MC's Gemini of Transdermal Fat Loss Log - Napalm + Lipoderm (Sponsored)
- 09-03-2008, 10:04 PM
MC's Gemini of Transdermal Fat Loss Log - Napalm + Lipoderm (Sponsored)
The Science Behind Topical Fatloss
Targeting the delivery to the adipose tissue was the most substantial problem facing efficacious topical formulations. Atop that, is the role of the skin: it is an essential physical barrier which evolved for our protection. Thus, the necessity for a penetration enhancer emerged to loosen, or ease, the passage of ingredients within the topical matrix through the dermal layers and into the adipose. Pioneering scientific literature using common therapeutic drugs (1,2,3,4,5) proved that skin penetration and local deliver is attainable and feasible for certain compounds. But, why only certain compounds?
As you might expect chemicals, drugs, nutraceuticals, etc. come in all shapes and sizes. Finding the ideal combination triumphantly yielded the formulation for the Lipoderm Series, which has been adopted and improved upon by Avant Research to create the most effective all-in-one topical to date- Napalm.
Adipose tissue, which is renowned for its poor perfusion (or relative blood supply), is another important physiological barrier that can impede our body’s natural efforts to get skinny. Since fat must first be broken down prior to oxidation, an increase in perfusion to concentrated areas of stubborn fat will facilitate a reduction in fat mass by shuttling away liberated free fatty acids. Our knowledge of the adrenergic system tells us this is easily achievable by coupling alpha-2 antagonism (yohimbine) and beta-receptor activation (synephrine).
Performing adrenergic stimulation from the topical angle is particularly advantageous to the athlete looking to avoid the central (CNS) affects manifesting from the beta agonism. Our specialized carrier allows users to skirt this potentially unwanted side effect, but spares no assault on the fatty area of application.
The Cast & CrewYohimbine
Reviewing the role of yohimbine in the adrenergic system can be simplified down to its actions at the alpha-2 adreoreceptor(AR), where it is a selective antagonist (or simply, but misleadingly: an inhibitor). The functional properties of the alpha-2 AR are noteworthy for athletes since they play a key role in the regulation of lipolysis by inhibiting the release of norepinephrine (NE). This is achieved through a self-generated negative feedback loop following NE binding at the alpha-2 AR. The role of yohimbine here is to bind selectively at the alpha-2 AR and inhibit the stimulatory actions of circulating catecholamines, such as NE, and its mimetics, such as ephedrine. An adequate dosage of topical yohimbine will concomitantly increase blood flow in adipose tissue (at the site of application) (6), and ensure liberated fat will not be retained(7) – all without the deleterious and unwanted effects in the CNS and cardiovascular systems. Furthermore, the negative feedback loop alluded to earlier is now essentially 'short circuited' allowing hyperactivation of Beta receptors and potentiation of downstream lipolytic effectors, namely cAMP and adenosine antagonism. Moving forward we'll see the critical interplay between these processes and those incited by other actives found in Napalm.
You know it and you love it. No stranger to inclusion in successful topicals, SesaThin can be found in identical concentrations as is in Lipoderm Ultra. The active ingredient in SesaThin -- sesamin -- acts just like certain fish fats as a ligand for PPARalpha (peroxisome proliferator receptor alpha), a type of ligand-activated transcription factor in human cells which plays an important role in fat-metabolism, fat-storage, and glucose homeostasis(8,9,10). Moreover, studies have shown that sesamin-induced PPAR-alpha activation elevates fatty acid oxidation as much as 10-fold over normal levels (11,12,13). Couple its ability to increase fatty acid utilization while suppressing fat-storage (8,13,14,15) and it's clear to see why it works so well with the other active ingredients in Napalm.
Another carry-over from the Lipoderm series included in Napalm is synephrine. Commonly found in 'ephedra/epherine free' fat loss products, it shares some of the well know characteristics of this famous symphathomimetic, while offering some unique addition benefits. It is an agonist of the alpha-1 adrenoreceptor (16,17) which is involved in variety of roles in adipose tissue, inclusive to modulating intracellular Ca2+ and protein kinase C levels and glycogenolysis(18), as well as serving to increase lipolysis in human adipose tissue (19). Without getting overly technical, this creates a significant degree of synergism between cAMP-inducing mechanisms offered by other component of Napalm (see below & RK's). Additional synergism lies in synephrines' ability to stimulate beta receptors, albeit to a lesser degree than other more specific beta-1 and beta-2 agonists (20).
Raspberries are appropriately touted as a wonderfully nutritious fruit and snack. Interestingly, several of its chemical constituents -- when extracted and isolated -- are found to have medicinal benefits. Such is the case with the raspberry ketone (4-(4-hydroxyphenyl) butan-2-one; abv. RK). Researchers were curious to contrast its affects to structurally similar drugs: synephrine and capsaicin.
As one might expect the physical characteristics of RK elicit a unique response at the cellular level. Whereas synephrine has been shown to directly bind and activate beta receptors, a quality that RK's lack, their key functional role lies in the potentiation of the rate limiting step in the fat burning process: the hydrolysis of triacylglycerol (TAG). This process is mediated by the catalytic protein HSL, or hormone-sensitive lipase, which is recruited to lipid droplets in the cytoplasm in a cAMP-dependent manner (21). RK's have been shown to sufficiently enhance the localization of HSL within the cell to dramatically increase the rate of this crucial reaction (22).
Unfortunately, the literature has yet to characterize RK's to the degree in which its structural analogs, notably capsaicin, have been scrutinized and investigated. With caution, we can extend their physical similarity unto the potential for paralleled signaling pathways, and thus observe commonalities in downstream cellular events. In this vein, the warming sensation observed in our beta testing suggests that RK's do have similar metabolic consequences when administered in a topical matrix. Offering support are the observations made by Kawada et al (1986) whose group documented comparable increases in oxygen consumption following ingestion of either capcaisin, or RK's (23). Additionally, unpublished data recorded the ability for RK's to enhance a critical marker of mitochondrial activity, cytochrome C oxidase, demonstrating RK's ability to increase cellular metabolism, albeit in a mouse model.
Further consideration should be given to the capsaicin-like properties of RK's given their potency as a vasodialator, and its ability to induce transient insulin insensitivity. The latter, through stimulation of vanilliod receptors prompting the release of Calcitonin Gene Related Peptide (CGRP), another highly potent vasodialator. CGRP is highly instrumental in reducing the capacity of the adipocyte to absorb glucose through the insensitivity alluded to above. While this property is unfavorable in other tissues, starving adipocytes of the necessary energy supply is a novel mechanism to induce apoptosis and consequently lose fat! This brilliant hypothesis brought us SpookyDerm, a vicious blend of Lipoderm Ultra, pain-inducing capsaicin, and nicotine. While we have Spook to thank for the original concept, we have RK's to thank for the widespread popularity of this pain-free approach to unsurpassed topical fat loss.
Licorice has a lengthy historical association with reduction fat mass and weight loss dating back to the 4th century BC. The Greek physician Theophrastus noted that licorice root granted his patience 'freedom from hunger and thirst'(24), an observation that was reaffirmed in the 1st century BC by Plinius (25). It wasn't until modern technological advancements allowed us to characterize the licorice root in order to reveal the main active ingredient: glycyrrhetinic acid (GA).
These ancient observations are supported thoroughly by modern literature which documents the relationship between GA and 11?-hydroxysteroid dehydrogenase (11HSD) (26). For our purposes we will concern ourselves with the first of two 11HSD subtypes. 11HSD1 is found in subcutaneous adipocytes in a relatively lesser abundance than it's visceral counterpart (27). However, 11HSB-1 is sufficiently concentrated to perform its primary function and influence the level of cortisol by reactivating the inactive cortisone. A hyperactive mutant form of 11HSD-1 is observed in cases of the pathologically obese, suggesting that inhibition of this enzyme will facilitate reduction in adipocytic mass.
This is where GA performs its duties and helps you get skinny, the ultimate result can be attributed to a few proximate causes. Firstly, the vital role of GA and cortisol. By reducing the local availability of cortisol via 11HSD-1 inhibition (28), GA causes a reduction in the concentration of intracellular triglycerides (29), in addition to impeding the differentiation preadipocytes(30).
The merits for topical applications of GA are not limited to the above, but further investigation also showed the ability for GA to positively affect fat metabolism by inactivating fat lipase and increasing mobilization of adipose stores (31).
Containing Yohimbine Hydrochloride in Avant Labs' hydroalcoholic gel, Lipoderm ULTRA activates targeted fat reduction at the site(s) of application, while avoiding the negative side effects associated with systematic distribution. Expanding upon its predecessor's revolutionary formula, LipoDerm-ULTRA utilizes a number of ancillary fat-fighting ingredients that decrease nutrient uptake and insulin sensitivity in the fat cell, while concurrently increasing leptin expression, leptin sensitivity, and other lipolytic signals such as cAMP and norepinephrine, for maximal fat depletion. In addition, this new formula modestly facilitates increased utilization of fatty acids in muscle while sparing glycogen. Lastly, Lipoderm-ULTRA incorporates a local diuretic that neutralizes water retention, making it easier to evaluate progress during use.
In addition to Yohimbine, each bottle of Lipoderm-ULTRA contains:
I want to say a big thank you to the guys at Avant, especially SirSavage for giving me this opportunity to log this for you guys. I love both of these products on their own, I can't wait to see how applying them stacked will do.
Last edited by mrchristian; 09-10-2008 at 10:13 AM.
- 09-03-2008, 10:04 PM
MC's Gemini of Transdermal Fat Loss Log - Napalm + Lipoderm (Sponsored)
I thought I would lay this all out now so I could give everyone a chance to chime in. I am entering this log with an open mind, always willing to learn, grow, and accel in my workout goals. I implore anyone to offer advice or pass a long suggestions for me to tweak my diet/workout regimen to get the most out of this log. I look forward to hearing your suggestions (especially diet suggestions).
Transformation In Process:
It's been a long and arduous process, but is mainly due to my own irresponsibility with my personal health and diet. I have been making improvements for several years now. In total I have lost about 75lbs, and I have been making huge strides in adding as much muscle and strength as I can. I still have remaining pesky abdomen fat though (especially love handles from hell). I am trying to lean out in this area as much as possible. Any suggestions of some killer ab rouines would be greatly appreciated!!!
I have used both Napalm & Lipoderm for solo runs in the past. I LOVE Lipoderm. I can definetly notice a leaner/tightening appearance of my ab region when I use it after a few weeks. I have even ran Lipoderm Ultra + Capsaicin before. I LOVE this combo. Your applied area turns into an oven, not burning, but warm, and you sweat like crazy. I was ecstatic whent Avant Labs chose me to log the combo of Napalm/LipoDerm. I want to give much thanks and praises for allowing me to do this.
My protocol will consist of an application of Napalm first thing in the AM prior to work, and then an application of Lipoderm after workout shower in the evening. I will be adding Caffeine to my Napalm in accordance with some anectdotal evidence that it will have a slight diuretic effect in the area of application. I am not sure if I will be adding Capsaicin to my regimen of nightly Lipoderm or not. All depends on whether Avant would permit or want this. Here is where it gets interesting, Ive discovered a way (at least I personally feel) to make the Lipoderm more effective and to get it to absorb better. My wife & friends mock me, but I swear it works. After my Capsaicin/Lipoderm application in the evening, I let it work for a few minutes without a shirt, and then I put on what my wife calls my "fat wrap", which is just an atheletic trufit wrap that you wrap around your abdomen to provide more heat and to firm up. I purchased mine for a few bucks at Dunhams, but I tell you, you can DEFINETLEY feel the Lipoderm working more when it is on then when it is not. I truely believe it assists in driving the Lipoderm in for better absorption.
Here is where I am undecided as of yet. I eat pretty healthy and well balanced now, but I want to go on a true cut. I am undecided if I want to do a SKD, CKD or TKD diet. Any advice or input would be GREATLY appreciated. Good luck to all the testers. I hope we all have tremendous results!
God, Ive been torn about/dreading posting pics on here, but here are my before pics. Please dont laugh to hard :
Besides my regimen of Napalm/Lipoderm, I plan on taking the following also:
DCP by RPN
Prime by USPLabs (If It Ever Gets Here!!!!!!!!!)
Last edited by mrchristian; 09-09-2008 at 01:39 PM.
- 09-03-2008, 10:22 PM
sub'ed on this I really do want to see the results of running both these together. Had I thought about it at the time of buying my Napalm I would of got it too haha!
09-04-2008, 10:11 AM
09-04-2008, 11:26 AM
09-05-2008, 10:01 AM
What does everyone think I will have more success with preserving muscle while losing weight? TKD OR CKD diet?
09-05-2008, 10:15 AM
09-05-2008, 10:34 AM
I feel I do fine with CKD but it is really up to the person. The big thing that is great about TKD is it gives you that extra bump of energy when lifting heavy in the gym.
With that in mind if it is easier for you to train with that energy then it would help to keep your strength up.
One thing about a low carb. diet is that it makes your muscles go flat so I like to judge things by strength slightly more.
09-05-2008, 10:47 AM
09-05-2008, 11:21 AM
09-05-2008, 11:33 AM
I really don't feel TKD hinders the diet all that much as long as your not taking in crazy amounts of carbs.
I know what your saying though! By my friday depletion workout (just got done with it) I am dead! thankfully with the refeed right after it I get a second wind! hehe.
I feel you though man! I have to fight to keep going esp. on wed. and thur. when running that really drains me!
09-05-2008, 11:42 AM
09-05-2008, 02:03 PM
09-05-2008, 03:44 PM
09-05-2008, 04:21 PM
09-05-2008, 04:49 PM
09-05-2008, 04:50 PM
09-06-2008, 08:57 PM
09-06-2008, 09:08 PM
Is this protocal more effective than just running napalm straight through? say a 3 week on/1 week of protocal. Ill be watching this log of course.
09-06-2008, 09:23 PM
09-06-2008, 09:31 PM
09-17-2008, 01:03 PM
09-17-2008, 01:49 PM
09-17-2008, 01:50 PM
Nope, mine hasnt arrived yet. I just wanted to get this up to get feedback. Tony told me that they would be sending to us this week.
09-17-2008, 08:24 PM
09-17-2008, 10:58 PM
10-15-2008, 11:31 AM
10-15-2008, 01:23 PM
We have had a major backorder on Napalm for the past 6 weeks, but the light is starting to show. Hopefully, it will be out within the next 10 days. We again apologize for the inconvenience.
M.Ed. Ex Phys
12-13-2008, 06:57 PM
Holy **** I finally received the Napalm/Lipoderm. To be perfectly honest, I had completely forgot about this. To be continued in early '09....
12-13-2008, 07:01 PM
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