly favorable changes in body composition. As of 2015, it is still the only study proving the effectiveness of Andros in causing real-world results in body composition and performance, and this study specifically used high dosage Free-Form in delivering Andros, thus being the most logical choice when choosing a method of delivery.
So when choosing an Andro product to help you reach your goals, ask yourself, do you want a product that is backed my theories and hypotheticals, or by science? Does it look good on paper, with no real-world proof to convince you one way or another, or is it scientifically backed to give you the results you're looking for?