Transdermal Phosphatidyl Choline
- 05-01-2004, 07:22 PM
Transdermal Phosphatidyl Choline
Does anyone have any thoughts on this subject. I am thinking of making a solution similar to that described by Big Cat, with Phosphatidyl Choline aka lipostabil. Who thinks that it would work, and who thinks that there are better compounds out, besides Phospatidyl Choline. I have used yohimburn, lipoderm-y, lipoderm ultra, and qfs transdermal PGF2a, and I have failed to get the result that I wanted out of any of them. Any thoughts on any other substances would be appreciated
- 05-01-2004, 08:23 PM
I'm not sure this is the same compound but...
Name of Substance
The compound is huge and I couldn't find the MF or MW. I could add it up, but like I said it's huge. Just by looking at it I'd say it is rather unlikely to be a good Transdermal.
05-02-2004, 02:49 PM
05-23-2004, 07:54 PM
Its not that huge, choline weighs in around 104 and unless the two fatty acids are excessively large, I don't think the weight will be that big. The question rather is, is the molecule more polar or more organic. It has a hydrophillic head (choline + phosphate) and a hydrophobic tail (two fatty acids). Answering that is crucial to determine how well it will stay in the benzyl. It does however appear to be rather amphiphillic itself and may therefor not even require to stay in the benzyl completely to assure good local delivery.
A question that I'm stuck with though, what effects are you hoping to elicit with Phoshatodylcholine ?
05-23-2004, 07:56 PM
Never mind, I found it. Very interesting indeed. Let me know how this works out.
Aesthetic Plast Surg. 2003 Jul-Aug;27(4):315-8. Related Articles, Links
The use of phosphatidylcholine for correction of localized fat deposits.
Subjects with localized fat deposits commonly receive suction lipectomy as a cosmetic procedure. A new office procedure for correction of those superficial fat deposits was applied in 50 patients by injection of phosphatidylcholine. The method itself consists of using a 3OG1/2 insulin needle to inject about 5 ml (250 mg/5 ml) of phosphatidylcholine into the fat, distributing it evenly in an 80 cm2 area. Pre- and posttreatment photographs were taken for technical planning and analysis of the results over the long term. A clear improvement occurred in all, with a marked reduction of the fat deposits without recurrence over a 2-year follow-up period and no weight gain. The injection of phosphatidylcholine into the fat deposits is a simple office procedure that can sometimes postpone or even replace surgery and liposuction.
05-23-2004, 08:11 PM
Ok, I spent a whole 5 minutes researching this and I think the main problem is that you need a lot of PC to get into that tissues, since injections are along the lines of 250 mg per ml. This prompts me to suggest possibly looking into ways to make it more effective, such as the incorporation of PC into the cell and the type of PC used. On the latter issues I did find research suggesting that the higher the degree of unsaturation and the lower the elongation of the fatty acids the more resistant a cell becomes to insulin, which may be one of the ways it helps reduce fat.In other words, the more fluid your PC (the lower the melting point), the better.
05-23-2004, 09:29 PM
05-23-2004, 09:47 PM
Yes, I must say this has intrigued me drastically. Together with the proof now, i can definitely see a use for this. it appears PC incorporation into the membrane increases fluidity, which not only facilitates the release of fatty acids, it also seems to have an effect on LPL activity and interferes sterically with the functioning of alpha adrenoreceptors.
In practical application, 5 ml of 250 mg/ml is used, spread out over a certain surface area. That seems fairly large, and hard to achieve. However injects are spread out over 7-14 days, so with daily or at least more frequent application, a good local transd would do the trick. Here are the factors we would have to adress :
1.getting the TD to work. Skin becomes resistant to lipid layer surfactants after a single application. Most topicals as they are wouldn't exert a real effect for longer than two weeks. Pre-treatment with DMSO is an absolute must therefor to counter this.
2.Getting a good preparation. I see lipoderm ODB contains lecithin. Obviously its crap. that's probably because A) it doesn't contain much lecithin and B) most products called lecithin contain less than 20% actual PC. So finding some high quality PC is essential, not only regarding purity, but regarding fluidity. The lower the melting point, the better.
3.Possibly facilitating the effects of PC by finding factors that increase membrane incorporation etc.
05-23-2004, 10:51 PM
PC is actually composed of 6 different phospholipids. different concentrations in egg and soy. found a site that sells individual phospholipids. they have way too many of them.Originally Posted by Big Cat
just going to look for a site that sells a pure extract from soy, apparently egg is really expensive.
05-24-2004, 10:34 AM
PC can probably be composed of more than 6 phospholipids. But it also means it can be purified to contain only one specific phospholipid. If you can find a short one that is poly-unsaturated, you'd have the best results is my guess.
05-24-2004, 04:26 PM
there is claims that lipostabil (injectable Phosphatidyl Choline) causes apoptosis ( cell suicide) of fat cells when adminstrated.
05-24-2004, 04:52 PM
Its very possible. Increased membrane fluidity beyond a certain point has to affect the integrity of a cell. It would certainly explain why people kept the weight of so long afterwards, lower fat cell count leads to a lower body-fat setpoint.
05-24-2004, 10:08 PM
maybe i should just find the link and send it to you. they have polar, non-polar and some other ones. too bad i start biochem next semester. I could really use the info right now!Originally Posted by Big Cat
05-25-2004, 06:00 AM
Hmmm, yeah you better send me a link. Phosphatodylcholine always has a polar head and apolar tail. since its PHOSPHATOdylCHOLINE, it always contains the polar phosphate and the polar choline. Since its a phospholipid, it always contains two alkyl chains. These are always non-polar. Since any fatty acid can attach itself to a phospholipid, there are as many kinds of phosphatodylcholine as there are fatty acids.
05-25-2004, 01:39 PM
since this is a chemical house, i have no idea what the price is. it isn't listed. my guess is it's higher than just getting the mix refined from soy.Originally Posted by Big Cat
anyway here's the page with more phosphatidylcholine types than you can shake a stick at!
anyone else looking at this, will get the craziness that is organic chemistry.
05-25-2004, 03:42 PM
Phew, hard to keep a good product, only 3 month shelf life for poly-unsaturated products. They do offer specific synthesis, one could come up with an ideal phosphatodylcholine, but to personally do it, I'd have to read up a lot more about cell-membrane biology. off the list linolenoyl seems to be the best. poly-unsaturated, only 18 carbon chains, all cis, guaranteed to cause more hindrance and greater fluidity.Originally Posted by fiddler
On a brighter note, I found some old notes of mine for transdermals that listed 1% PC as one of the penetration enhancers. I haven't been able to find any paper or study that lead me to that conclusion, but if its there its there for a reason. That definitely makes it a good candidate for TD delivery, and being amphiphillic, a good candidate for local delivery.
05-27-2004, 04:53 AM
So lipoderm ODB is crap as a whole, or the lecithin in ODB is crap? I was thinking of trying it.Originally Posted by Big Cat
05-27-2004, 01:23 PM
As a whole :
1.It does not apply TPDS correctly (Nimni et al, 1989,1997,1998) by omitting acetone, which is clearly the better penetrant as demonstrated by onken and Moyer in 1963, and explained by Idson in 1975, basing himself on Mclellan (1949) and Fitzgerald (1957).
2.TPDS gets ****ed up by adding non-evaporating products, such as penetration enhancers. The PE's in Lipo are only effective in a fairly large volume (several percent each) forming a substantial amount of product that inhibits the evaporation of the first phase of TPDS. This causes the first phase to partially traverse the skin, still carrying some of the product (since it wasn't funneled to the second phase by evaporation). The first phase, being a better solvent, is not a carrier and results in systemic delivery of a significant amount of product.
3.Said PE's are also good solvents for the organic molecules, more so than benzyl alcohol. Benzyl forms micelles with organic compounds in an aqueous environment only, in a non-polar environment the compounds show more affinity for the less polar solvent , including most of the PE's included. This means apart from the amount dissolved in the non-evaporated first phase, an amount of compound is dissolved in the susbtantial amount of PE included. These ALSO do NOT act as carriers and result in systemic delivery.
4.Combined points 2 and 3 completely negate the point of adding PE's, since whatever gets across the skin more than without them, is taken up systemically. Given the good penetration rate of the benzyl micelles one could probably assume that LESS product makes it to the local area. My experiences confirm this, a Lipo analog was outperformed by the much cheaper pure TPDS in correct application (using only benzyl, acetone and isopropanol). You can find instructions on making the latter for a whole lot less money than Lipo, in this section as well.
5.Lipo also contains glycerol, a highly hygroscopic product. That means it has a high affinity for water. These substances tend to dehydrate the skin and decrease permeation (Idson, 1975). This has also been reiterated in The work of Barry et al in 1972 concerning diminished returns of topical application. A single application evoked a resistance to permeation that lasted in excess of one week, and one of the possible explanations was increased dehydration of the skin.
6.Glycerol does not readily penetrate the skin, mostly because it draws water, forming a large acqueous mass that is usually lost and does not penetrate. Apart from that it also shows interaction with the hydroxyl group on the benzyl alcohol, and may prevent benzyl alcohol from penetrating, effectively reducing the amount of vehicle, again resulting in a) reduced uptake, and b) increased systemic uptake of what does pass.
7.One of the ingredients is tyramine, a product that shows very limited lipolytic action and contrary to that, a very large amount of ANTI-lipolytic action due to its interactions with amino oxidases. something that is supposedly solved by the addition of products like NAC. Except these products only adress MAO, and not the principle SSA oxidation. And aparrently someone forgot to inform the people at avant that NAC is too hydrophillic to form a micelle with benzyl, and therefor will NOT pass the skin, and in case any minimal amount should make it through, it will be taken up systemically.
8.Another ingredient is octopamine, a specific b3-agonist. This is of course ridiculous since norepinephrine shows a 2-fold higher activation of the b3-receptor than octopamine does, humans possess very little b3 receptors, and of all things subcutanoeus fat contains the very least amount of b3-receptors of all fat depots. On top of that, the principle ingredient yohimbine blocks the alpha-2 receptor, which effectively inhibits the b3-receptor.
9.It contains caffeine. In itself not a bad choice, except they seem to claim that local caffeine acts as a diuretic. Xanthines work as diuretics via effects on the kidney. Local caffeine has no effect as a diuretic. On top of that, why did they opt for caffeine and not a less water-soluble xanthine like aminophylline ? Aminophylline that after has extensive research behind it as a topical fat loss aid.
These are just SOME of the concerns associated with the efficacy of Lipoderm ODB. That is not to say it doesn't work at all, but why fork over that cash if you can make an imminently better product yourself for so much less ?
05-28-2004, 02:35 AM
First, thanks for such an in-depth response to why it's crap . What you mention about tyramine, is that only as a topical, or does that apply to oral supplementation like with Avant's H.E.A.T or Xtreme Formulations Chizled as well?Originally Posted by Big Cat
05-29-2004, 03:29 PM
The same problems apply systemically as they do locally, tyrine gets oxidized by MAO and SSAO and has anti-lipolytic properties. it is not entirely excluded that this anti-lipolytic activity isn't related to other things as well, but studies seem to link it primarily to its interaction with SSAO, since MAO inhibition did not reduce the anti-lipolytic effects.Originally Posted by supersoldier
05-30-2004, 08:55 AM
Assuming, I have phosphatodylcholine, I still don't know what to mix together to get a transdermal gel or solution.
06-02-2004, 09:11 PM
we have been after this one for months...good luck getting it to work. If you do send me an email we should talk...
06-03-2004, 12:04 PM
if you like I can have a look at what you have and tell you what changes you could make to get it to work better.
11-14-2004, 03:47 PM
big cat what do you think about using L-Alpha-
L-alpha-glycerylphosphorylcholine is a substance derived from soy lecithin. It is phosphatidylcholine without the two fatty acid chains contained within the phosphatidylcholine structure. Although it is popularly referred to as a phospholipid, it is not. It is a phospholipid-derived substance.
here is some studies i found:
finaly a research was published on Lipostabil, just released last july of this year.
Detergent effects of sodium deoxycholate are a major feature of an injectable phosphatidylcholine formulation used for localized fat dissolution.
Rotunda AM, Suzuki H, Moy RL, Kolodney MS.
Division of Dermatology, University of California Los Angeles, David Geffen School of Medicine, Los Angeles, California, USA.
BACKGROUND: Phosphatidylcholine injections are becoming an increasingly popular technique to treat localized fat accumulation. This formula is composed primarily of phosphatidylcholine and sodium deoxycholate, a bile salt used to solubilize the natural phospholipid in water. The mechanism through which this injectable phosphatidylcholine formulation causes localized fat reduction is unknown. OBJECTIVE: To investigate the active component and mechanism of action of an injectable phosphatidylcholine formulation in clinical use. METHODS: Cell viability and cell membrane lysis assays were performed on cell cultures and porcine skin after treatment with the phosphatidylcholine formula, isolated sodium deoxycholate, or common laboratory detergents Triton-X 100 and Empigen BB. In addition, we described the histologic changes after injection of these substances into porcine tissue. RESULTS: A significant and comparable loss of cell viability, cell membrane lysis, and disruption of fat and muscle architecture was seen in cell cultures and tissue specimens treated with the phosphatidylcholine formula and isolated sodium deoxycholate. These findings were similar to the effects produced after treatment with laboratory detergents. CONCLUSIONS: The phosphatidylcholine formula popularly used in subcutaneous injections for fat dissolution works primarily as a detergent causing nonspecific lysis of cell membranes. Our findings suggest that sodium deoxycholate is the major active component responsible for cell lysis. Detergent substances may have a role in eliminating unwanted adipose tissue. It is advised that physicians use caution until adequate safety data are available.
CONTROVERSIES IN DERMATOLOGIC SURGERY
Treatment of Lower Eyelid Fat Pads Using Phosphatidylcholine: Clinical Trial and Review
Glynis Ablon, MD*, and Adam M. Rotunda, MD
Background. Injectable phosphatidylcholine, a lecithin-derived phospholipid, has been previously demonstrated to improve the appearance of infraorbital fat pad herniation. Current use internationally has led to a significant interest in this novel substance.
Objective. To evaluate the efficacy and safety of injectable phosphatidylcholine, we conducted an open-label study for the treatment of infraorbital fat pad herniation.
Methods. Patients received 0.4-mL phosphatidylcholine (50 mg/mL) injections within infraorbital fat pads every 2 weeks. Patient and physician grading of fat herniation, side effects, digital photographs, and a follow-up questionnaire was recorded.
Results. Ten of the 13 enrolled patients had three to five treatments. Improvements in fat herniation were reported in 80% and 70% of patients as graded by the physician and patients, respectively. Sixty percent of patients assessed their improvement as equal or greater than 5 points (on a 10-point fat herniation scale); however, the physician judged 40% of patients improving to this degree. Little or no response was seen in three patients. Side effects included burning, erythema, and swelling at the injection site. At follow-up averaging 9 months, 50% of patients reported persistence of benefit, 20% experienced some fading, and 30% were the nonresponders.
Conclusions. Injectable phosphatidylcholine is a novel treatment for infraorbital fat herniation that may benefit some patients who are considering blepharoplasty. Larger studies evaluating long-term safety and efficacy of phosphatidylcholine for cosmetic purposes are warranted.
11-14-2004, 03:55 PM
L-Alpha-Glycerylphosphorylcholine (Alpha-GPC) is avilable in pure powder
regular PC highier purity i found is 35%:
im thinking to try transdermal PC soon, with T3, Celn, nad capsicam to enhance absorption.
11-17-2004, 03:26 PM
Just something I noticed.... BC and others are going on about how you need 250mg/ml but in the orignal post, it was listed as "250mg/5ml" which would indicate to me a total of 250mg delivered via 5ml of solution total.. No? If I'm right, that reduced the ammount you would need considerably... Just a minor nit I thought I'd pick.
11-17-2004, 05:35 PM
11-19-2004, 02:27 PM
That there is what I was talking about... It doesn't say 250mg/ml now does it? That's right, it says 250mg/5mlThe method itself consists of using a 3OG1/2 insulin needle to inject about 5 ml (250 mg/5 ml) of phosphatidylcholine into the fat, distributing it evenly in an 80 cm2 area.
my point stands.
01-16-2006, 01:28 PM
04-28-2006, 07:33 PM
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