Topicals Info And Products
Powerful Products That You Rub On

1. What is a transdermal and how does it work?

TRANS; meaning "across", DERMAL; meaning "the skin". Although we think of the primary purpose of the skin as a barrier to keep things out of the body, scientists have known for at least 2 centuries that certain compounds have the ability to cross the layers of the skin and obtain access to blood vessels and the general circulation.

Modern medicine has responded with the development of methods to deliver drugs transdermally for therapeutic use as an alternative to traditional routes.

Why would one need to go through the trouble of formulating a transdermal when perhaps a simple tablet would do?

Well, the advantages of transdermal drug delivery systems speak for themselves and include avoidance of side effects, avoidance of the gastrointestinal tract and hepatic first-pass biotransformation and metabolism, control of absorption, availability of multiple skin sites to avoid local irritation and toxicity, and improved compliance. The result is a wider range of therapeutic options for physicians to use in optimizing their patients care.

The main type of transdermal that a bodybuilder would be interested in is one that contains prohormones. These help raise your testosterone naturally without any known negative side effects. Are you getting your money's worth when you buy prohormones in a capsule or tablet? Maybe not! Whenever you take a prohormone in tablet or capsule form, it goes rather directly to your liver. That's where up to 95% of the active prohormones get "de-activated." In other words, rendered useless. You pay for 100% of the prohormone. You only get about 5%.

Still, even with this estimated 5%, you've probably seen dramatic results in your body. And in your power output. So, imagine what would happen if you got over 90% of your money's worth of pro-hormone?

Well, first off, your testosterone level would probably soar. And so would your performance. Not only in the gym, but probably in the bedroom too.

That's if you could use most of the prohormones you took. Now, amazingly enough, you can if you use a transdermal.

How do you use a transdermal? Read the directions on the box for whichever product you choose for exact directions. Usually, you simply rub the topical lotion on your inner thighs or inner arms once a day. Some transdermals are best used by applying it to your testicles. Never consume by the mouth.

From his huge article on prohormones.

Topical delivery

A great deal better than the previous techniques, though no match for oral delivery. The first question that arises, and certainly the first one I posed, was whether or not prohormones can be absorbed through the skin. We all know that thanks to live passage a lot of the oral uptake is stopped and rendered useless. We also know that sublingual delivery works at a great rate but has limited absorption possibilities. In comes transdermal. There are two conditions that need to be fulfilled for something to be delivered in this fashion. The first being that the molecule being introduced is small enough to pass through the Stratum corneum, the upper layer of the skin. For this it has to have a molecular weight smaller than 500. Most prohormones have a molecular weight that approached 300, so this checks out. The second factor is that only lipophyllic (oil-loving) substances can permeate the skin. As you know the skin is oily and water-resistant, so water-based solutions cannot be introduced in this fashion. Since prohormones are made from cholesterol they are lipophyllic enough to be transported in this fashion.

One study done in 1986¹ documented that a hydroalcoholic (water and alcohol base) gel containing 50 mg of androstenedione was applied twice daily to the abdomen of 5 women. Plasma measurements of both the andro and the testosterone levels were conducted and showed that levels increased progressively for 6 days, after which they leveled off at 4-5 times higher than baseline for andro and 3-4 times over baseline for testosterone. This would indicate that this entails a very sustained release (applied only twice a day, effective for a duration of 24 hours or longer) with levels peaking and staying at 3-4 times higher than the average, this showed that transdermal delivery could be used to obtain and maintain optimal levels of the target hormones.

That answers the question of it being possible. That doesn't mean it can be accomplished. Mostly for transdermal purposes an alcoholic base was concocted, similar to that used in many sublingual technologies. The problem with this was that the alcohol quickly dried out, which gave you a fragile, dry skin, but left most of the prohormones dry on the surface of the skin, which would allow them to be washed off. Absorption in this manner could last very long, as illustrated above. So they had to speed up delivery. That's right, speed it up. It was too sustained and had to be brought down. More on that later.

First some remarks on this study. You will have noticed that it was done on women, and that increasing levels up to 4 times is not that hard to achieve compared to the female baseline levels. But I urge you to also look at the dose of 50 mg and the prohormone used, which were also strongly inferior. These days doses over ten times this and 3-4 times more effective products are used. Also they used a less effective delivery system.

The permeation through the skin can be enhance by a couple of factors. First of all the thickness of the skin in the area. Selecting skin parts that are thinner, like behind the ear, would increase absorption drastically, up to 10 times compared to the skin on your palm which is rather thick. Absorption seems to happen best when applied to the back and spread evenly. If you have eczema or another skin problem, applying it there may severely increase access for the prohormone molecule as well. Another factor is the formulation of the topical spray or cream. There are substances used in medical circles known as penetration enhancers that optimize this way of delivery. The two best know are DMSO (dimethylsulfoxide) which is found in most topical products and the other is IPM (isopropyl myristate) which is only found in select products. The IPM especially was shown to enhance delivery very well.

The positive aspects of this product are obvious: a prolonged sustained delivery, that only requires twice a day use for round the clock hormone elevation, and it doesn't need to pass the liver like the orals do, allowing better conversion, less of the amount of prohormones lost and less toxicity for the liver. It also doesn't interfere in your gastric processes assuring an almost time-based delivery. The downsides of using topicals are of course that depending on the permeability of the skin at different times, sweating profusely and other activities that may remove the stuff prior to absorption (showering for instance) you are never quite sure of the amount being absorbed and how fast it is being absorbed. Another obvious flaw is the limited delivery, you have to spread it out fairly well because laying it on too thick will only leave most of it as a residu on the skin. It's not my favorite method of delivery, but you'll find it very useful nonetheless, and for serious athletes it outclasses sublingual (under the tongue) delivery drastically. I give this a 3 out of 4.

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