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Transdermal Phosphatidyl Choline

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    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


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    I'm not sure this is the same compound but...

    Name of Substance
    Lecithin

    Superlist Name
    Lecithin
    Lecithin (soyabean)
    Lecithins

    Synonyms
    Acti-flow 68-sb
    Alcolec S
    CCRIS 7265
    EINECS 232-307-2
    Egg yolk
    Emulthin M-35
    Gliddex
    Granulestin
    HSDB 1903
    Kelecin
    Lecithin
    Lecithin, soybean
    Lecithins
    Lecithol
    Ovovitellin
    Phosphatidylcholine
    Phospholutein
    Soybean lecithin
    Vitellin

    Systematic Name
    Lecithine
    Lecithins
    Soybean lecithin

    CAS#8002-43-5

    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.

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    That is indeed the substance

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    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 ?

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    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.

    Rittes PG.

    prittes@terra.com.br

    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.

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    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.

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    Nice work BC.

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    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.

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    Quote Originally Posted by Big Cat
    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.
    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.

    just going to look for a site that sells a pure extract from soy, apparently egg is really expensive.

    fiddler

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    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.

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    there is claims that lipostabil (injectable Phosphatidyl Choline) causes apoptosis ( cell suicide) of fat cells when adminstrated.

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    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.

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    Quote Originally Posted by Big Cat
    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.
    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!

    fiddler

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    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.

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    Quote Originally Posted by Big Cat
    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.
    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.

    anyway here's the page with more phosphatidylcholine types than you can shake a stick at!

    http://www.avantilipids.com/Syntheti...dylcholine.asp

    anyone else looking at this, will get the craziness that is organic chemistry.

    fiddler

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    Quote Originally Posted by fiddler
    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.

    anyway here's the page with more phosphatidylcholine types than you can shake a stick at!

    http://www.avantilipids.com/Syntheti...dylcholine.asp

    anyone else looking at this, will get the craziness that is organic chemistry.
    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.

    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.

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    Quote Originally Posted by Big Cat
    I see lipoderm ODB contains lecithin. Obviously its crap.
    So lipoderm ODB is crap as a whole, or the lecithin in ODB is crap? I was thinking of trying it.

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    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 ?

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    Quote Originally Posted by Big Cat
    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.
    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?

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    Quote Originally Posted by supersoldier
    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?
    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.

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