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In the past I have been experimenting with transdermal gels and cremes. I?ve used DMSO,Phlojel and self designed transport liquids.
I was hired by UG labs to create gels ? cremes and lotions for steroids, PGF2A, Yohimbine HCL and Glycyrrhetinic acid. If you people like it we can discuss homebrewing for spotreduction etc etc.
The Science of Topical Fat Loss
By: Par Deus
Introduction
I have previously stated that I believe transdermal prohormones to be the most effective supplements ever to hit the market. That statement must now be amended. Transdermal prohormones are indeed the most effective MUSCLE BUILDING supplements ever to hit the market. But, topical fat loss products have the potential to be an even bigger overall breakthrough in the never ending quest to improve body composition.
There are four areas that need to be addressed in regards to topical fat loss products and so called "spot reducers" in general.
First, one needs to distinguish between the products that are merely diuretics and those that the manufacturer (assuming they have a brain) actually thinks might significantly reduce body fat.
Second, we have to have an understanding of the andrenergic system, which is primarily what these products attempt to manipulate in order to aid lipolysis.
Third, we must have an understanding of transdermal/percutaneous delivery, in order to understand why a topical formulation could present advantages vs. orals, as well as to understand why nearly every product on the market fails miserably. Within this category there are two issues -- getting adequate amounts past the skin barrier and localizing its distribution to adipose tissue.
And, finally, there is the issue of Yohimbine HCl vs. yohimbe.
After reading this, you should have an understanding of why true "spot reduction" is physiologically quite possible, as well as enough information to make an informed decision as to which products can and cannot accomplish it.
Fat Loss Agents vs. Diuretics
Assuming we are not preparing for a photoshoot or competition, a product that merely acts as a diuretic rather than significantly aiding actual lipolysis is not what we want. "Cutting Gel" and "Dermalin-APg" belong in this category -- their active ingredient is aminophylline:
Aminophylline is a xanthine derivative, similar to caffeine, which, as we know, is not a particularly potent fat burner on its own. In rat studies, it has shown good thermogenic properties due to blockade of adenosine receptors (which provide one of the negative feedback mechanisms for catecholamine induced thermogenesis) and inhibition of phosphodiesterase (which degrade cyclic AMP) -- but this is at extremely high doses, which would kill a human, so it is not applicable (1,2). At therapeutic doses, only adenosine blockade occurs, which will act to increase norepinephrine levels (3)-- but as you will see, norepinephrine stimulates alpha 2 receptors (bad) in addition to beta 2 receptors (good) -- and in stubborn fat, alpha 2's outnumber beta 2's (4).
Like caffeine, aminophylline IS a good diuretic (5), which would account for the girth loss in the studies they reference, which did not measure actual fat loss (6,7). One study did look at fat depth after use of an aminophylline cream, and no difference was found vs. control (8). As a local diuretic, it is likely effective, but as a true fat loss agent, it quite likely is not. Such products WILL make you look more cut while you are taking them, but the true test of their efficacy is a week or two after you have stopped.
Products such as Avant Lab's LipoDerm-Y, Impact's DermaLean, SAN's LipoBurn, and Yohimburn -- basically any of the products with yohimbine and a handful of other ingredients -- fall into the latter category. They are intended to manipulate the adrenergic system, thus such products could cause true localized fat loss if formulated properly (and since yohimbine tends to make you HOLD water, their true test is also a week or two after you have stopped).
The Adrenergic System
Introduction
One of the major contributors to body weight homeostasis in the human body is the adrenergic system. There are two types of adrenergic receptors, alpha and beta, as well as subtypes of each -- and depending on which are activated, lipolysis (breakdown of fat) can be either stimulated or inhibited.
The most well-known adrenoreceptors to bodybuilders are the beta receptors. These can be divided into subtypes 1, 2, and 3 -- and it is through these receptors that drugs such as the ephedrine/caffeine stack and Clenbuterol exert their effects. While Clenbuterol acts directly on beta 2 receptors, ephedrine exerts its effects indirectly by stimulating the release of norepinephrine (NE), the body's primary endogenous thermogenic hormone. Unlike Clenbuterol, NE is not selective in its binding. In addition to binding to the beta 2 receptor, it also binds to both alpha receptors, as well as the beta 1 and 3 receptors. It is in regards to its binding to the alpha 2 receptor that yohimbine comes into play.
Norepinephrine and Yohimbine
Activation of the alpha 2 receptor inhibits the release of NE. Thus, by binding to this receptor, NE functions as its own negative feedback signal. In other words, it shuts off its own release. Obviously, this is not a good thing for fat loss. This is particularly true at rest (which, unless you are a marathon runner is 95% of your day) -- this is because alpha 2 receptors are activated at lower catecholamine levels than are the beta receptors (9). Thus, thermogenesis is basically always turned off, particularly in areas with high alpha 2 densities.
There are regional differences in the distribution of alpha 2 and the beta receptors as well as gender differences -- this is what is responsible for the observed variations in bodyfat storage patterns(4). Basically, females tend to have a large number of alpha 2 receptors and few beta receptors in the gluteofemoral area (hips, thighs, and butt), while men have the same problem in the midsection. With exercise or the use of compounds such as the ephedrine/caffeine stack, catecholamine levels can be increased to a point where the alpha 2 induced inhibition of lipolysis is partially overcome (9). However, even then, the alpha 2 receptors ARE still acting to reduce lipolysis.
Yohimbine is a selective alpha 2 antagonist (10) and can thus short circuit this feedback loop, maximizing NE levels, thus maximizing fat loss, particularly in these problem areas -- and even more so if we can achieve high levels of yohimbine and NE in the adipose tissue. Unfortunately, to do so with orals, or any other method that results in high blood levels, means that we will also have high levels in the heart and CNS -- thus, we will also have unpleasant and dangerous side effects such as tachycardia, high blood pressure, and anxiety. Considering the subject of this article, I obviously believe the solution lies in transdermal administration -- but more on that in a bit.
I was hired by UG labs to create gels ? cremes and lotions for steroids, PGF2A, Yohimbine HCL and Glycyrrhetinic acid. If you people like it we can discuss homebrewing for spotreduction etc etc.
The Science of Topical Fat Loss
By: Par Deus
Introduction
I have previously stated that I believe transdermal prohormones to be the most effective supplements ever to hit the market. That statement must now be amended. Transdermal prohormones are indeed the most effective MUSCLE BUILDING supplements ever to hit the market. But, topical fat loss products have the potential to be an even bigger overall breakthrough in the never ending quest to improve body composition.
There are four areas that need to be addressed in regards to topical fat loss products and so called "spot reducers" in general.
First, one needs to distinguish between the products that are merely diuretics and those that the manufacturer (assuming they have a brain) actually thinks might significantly reduce body fat.
Second, we have to have an understanding of the andrenergic system, which is primarily what these products attempt to manipulate in order to aid lipolysis.
Third, we must have an understanding of transdermal/percutaneous delivery, in order to understand why a topical formulation could present advantages vs. orals, as well as to understand why nearly every product on the market fails miserably. Within this category there are two issues -- getting adequate amounts past the skin barrier and localizing its distribution to adipose tissue.
And, finally, there is the issue of Yohimbine HCl vs. yohimbe.
After reading this, you should have an understanding of why true "spot reduction" is physiologically quite possible, as well as enough information to make an informed decision as to which products can and cannot accomplish it.
Fat Loss Agents vs. Diuretics
Assuming we are not preparing for a photoshoot or competition, a product that merely acts as a diuretic rather than significantly aiding actual lipolysis is not what we want. "Cutting Gel" and "Dermalin-APg" belong in this category -- their active ingredient is aminophylline:
Aminophylline is a xanthine derivative, similar to caffeine, which, as we know, is not a particularly potent fat burner on its own. In rat studies, it has shown good thermogenic properties due to blockade of adenosine receptors (which provide one of the negative feedback mechanisms for catecholamine induced thermogenesis) and inhibition of phosphodiesterase (which degrade cyclic AMP) -- but this is at extremely high doses, which would kill a human, so it is not applicable (1,2). At therapeutic doses, only adenosine blockade occurs, which will act to increase norepinephrine levels (3)-- but as you will see, norepinephrine stimulates alpha 2 receptors (bad) in addition to beta 2 receptors (good) -- and in stubborn fat, alpha 2's outnumber beta 2's (4).
Like caffeine, aminophylline IS a good diuretic (5), which would account for the girth loss in the studies they reference, which did not measure actual fat loss (6,7). One study did look at fat depth after use of an aminophylline cream, and no difference was found vs. control (8). As a local diuretic, it is likely effective, but as a true fat loss agent, it quite likely is not. Such products WILL make you look more cut while you are taking them, but the true test of their efficacy is a week or two after you have stopped.
Products such as Avant Lab's LipoDerm-Y, Impact's DermaLean, SAN's LipoBurn, and Yohimburn -- basically any of the products with yohimbine and a handful of other ingredients -- fall into the latter category. They are intended to manipulate the adrenergic system, thus such products could cause true localized fat loss if formulated properly (and since yohimbine tends to make you HOLD water, their true test is also a week or two after you have stopped).
The Adrenergic System
Introduction
One of the major contributors to body weight homeostasis in the human body is the adrenergic system. There are two types of adrenergic receptors, alpha and beta, as well as subtypes of each -- and depending on which are activated, lipolysis (breakdown of fat) can be either stimulated or inhibited.
The most well-known adrenoreceptors to bodybuilders are the beta receptors. These can be divided into subtypes 1, 2, and 3 -- and it is through these receptors that drugs such as the ephedrine/caffeine stack and Clenbuterol exert their effects. While Clenbuterol acts directly on beta 2 receptors, ephedrine exerts its effects indirectly by stimulating the release of norepinephrine (NE), the body's primary endogenous thermogenic hormone. Unlike Clenbuterol, NE is not selective in its binding. In addition to binding to the beta 2 receptor, it also binds to both alpha receptors, as well as the beta 1 and 3 receptors. It is in regards to its binding to the alpha 2 receptor that yohimbine comes into play.
Norepinephrine and Yohimbine
Activation of the alpha 2 receptor inhibits the release of NE. Thus, by binding to this receptor, NE functions as its own negative feedback signal. In other words, it shuts off its own release. Obviously, this is not a good thing for fat loss. This is particularly true at rest (which, unless you are a marathon runner is 95% of your day) -- this is because alpha 2 receptors are activated at lower catecholamine levels than are the beta receptors (9). Thus, thermogenesis is basically always turned off, particularly in areas with high alpha 2 densities.
There are regional differences in the distribution of alpha 2 and the beta receptors as well as gender differences -- this is what is responsible for the observed variations in bodyfat storage patterns(4). Basically, females tend to have a large number of alpha 2 receptors and few beta receptors in the gluteofemoral area (hips, thighs, and butt), while men have the same problem in the midsection. With exercise or the use of compounds such as the ephedrine/caffeine stack, catecholamine levels can be increased to a point where the alpha 2 induced inhibition of lipolysis is partially overcome (9). However, even then, the alpha 2 receptors ARE still acting to reduce lipolysis.
Yohimbine is a selective alpha 2 antagonist (10) and can thus short circuit this feedback loop, maximizing NE levels, thus maximizing fat loss, particularly in these problem areas -- and even more so if we can achieve high levels of yohimbine and NE in the adipose tissue. Unfortunately, to do so with orals, or any other method that results in high blood levels, means that we will also have high levels in the heart and CNS -- thus, we will also have unpleasant and dangerous side effects such as tachycardia, high blood pressure, and anxiety. Considering the subject of this article, I obviously believe the solution lies in transdermal administration -- but more on that in a bit.
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