Antaeus Labs Trenazone - Transdermal Dienolone!

Trenazone is Dienolone (estra-4,9-dien-17b-ol-3-one) -- a powerful anabolic agent -- in a revolutionary and patent-pending transdermal delivery system, designed to boost bioavailability to levels that would simply not be possible via oral administration. In other words, it allows more of the active ingredient to get into your bloodstream. It represents the next step in commercial muscle-building formulas, and the results it generates will need to be seen to be believed!

The active ingredient in Trenazone, Dienolone (also known as, hydroxyestradienone, 9(10)-Dehydronandrolone, and estra-4,9-dien-17b-ol-3-one), is notable as there has never been a more potent non-methylated anabolic supplement on the market.

The only problem with Dienolone is low oral bioavailability. Which isn't a problem with Trenazone, as its advanced transdermal delivery system increases Dienolone absorption by around 600% (from roughly 6% bioavailability with a capsule to roughly 60%, and as much as 70%,) and results in a controlled rate of absorption for stable blood plasma concentrations. Dienolone is a very powerful anabolic agent; it is now contained in one of the world's most advanced and synergystically-leveraged transdermal delivery systems. Trenazone is, quite simply, the most potent muscle-building product that your money can legally buy.

...Trenazone is an evolutionary step in prohormone technology, is available now, and comes with a 30-day, 105% money back guarantee.

Research: Transdermal Systems

Unmethylated compounds such as Dienolone are safer and 'healthier' than their methylated cousins, but they lack something very important: oral bio-availability. In other words, it is not optimal to take them as pills/capsules/tablets, as after ingestion and hepatic metabolism, only a fraction (typically around 6%) of the active ingredient you ingest will reach your bloodstream. Add a short half-life into the equation, and it becomes clear that oral dosing is inefficient, inconvenient, and expensive. Now, Bioavailability would be 100% if you injected a Dienolone suspension or implanted a pellet -- but these methods would be very clearly ill-advised for a mass-market product. Fortunately, there is another way...

Transdermal drug delivery is the administration of an active compound through intact skin for a systematic effect. The specific advantages of transdermal delivery have been fully discussed elsewhere. Briefly: Transdermal lotions and semisolids are easy to apply, and are easily washed-off following, or during, a dosing regimen. The reduced dosing frequency, and the production of controllable and sustained plasma levels, tend to minimize the risk of undesirable side effects sometimes observed after oral delivery. The avoidance of extensive hepatic first-pass metabolism is a further advantage. (Especially as, hepatic breakdown aside, there are reasons to believe that Dienolone is more effective if metabolized in the skin.) The major limitation to transdermal drug delivery is the intrinsic barrier property of the stratum corneum. The vast majority of active pharmaceutical ingredients and nutritional supplements do not possess any significant ability to cross the skin; therefore, the barrier properties of the skin must be chemically modified to reduce diffusive resistance by the use of penetration enhancers, or modulated using thermodynamic strategies. Both of these techniques are used in Trenazone to increase the penetration of Dienolone.

Numerous compounds have been evaluated for skin penetration enhancing ability, including sulfoxides (such as decylmethylsulfoxide, and 'DMSO': dimethylsulfoxide), Azone (e.g. laurocapram), pyrrolidones (for example, 2-pyrrolidone, 2P), alcohols and alkanols (ethanol, decanol, isopropanol), glycols (for example, propylene glycol, PG, a common excipient in topically applied dosage forms), surfactants (also common in dosage forms), fatty acids, and terpenes (non-aromatic hydrocarbons which can contain oxygen -- found in many plant extracts and essential oils -- such as camphor, menthol, and d-limonene.)

The most frequently-encountered of the above have their share of problems. DMSO's penetration-enhancing effect is extremely dose-dependent: It is largely ineffective at less than 70% concentration. [1] Unfortunately, at these relatively high concentrations, it will eventually denature skin proteins and cause a stinging rash. D-limonene, another common addition to commercial transdermal formulas, is of relatively weak potency (nerolidol and eucalyptol are both much more effective)[2] -- and, in general, terpenes fall short in the field of skin-safety.[3] D-limonene sure smells nice, but it's just not a very good penetration enhancer.



Azone (1-dodecyl-azacycloheptan-2-one, laurocapram) would be a better choice as a primary penetration enhancer, and I'm surprised that it hasn't made inroads into the supplement market. It was the first chemical to be developed solely as a skin-penetration enhancer, has been thoroughly researched, and has been shown to be a very effective enhancer of skin permeability. Surprisingly (and very much unlike DMSO, for example,) Azone concentrations in solution should not exceed 5%, and it is typically most effective at around 1-3%. The fact that it is most powerful at such low concentrations is noteworthy. As for its method of action, Fourier transform infrared (FT-IR) spectroscopy has indicated that Azone distributes homogeneously within stratum corneum lipids, in which it increases fluidity. This contrasts from the method of action of oleic acid -- which I will touch on later -- that appears to phase-separate and form liquid pools. In any case, the predominant method of action of Azone is to increase the diffusion coefficient of the permeant in the stratum corneum.

So, in other words, Azone is very good at getting active ingredients through your skin and into your bloodstream. But benzisothiazol-3(2H)-one-2-butyl-1,1-dioxide -- or 'Thiazone' -- is better. In very recent clinical studies,[4,5] the two were directly compared, and Thiazone was found to have a penetration-enhancing effect 2.99 times greater than Azone. Like Azone, it is non-toxic, powerful in very low concentrations, and is not an irritant. Though its method of action is as yet unresolved, there are indications that it works in the same manner as Azone -- that is to say, that it increases the diffusion coefficient of the permeant in the stratum corneum, and induces stratum corneum lipid layer fluidity via reducing the condensation state of those lipids. Thiazone is simply the most powerful penetration-enhancer on the market, represents the cutting-edge of applicable transdermal technology, and is the primary penetration enhancer for Dienolone in Trenazone.

Other ingredients include:

-Super-refined oleic acid
Both saturated and unsaturated fatty acids have been established as skin permeation enhancers, which operate via disordering the highly ordered structure of the skin lipid barrier. Oleic acid -- a C18 unsaturated fatty acid -- is one of the most extensively studied penetration enhancers among the fatty acids. [6,7] It possesses a very strong synergistic effect with propylene glycol; in one study, OA+PG enhanced the skin permeability coefficient of melatonin more than 950-fold over the effect of propylene glycol alone. [8] Moreover, as its method of action is slightly different from that of Thiazone, it should also have a synergistic effect with that compound. Although it is a slight irritant, using a very high grade of OA at a relatively low concentration should reduce the risk of skin irritation.

-Propylene glycol
The world's best excipient and co-solvent for transdermal formulations. In itself, it was found to enhance the skin permeability of steroids [9, 10] and estradiol [11]. The activity of other enhancers can also, as was previously mentioned, be significantly increased when applied in combination with propylene glycol. [12, 13] In contrast, polyethelene glycols (PEG) appear ineffective in promoting transdermal absorption, and in many cases actually reduce the rate of penetration. [13]

-Glycerin
Research has shown that topical formulations which contain oleic acid should also contain either alpha-tocopherol or glycerin in order to prevent skin irritation. Trenazone includes a generous dose of the latter. We're not going to claim that that our transdermal formulation is good for your skin, but it should be skin-safe for all but the most sensitive.

Thermodynamic modulation: Supersaturation

The concept and an understanding of supersaturated systems evolved from crystallization theory, in which a solution must first be supersaturated in order for crystals to form. (See image to right. Click to enlarge.) The potential benefit to topical and transdermal systems was first recognized by Higuchi (1960). He considered a system in which the vehicle did not chemically alter the barrier properties of the skin, and the rate-controlling step to percutaneous absorption was in the outer layers of the stratum corneum.



Consequently, from the definition of the partition coefficient, and when the vehicle is saturated with the active ingredient, the SC must also be saturated. Similarly, when a supersaturated solution is placed on the surface of the skin, the concentration of the active ingredient in the SC also becomes supersaturated. When this happens, penetration enhancement proportional to the degree of supersaturation will occur.

This theory that supersaturated systems could offer greater penetration was tested by Coldman et al. in 1969. They introduced the steroid fluocinolone acetonide and its acetate ester onto human skin in a volatile:nonvolatile co-solvent vehicle (isopropanol:propylene glycol). Their experiment concluded that as the volatile component evaporated, the solution became more concentrated, and eventually a state of supersaturation was reached, giving rise to enhanced penetration.

There is anecdotal evidence for synergy between supersaturation and chemical penetration enhancement. For example, penetration from saturated, oleic acid pretreated skin, and oleic acid pretreated skin with sixfold supersaturated fluribuprofen systems is shown in the image on the right. (Click to enlarge.) The results demonstrate the potential for synergy between enhancers working to increase diffusivity in the stratum corneum and supersaturation.

Trenazone is mildly supersaturated -- not nearly as much as sixfold supersaturated. The reason for this is that supersaturated states are thermodynamically unstable, prone to crystallization -- and they are therefore difficult to produce, difficult to maintain, and difficult to bring to market. It goes without saying that a sixfold supersaturated solution would be nearly impossible to market as a commercial product... But that won't stop us from trying. A future version of Trenazone, perhaps as much as 3x supersaturated, may be released in a small run the near future.

At the moment, however, there is Trenazone. It is the most potent non-methylated compound available, in one of the world's most advanced and synergystically-leveraged transdermal delivery systems. We feel that it represents, quite simply, the most potent muscle-building product that your money can legally buy.

There is anecdotal evidence for synergy between supersaturation and chemical penetration enhancement. For example, penetration from saturated, oleic acid pretreated skin, and oleic acid pretreated skin with sixfold supersaturated fluribuprofen systems is shown in the image on the right. (Click to enlarge.) The results demonstrate the potential for synergy between enhancers working to increase diffusivity in the stratum corneum and supersaturation.



Trenazone is mildly supersaturated -- not nearly as much as sixfold supersaturated. The reason for this is that supersaturated states are thermodynamically unstable, prone to crystallization -- and they are therefore difficult to produce, difficult to maintain, and difficult to bring to market. It goes without saying that a sixfold supersaturated solution would be nearly impossible to market as a commercial product... But that won't stop us from trying. A future version of Trenazone, perhaps as much as 3x supersaturated, may be released in a small run the near future.

At the moment, however, there is Trenazone. It is the most potent non-methylated compound available, in one of the world's most advanced and synergystically-leveraged transdermal delivery systems. We feel that it represents, quite simply, the most potent muscle-building product that your money can legally buy.

Trenazone FAQ:

Q: What is Trenazone?

Trenazone is Dienolone in a revolutionary and patent-pending transdermal delivery system. Based on bleeding-edge research and using only the purest pharmaceutical-grade ingredients, Trenazone stands at the pinnacle of commercially-available muscle-building products.

Q: What does Trenazone do?

Trenazone's novel transdermal delivery system was engineered to increase the transdermal flux of Dienolone; this results in vastly increased bioavailability, which in turn results in noteworthy size and strength increases.

About our transdermal delivery system:

--It is nonmutagenic, nonteratogenic.
--It is essentially pharmacologically inert.
--It increases blood concentrations of Dienolone to levels that would not be possible via oral administration.
--When evaluated in clinical and non-clinical studies, average concentrations have been shown to not produce any level of systemic toxicity. In very high concentrations taken over long periods of time, thiazone may cause mild hemolysis, though this is not an issue at the concentrations found in Trenazone.
--In its current formula, it provides an in vivo transdermal flux of more than 3.0 and as much as 9.0 μg/cm2 per hour. To put this into perspective, Androgel averages just slightly under 1.0 μg/cm2/hr.

Q: Is it safe to use?

With regards to the delivery system:
Trenazone's transdermal delivery system is non-mutagenic, non-teratogenic, and is essentially pharmacologically inert. The greatest risk associated with its use is the development of contact dermatitis -- which, if developed, will quickly subside once use is discontinued.

With regards to the active ingredient:

Dienolone is a potent anabolic hormonal product. It is not to be used at doses exceeding 150mg/day. Furthermore, Dienolone is not to be used by women, children, the very elderly, and persons with a history of heart disease, high blood pressure, diabetes, cancer, autoimmune disease, psychological disorders, and other health problems. Dienolone is not to be used by persons under 21 years of age. Generally speaking, use of Trenazone is an order of magnitude safer than use of 17-alpha-alkylated hormones.

Q: Does Trenazone have a local anabolic effect?

No. Trenazone was formulated to elicit a systematic effect, solely. There are very simple ways to get transdermal solutions to produce localized effects, but these methods would, in fact, limit Trenazone's overall effectiveness, and were therefore not included in its current forumation.

Warnings:

Do not apply to broken or damaged skin. Avoid applying to skin which may be exposed to ultraviolet radiation (UVR) for an extended period of time. UVR has the capacity to energize molecules, and in this photoactive state, these molecules can produce photoirritant reactions. Do not run for longer than 12 weeks. After completion of your Trenazone regimen, take a break of at least several weeks. Rotate application sites frequently!

Irritation (i.e. contact dermatitis) is only rarely associated with the topical application of Trenazone. If irritation develops, discontinue use and it will quickly subside. Trenazone can transfer from your body to others. This transferral can occur if other people come into contact with the area where Trenazone was applied to your skin. Women and children should avoid contact with the unwashed or unclothed application area where Trenazone has been applied. If you expect to have skin-to-skin contact with another person, first wash the application area well with soap and water. It must be noted that once the application site is dry -- after the solvents evaporate -- the risk of transferral is extremely low.

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