My experiments with Resveratrol and lecithin

OK, so after all the discussions about solubility and bioavailability of resveratrol, I thought I would try out some regular lecithin from my health food store (soy based, of course!) [sfty]


I used both some 99% purity and 50% extract, enough for a 800 mg dose of resveratrol (look at the little signs to see the weights). The full titles in the expanded pics say what they are.

There are 5 pics, sort of in reverse order. They are:

1) both Resveratrols before addition

2) Resveratrols after 1 minute of stirring-still some chunks on top of liquid.

3) Resveratrols, 5 minutes after stirring is complete (notice the settling of the powder if you can see it)

4) Resveratrols + a pinch of lecithin, 10 minutes after stirring, definitely more of a suspension. Some bubbles on surface, indicative of a surfactant.

5) Resveratrols + lecithin, 80 min. after stirring. Some minor settling, still quite a bit in suspension.

http://s188.photobuc...z139/malbecman/


Any comments?

Enjoy!

Definitely works as well as Miralax. I assume the bio-availability is the same, and teh same as for tween 80 from the patent literature. Cyclodextrin was also mentioned in the patent if I recall correctly.

I'm switching to lecithin from Miralax

The next step would be to evaporate the water from the mixture; the resulting powder would be a water-soluble resveratrol, presumably more potent than the straight powder, suitable for encapsulating. An industrial grade spray dryer could do it very quickly.

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Don't know if this was posted before:

J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):2950-8.Links
Development and evaluation of emulsion-liposome blends for resveratrol delivery.Hung CF, Chen JK, Liao MH, Lo HM, Fang JY.
School of Medicine, Fu Jen Catholic University, Taipei, Taiwan.

Nano- and submicron-sized vesicles are beneficial for the controlled delivery of drugs. Resveratrol, the main active polyphenol in red wine, was incorporated into various combinations of emulsions and liposomes to examine its physicochemical characteristics and cardiovascular protection. The blends of emulsion-liposome were composed of coconut oil, soybean lecithin, glycerol formal, and non-ionic surfactants. Multiple systems were assessed by evaluating the droplet size, surface charge, drug encapsulation, release rate, and stability. The vesicle diameter of the systems ranged from 114 to 195 nm. The liposomal vesicles in the systems had smaller diameters (of 43 approximately 56 nm) (F6 and F7). Drug encapsulation of approximately 70% were achieved by the vesicles. The inclusion of resveratrol in these systems retarded the drug release in both the presence and absence of plasma in vitro. The emulsion-liposome blends which incorporated Brij 98 (F5) exhibited the slowest release at zero-order for resveratrol delivery. Treatment using resveratrol in the blended formulations dramatically inhibited vascular intimal thickening, which was tested in an experimental model in which endothelial injury was produced in normal rat carotid arteries. Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity. We concluded that encapsulation by the emulsion-liposome blends is a potent way to enhance the preventative and therapeutic benefits of resveratrol.
PMID: 17048503 [PubMed - indexed for MEDLINE]

Have to keep in mind that they are talking in vitro. Also, they compared the effect of the emulsion with resveratrol in what vehicle? Things might be better explained in the full paper which I didn't get yet.

Malbecman, might you be able to try dissolving the resveratrol in a small amount of EtOH, then diluting it in lecithin + water? (I'm only guessing that would work; does lecithin dissolve in water?) I'm just thinking about particle size reduction here. There was some amount of settling visible in the pics- is that due to large particle size? My impression of the PEG/EtOH rsv emulsions was that they were pretty stable. I just got 200 gm of synthetic in the mail today, so it's time to rev up the lab...

I will try some ETOH next, thank niner. I do notice that the lecithin works better if you dissolve it into some warm water first before you add the Resveratrol; it takes awhile for the small lecithin particles to go into solution. You can slowly see the small lecithin balls dissolve from the outside-in over ~2-3 minutes....

In awe, that looks like an interesting paper. Unfortunately, I can't get it, its on the dreaded InGenta Connect service and even for me, with a major University account, they want $210 for the paper. [ang]

Two HUNDRED Ten dollars!? Holy crap. Best not to get me started on the journal publication industry. That is completely out of control.

Wouldn't that concoction taste absolutely wretched, though?

No worse than lecithin alone if you use a 98% or better extract; but I was thinking of putting it in a pill = no taste.

Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity.
PMID: 17048503 [PubMed - indexed for MEDLINE]

Have to keep in mind that they are talking in vitro.

The above quote implies some in vivo experiments too, no?

You've got that backwards.

Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity.
PMID: 17048503 [PubMed - indexed for MEDLINE]

Have to keep in mind that they are talking in vitro.

The above quote implies some in vivo experiments too, no?

No, no, interaperitoneal injection means that they squeezed some of that grape juice into their abdomen via syringe, so it's vitro. It'd be vivo if they took some tissues and looked at them under a microscope after bathing them in welch's immortality serum.

How much soy lecithin should be used per gram of 98% resveratrol?

Don't know if this was posted before:

J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):2950-8.Links
Development and evaluation of emulsion-liposome blends for resveratrol delivery.Hung CF, Chen JK, Liao MH, Lo HM, Fang JY.
School of Medicine, Fu Jen Catholic University, Taipei, Taiwan.

Nano- and submicron-sized vesicles are beneficial for the controlled delivery of drugs. Resveratrol, the main active polyphenol in red wine, was incorporated into various combinations of emulsions and liposomes to examine its physicochemical characteristics and cardiovascular protection. The blends of emulsion-liposome were composed of coconut oil, soybean lecithin, glycerol formal, and non-ionic surfactants. Multiple systems were assessed by evaluating the droplet size, surface charge, drug encapsulation, release rate, and stability. The vesicle diameter of the systems ranged from 114 to 195 nm. The liposomal vesicles in the systems had smaller diameters (of 43 approximately 56 nm) (F6 and F7). Drug encapsulation of approximately 70% were achieved by the vesicles. The inclusion of resveratrol in these systems retarded the drug release in both the presence and absence of plasma in vitro. The emulsion-liposome blends which incorporated Brij 98 (F5) exhibited the slowest release at zero-order for resveratrol deliverytment using resveratrol in the blended formulations dramatically inhibited vascular intimal thickening, which was tested in an experimental model in which endothelial injury was produced in normal rat carotid arteries. Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity. We concluded that encapsulation by the emulsion-liposome blends is a potent way to enhance the preventative and therapeutic benefits of resveratrol.
PMID: 17048503 [PubMed - indexed for MEDLINE]

Have to keep in mind that they are talking in vitro. Also, they compared the effect of the emulsion with resveratrol in what vehicle? Things might be better explained in the full paper which I didn't get yet.

I find this highly relevant; I spoke to my 87 year old father, who has had congestive heart failure and has been taking resveratrol for two months (a quarter teaspoon of synthetic 99%, about 0.5 to 0.8 grams I estimate). He got back from a visit to the cardiologist, who tells him his heart function has improved by 38%.

Here's another paper:

Circ J. 2007 Mar;71(3):397-404.
Resveratrol ameliorates experimental autoimmune myocarditis.Yoshida Y, Shioi T, Izumi T.
Department of Internal Medicine and Cardiology, Kitasato University School of Medicine, Sagamihara, Japan.

BACKGROUND: Myosin-induced autoimmune myocarditis of rats is a model of human dilated cardiomyopathy. Resveratrol is a natural polyphenol found in grapes and wine that is reported to have cardioprotective and immunomodulatory effects. METHODS AND RESULTS: To examine the effect of resveratrol on myocarditis, vehicle or resveratrol (50 mg/kg per day) was administered to cardiac myosin immunized rats 1 day before the immunization. At 14 days after immunization, resveratrol had preserved cardiac function of myosin-immunized rats according to echocardiographic analysis. The heart weight/tibial length ratio of vehicle-treated myosin-immunized rats was increased by 1.8-fold compared with unimmunized rats, and resveratrol attenuated the heart weight increase. Resveratrol significantly decreased cellular infiltration, fibrosis, and expression of inflammatory cytokines in the myocardium. Expressions of antioxidant genes were increased in myosin-immunized hearts, and resveratrol decreased those expressions. Resveratrol also attenuated myocarditis 21 days after immunization. SIRT1, a potential effector of resveratrol, was increased in the myocardium of myosin-immunized rats compared with unimmunized rats. The SIRT1 protein was localized mainly in infiltrating mononuclear cells. CONCLUSIONS: Resveratrol significantly ameliorated myocardial injury and preserved cardiac function in a rat model of autoimmune myocarditis. Resveratrol may be a therapeutic modality for myocarditis.

PMID: 17322642

Great news!

How much soy lecithin should be used per gram of 98% resveratrol?

I'm still playing with that a bit. It does not take very much, I am only using ~1/4-1/2 tsp of soy lecithin right now in ~1 1/2 cups water....
Again, let it dissolve first, it takes some time, then add your resveratrol...

What kind of cost effective equipment could do automatic stirring in a home /kitchen environment?
Should I take precautions towards development of micro-biological contamination in this liquid environment?

What kind of cost effective equipment could do automatic stirring in a home /kitchen environment?
Should I take precautions towards development of micro-biological contamination in this liquid environment?

A conventional kitchen mixer run on low speed would probably work, or maybe a blender if it went slow enough. Chemists use magnetic stirrers, where a Teflon coated magnet bar inside the beaker or flask is driven by a motorized magnet device that the container sits on. Something like this could be built at home given a garage full of salvaged parts, assuming you could buy the stir bar somewhere. You probably don't need to go much beyond normal housecleaning to keep microbes at bay if you are consuming solutions quickly. If you wanted to store bulk solutions for a while then you might run into a bigger microbe problem. Chemical decomposition is also more rapid in the liquid phase.

Chemists use magnetic stirrers, where a Teflon coated magnet bar inside the beaker or flask is driven by a motorized magnet device that the container sits on.  Something like this could be built at home given a garage full of salvaged parts, assuming you could buy the stir bar somewhere.

http://sciencekit.com/ sells to individuals.

Has anybody else tried the lecithin technique with 50% resveratrol? I've got a lot of 50% powder and to "use it up" added about 800 mg (400 mg resveratrol) to my daily dose of a gram of 98% resveratrol with lecithin. I've taken up to 1200 mg (600 mg of resveratrol) of 50% powder per day for extended periods of time with no effects from the emodin. It could have just been a coincidence. I might have had a bug. But the apparent emodin effects of adding the 800 mg of 50% powder to my lecithin augmented resveratrol dose were unpleasantly dramatic.

I finally got a chance to try lecithin with resveratrol. The result does not so much taste yucky as feel yucky, sort of like drinking raw egg whites.

I used a new batch of 98% resveratrol I've acquired; the particles are supposed to be under 20 microns. I can't measure it, I am trying to confirm the exact particle size. However, the particles are so small they can be stirred into water and appear to form a suspension that is extremely slow to settle, if indeed it ever does; I've not waited long enough yet to see. The small particle size combines with Miralax or lecithin much more quickly and thoroughly than larger particle sizes, and no large particles settle out of suspension, as had happened previously with Miralax an 80 mesh or smaller resveratrol extracts.

Maxwatt,

How much lecithin did you use? I'm only adding 1/4-1/2 tsp now to 8-10 oz of water. There is a little sliminess to it but nothing I felt was bad tasting. I agree, it looks like the suspension will take forever to settle. Now I might have to get ahold of some Miralax just for comparison's sake on my end.

I finally got a chance to try lecithin with resveratrol.  The result does not so much taste yucky as feel yucky, sort of like drinking raw egg whites.

I used a new batch of 98% resveratrol I've acquired; the particles are supposed to be under 20 microns.  I can't measure it, I am trying to confirm the exact particle size.  However, the particles are so small they can be stirred into water and appear to form a suspension that is extremely slow to settle, if indeed it ever does; I've not waited long enough yet to see.  The small particle size combines with Miralax or lecithin much more quickly and thoroughly than larger particle sizes, and no large particles settle out of suspension, as had happened previously with Miralax an 80 mesh or smaller resveratrol extracts.

I've just got some 99% resveratrol in to do the same thing. I've been taking a heaping tablespoon of lecithin over the past week (LEF brand) with a glass of water. I was surprised that it was basically tasteless. Tomorrow I'll start mixing resveratrol with it.

Anyone know how many grams of high purity resveratrol powder are in a teaspoon?

Stephen

After all this suspension talk I had to try it!

I took a tall glass of filtered water (16 OZ) and added 1/2 TSP of Lecithin granules (Lewis Labs) and stirred and stirred and stirred. After about 5 minutes the Lecithin was dissolved. I then added about 1 TSP of 98% TR Powder from RevGenetics and again stirred and stirred and after about 4 minutes the powder was fully in suspension and I could no longer detect any particles by eye. So I drank it down and lived to tell about it!

I've just got some 99% resveratrol in to do the same thing. I've been taking a heaping tablespoon of lecithin over the past week (LEF brand) with a glass of water. I was surprised that it was basically tasteless. Tomorrow I'll start mixing resveratrol with it.

Anyone know how many grams of high purity resveratrol powder are in a teaspoon?

Stephen

US teaspoon ~= 4.93 ml

I've seen PC 99% t-resv. listed as 0.35-0.42g/ml

Therefore 1 US teaspoon 99% t-resv. powder likely equals ~2 grams. YMMV.

I had been using 1, 100mg Country Life cap twice a day since late March 07.
About 5 days ago I started opening the 2 caps into a shot glass, then adding 1 tsp of lecithin granules and about 1/2 oz of vodka (40% EtOH) and stirring for a minute or so. While it is not all in solution, there is not much solid granule left. Taste is not pleasant, (somewhat bitter), but not revolting. I take my daily dose in 1 shot now, as someone remarked that the spike in blood concentration is the best way to get the benefit. When my CL caps are gone, I will change to 99% powder and increase the dose to about 500mg. per day.
Haven't noticed any significant effects yet. I am 63 years old, have had a pacemaker for 2 years for bradycardia (very slow heartrate) and was diagnosed as diabetic about a year ago although all my glucose tests have been normal since initial diagnosis. Will be getting some tests this month and will share results with you. Also started ALCAR and l-carnosine at same time as Resv. Comments/questions are welcome.

... Also started ALCAR and l-carnosine at same time as Resv. Comments/questions are welcome.

Suggest adding an anti-oxidant that is effective at the mitochondrial membrane if you take ALCAR, as it increases ROS and you need to quench the free radicals to avoid oxidative damage to the cell. R-alpha lipoic acid is preferred by many, though some claim the cheaper racemic mixture is more cost-effective. There is a thread on that topic.

Other such antioxidants include n-tert butyl hydroxylamine and PBN.

Back to resveratrol:

I was using about 1 tsp in a cup of water, about two to four times the amount Malbecman used. Super slimy. Little taste. I will try again.

The most recent batch of 98% resveratrol I've acquired passes through a 120 mesh screen. Not quite micronized, but better than the 80 mesh grades we've been using. It goes into suspension when stirred in water. It doesn't dissolve, tiny particles are clearly visible, but they don't settle before I get bored and drink it. The particles are so small that brownian motion keeps them suspended? Is this more bioavailable? Certainly there is more surface area than with larger particle sizes, which is thought to be helpful for absopbtion at the cellular level. I'm going to try adding this to water before adding lecithin. It should also dissolve in 80 proof vodka better than a coarser-particle sized resveratrol.

The most recent batch of 98% resveratrol I've acquired passes through a 120 mesh screen. Not quite micronized, but better than the 80 mesh grades we've been using

Were did you buy this? I'm highly interested. What is the price wrt. T-Res with "normal" partical size?

The most recent batch of 98% resveratrol I've acquired passes through a 120 mesh screen. Not quite micronized, but better than the 80 mesh grades we've been using

Were did you buy this? I'm highly interested. What is the price wrt. T-Res with "normal" partical size?

Same price. PM or email me for details.

FWIW. adding a couple of teaspoons of cider vinegar to the lecithin water improved solubility both of lecithin and of water. Also should halp the stability of t-res in an aqueous solution; not that I expect it to stand around for long.

I just mixed up and drank a 1 g dose of 99% resveratrol with a heaping teaspoon of LEF's lecithin in about 8 oz of water. It seemed to mix very well and was basically tasteless.

Stephen

Optimal Resveratrol mix question:

In preparation for the time when I purchase some high purity res powder I am thinking about how best to consume it and what I would need to buy, so that I can cost it out.

I think I will go with lecithin since Mirilax seems to be an American thing.

I think I might also add quercetin. Would purchasing quercetin powder and adding it to the mix be better than popping a quercetin pill, or is there no significant difference?

Lastly how important or beneficial would the addition of grape seed extract be? I am keen to not over complicate things but I'm wondering if this would be a worthy inclusion?

Any thoughts appreciated.

LEF is way high on grape

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Optimal Resveratrol mix question:

In preparation for the time when I purchase some high purity res powder I am thinking about how best to consume it and what I would need to buy, so that I can cost it out.

I think I will go with lecithin since Mirilax seems to be an American thing.

I think I might also add quercetin. Would purchasing quercetin powder and adding it to the mix be better than popping a quercetin pill, or is there no significant difference?

Lastly how important or beneficial would the addition of grape seed extract be? I am keen to not over complicate things but I'm wondering if this would be a worthy inclusion?

Any thoughts appreciated.

Grape seed extracts may be beneficial in their own right, but they do not activate SIRT1, which is the reason so many are taking resveratrol in high doses.
Quercetin is thought to increase the potency of resveratrol through competitive inhibition of glucoridation. IMO, its addition is unnecessary if resveratrol is taken with or near meals; most foods will competitively inhibit glucoridation, especially but not only foods with onions, which are rich in quercetin. Remember the rodent studies that started the Imminst resveratrol craze showed significant effects when administered with food, without quercetin or bioterpin or grape seed extract or magic purple air-tight nitrogen-sealed oil-filled capsules.