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Androderm & Androgel

Transdermal Testosterone has been marketed heavily in the Hormone Replacement Therapy Market for the last decade. For over 50 years, testosterone therapy has been used for the treatment of hypogonadism. In recent years, there has been an increase in the use of testosterone therapy for men with late-onset hypogonadism, sometimes referred to as andropause. Testosterone therapy in older and hypogonadic men can significantly improve their sense of well-being, and lead to increases in muscle and bone mass, upper body strength, virility, and libido (5). Oral delivery of unmodified testosterone is not really a viable option, due to its rapid first-pass metabolism, possible liver toxicity, and its relatively short half-life. Thus, injectable testosterone was used for a very long time as an effective hormone replacement method. Roughly a decade ago, alternatives to injectable and oral testosterone were developed. Originally, these alternative methods of application for testosterone meant shaving an area of the skin’s surface (*usually the scrotum, no, really) and attaching a testosterone patch with low, dry heat like a hairdryer, which basically hot-glued the testosterone patch to the scrotum. Luckily, this painful procedure progressed to the point where it is at now; you can simply apply a self sticking patch or rub some testosterone gel anywhere on your body, and get the same effect.

When some (nonscrotal) transdermal testosterone preparations were examined, they showed that the plasma concentration of TS increased very rapidly, and reached the peak level within 3-6 hours of the application of the experimental patch.(2) This is comparable with some of the better oral products out there. In my experience, an athlete would usually swallow a pill rather than have a patch hanging on them for a day.

Basically, you can expect all of the benefits of injectable testosterone with the transdermals (if the mg doses were the same…which they are not). What we’re dealing with here is Androderm, which is a patch containing 12.2mgs of testosterone and androgel, which gives you about the same (you only get 10% of the total drug contained in the preparation….thus a hundred mgs of test in a gel form, would yield a 10mg amount in your body).

A mere 100mg shot of injectable testosterone provides much higher peak plasma concentrations of testosterone, even though the transdermal testosterone was more stable, with regards to blood plasma levels. So what are the advantages of transdermal application? Clearly, it provides a very stable blood level of the compound administered.

The levels of testosterone it gives us are just enough to provide a slight boost, at a high (financial) cost. Wouldn’t it be great if we could get this stuff dosed more highly? Or maybe even with Clen, so we could apply it directly to fatty areas? Or with Tren? It would even have potential for first time needle-phobic steroid users to use items which were formerly only available as an injectable! Women could use a Tren product without leaving needle marks! In fact, with a little creativity, underground Labs could even make transdermal products which would never get caught by customs (perhaps disguised as stickers or whatever).

One particularly successful transdermal testosterone delivery method involves the combination of DuroTak 87-2510 as an adhesive polymer. This is combined with 3% dodecylamine and 10% span 80. This, combined with testosterone creates a nice transdermal delivery system (4). Another experimental transdermal testosterone preparation contains occlusion, octisalate (OS), and propylene glycol (PG), called Solugel (which is a proprietary hydrogel containing PG 25% w/w) and Tegaderm (a semipermeable film dressing) on the permeation of TES was assessed. Occlusion had no effect on the permeation of TES, however, OS increased the flux of TES 2.9-fold. The concentration of PG which produced optimal TES flux was 20% v/v, and this concentration resulted in a 1.9-fold increase in TES permeation. By combining OS, PG, and occlusion, transdermal testosterone permeation through the skin was increased 8.7-fold, which was a synergistic enhancement, obviously…meaning the sum of the parts was far more than their individual totals (3).

References:
1. jcem.endojournals.org/content/vol84/issuel0
2. In vitro and in vivo evaluation of a novel nonscrotal matrix-type transdermal delivery system of testosterone. Drug Dev Ind Pharm. 2005 Mar;31(3):257-61.
3. Synergistic enhancement of testosterone transdermal delivery. J Control Release. 2005 Apr 18;103(3):577-85.
4. The current status of therapy for symptomatic late-onset hypogonadism with transdermal testosterone gel. Eur Urol. 2005 Feb;47(2):137-46.
5. Effects of androgen substitution on lipid profile in the adult and aging hypogonadal male. Eur J Endocrinol. 2004 Oct;151(4):415-24. Review.
6. [Gruenewald, Matsumoto. J Am Geriatr Soc 2003;51:101 Morales. Aging Male 2004; in press].

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