Micronized Resveratrol: Is it better?

In earlier posts I spoke about the importance of bioavailability and resveratrol.  We know that when a drug or supplement is taken orally it must pass through our digestive system and is metabolized.  Many substances that are not very water soluble have a hard time making it through this process without first being eliminated or structurally broken down.  This means it never makes it to it's desired destination in our bodies.  To make these types of substances more bioavailable, a method called "micronization" is implemented.

"Micronization is the process of reducing the average diameter of a solid material's particles. Usually, the term micronization is used when the particles that are produced are only a few micrometres in diameter. However, modern applications (usually in the pharmaceutical's industry) require average particle diameters of the nanometer scale." from http://en.wikipedia.org/wiki/Micronization

For example: Talcum powder is approximately 10 microns (1 micron, or um, is a millionth of a meter).  Human hair is approximately 70 um in diameter.  Micronized supplements are known to be under 10um and sometimes smaller then 1um making it onto the nanometer scale.

Now try to imagine pinching regular sugar grains between your fingers.  Can you feel the granules between your fingers?  Now imagine doing the same thing with powdered sugar.  The powdered sugar is more fine and soft and you can imagine would be much easier to dissolve in water.  This is the case with micronized drugs and supplements.

So, if trans-resveratrol is micronized does it become more bioavailable? 

I have not been able to find any published human studies showing the answer to this is a 100% yes.  That said, my research into micronized resveratrol leads me to believe that in fact it is.  It is said that Sirtis Pharmaceuticals (recently acquired by Glaxo Smithkline) experimental drug SRT501 is a micronized version of resveratrol that the company claims is up to 1000 times more potent then standard resveratrol.  The company states SRT501 is a, "formulation of resveratrol with improved bioavailability" and it also states that the company is, "focused on discovering and developing proprietary, orally available, small molecule drugs..."  Ok, so what are the other components and how small is "small molecule" drugs?  I don't like to assume but I am fairly certain Glaxo wouldn't pay $720 million for a company if it weren't producing something much better then the readily available supplement grade resveratrol.  I guess only time will tell...

Micronized Resveratrol is now available in supplement form.  Click the following link for more information on the Micronized Resveratrol I use.

I will keep you updated with any information I find out regarding micronized resveratrol.  If you come across any studies yourself please post them below.  I will leave you all with a few links to non-resveratrol related micronization research links:

http://www.sirtrispharma.com

Micronization: A method of improving the bioavailability of poorly soluble drugs

Improved Bioavailability of a Poorly Water Soluble Drug by Nanosizing

Micron-size drug particles: common and novel micronization techniques.

Live Longer,

Markus

Resveratrol Related Web Search

Comments

[Pamela McMasters Ph.D.]

There is no published data to support enhanced bioavailability of resveratrol through micronization. In fact quite the opposite is true. Micronization is being touted by some suppliers even though the data shows that it actually decreases total resveratrol absorption. It is true that some drugs and nutrients are enhanced by micronization however resveratrol is not one of them. Furthermore, once a micronized powder is packed into a capsule it aggregates within a short time due to the pressure and moisture and no longer is micronized. Biotivia has studied the issue of particle size in relation to free resveratrol and resveratrol metabolite bioavailability. Our conclusion, and that of other bio chemists, is that at a particle size of between 1 and 10 nanometers (micronized) a graph of blood plasma levels vs. time shows an initial spike of resveratrol concentration but one which is no higher than the maximum amplitude of the concentration curve shown with resveratrol particles of 200nm (normal resveratrol). In the case of micronized resveratrol the blood plasma level very quickly drops to a substantially lower level than that of normal resveratrol. The result is that the total amount of free resveratrol (area under the curve) existing in the blood plasma and tissues is significantly lower with micronized resveratrol than with normal resveratrol. In fact larger particle sizes actually increase bioavailability. Some researchers have hypothesized that this is because micronized resveratrol is much more easily cleared from the blood by the liver resulting in a rapid drop off of resveratrol blood plasma and tissue concentrations. So why does Sirtris use micronized resveratrol in their formulation? The answer is simple, to a bio chemist at least. Sirtris uses it to facilitate the complexing of the particles with cyclodextrine. This is necessary in a liquid product, such as his SRT-501 formulation. The increased potency of this synthetic analog of resveratrol comes at the expense of the full spectrum effects of natural resveratrol and is due to a molecular modification. It has nothing to do with micronization. Why do some suppliers use micronization? In our opinion, it has more to do with the higher prices they are charging than with the science behind it.

[Anthony Loera]

Pamela, admit it, you are not a PHD and simply cut and pasting this whole comment. This looks like the typical sock puppetry used to anonymously comment using a fake name.

There are alot of issues with your post.

1- The absorption charts were done by Sirtris without any cyclodextrin present. They detail this in the document that you obviously did not read.

2- The notion that micronized resveratrol becomes "un-micronized" by pressure and moisture is pretty ridiculous. The HPMC capsules would be affected by any moisture in a bottle as well if this were true. If moisture were present, most vegetarian supplements using Pfizer VCaps would "melt" and create a sticky mess inside the bottle way before it would be a problem to the "non-soluble" resveratrol. Again resveratrol is an extremely low-soluble material, and has not issues with moisture because of it.

3- 1 to 10 nanometers is not micronized. The term nanoscale is used to refer to objects with dimensions on the order 1–100 nm. While a micron is used to refer to a micrometer scale. If you really where a PHD, you would know this instead of making the same mistake as others have made.

Again, your credibility suffers when you cut-paste from a source that simply doesn't know the difference between a nanometer and a micrometer.

A

[Anthony Loera]

Here Pam,

a simple metric conversion application so you can understand the difference:

http://www.metric-conversion.net/convert_nanometers_micrometers.htm

And normalresveratrol particles are not 200nm. As shown in this old Electron photo of "normal resveratrol"

http://www.pathway2curis.com/resveratrol/SEM/thumbnails/T-max%201000x_jpg.jpg

again the picture states "um" not "nm". Regarding absorption, we can only look at the charts made public by Sirtris regarding absorption. If other folks can show a different study that shows different data than that of the Sirtris animal data, we would love to see it.

I am sure the company would then be a candidate to be bought out by Glaxo-Smith Kline for such an important observation that Sirtris would have missed entirely. It would make alot of good news for anyone to properly prove that the Sirtris data is incorrect.

We currently believe the Sirtris animal data is correct regarding absorption.

Cheers
A