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Transdermal Delivery of Resveratrol


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#1 Smithy

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Posted 19 April 2008 - 01:24 AM


In my postings in the "Maximize Reservatrol Thread", it was suggested that Transdermal Reservatrol may help maximize the effectiveness of RESV. I did some preliminary calculations based upon a research paper originally quoted by Niner, which allows one to make predictions of the Flux of various compounds based upon their molecular weight. Taking the MW of RESV, I suggested that the predicted effectiveness of Transdermal Resv would be very good.

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Despite good partitioning into the SC, the permeability of highly lipophilic
molecules is always low. This is probably due to the accumulation of lipophilic drugs
in the SC. This phenomenon was not observed with non-ionic resveratrol, which
showed higher permeability via the skin. These results support the superiority of
resveratrol for both topical and transdermal delivery. Resveratrol transport via the skin
was closely related to the vehicle in which it was formulated, with aqueous buffers
with lower pH values exhibiting good permeability/deposition. The viable
epidermis/dermis but not the SC layer acted as a diffusion barrier for resveratrol
permeation. Piceatannol, a more-hydrophilic analogue of resveratrol, showed lower
permeation compared to resveratrol. Resveratrol delivery by skin route may avoid the
degradation because the low metabolism in the skin, resulting in the possible
prolongation of half-life and sufficient concentration in the systemic circulation.
Moreover, resveratrol retained within the skin after topical application can be an
efficient way to be a therapy or prevention of UV exposure and skin carcinogenesis.
Further study is, of course, needed to confirm these efficiencies. This study indicates
the promise of further in vivo and clinical applications of resveratrol delivery via the
skin.


Based upon the new research, I'm curious about what you guys think?

Edited by Smithy, 19 April 2008 - 01:26 AM.


#2 sUper GeNius

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Posted 19 April 2008 - 01:52 AM

In my postings in the "Maximize Reservatrol Thread", it was suggested that Transdermal Reservatrol may help maximize the effectiveness of RESV. I did some preliminary calculations based upon a research paper originally quoted by Niner, which allows one to make predictions of the Flux of various compounds based upon their molecular weight. Taking the MW of RESV, I suggested that the predicted effectiveness of Transdermal Resv would be very good.

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Despite good partitioning into the SC, the permeability of highly lipophilic
molecules is always low. This is probably due to the accumulation of lipophilic drugs
in the SC. This phenomenon was not observed with non-ionic resveratrol, which
showed higher permeability via the skin. These results support the superiority of
resveratrol for both topical and transdermal delivery. Resveratrol transport via the skin
was closely related to the vehicle in which it was formulated, with aqueous buffers
with lower pH values exhibiting good permeability/deposition. The viable
epidermis/dermis but not the SC layer acted as a diffusion barrier for resveratrol
permeation. Piceatannol, a more-hydrophilic analogue of resveratrol, showed lower
permeation compared to resveratrol. Resveratrol delivery by skin route may avoid the
degradation because the low metabolism in the skin, resulting in the possible
prolongation of half-life and sufficient concentration in the systemic circulation.
Moreover, resveratrol retained within the skin after topical application can be an
efficient way to be a therapy or prevention of UV exposure and skin carcinogenesis.
Further study is, of course, needed to confirm these efficiencies. This study indicates
the promise of further in vivo and clinical applications of resveratrol delivery via the
skin.


Based upon the new research, I'm curious about what you guys think?


Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#3 tintinet

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Posted 19 April 2008 - 01:57 AM

In my postings in the "Maximize Reservatrol Thread", it was suggested that Transdermal Reservatrol may help maximize the effectiveness of RESV. I did some preliminary calculations based upon a research paper originally quoted by Niner, which allows one to make predictions of the Flux of various compounds based upon their molecular weight. Taking the MW of RESV, I suggested that the predicted effectiveness of Transdermal Resv would be very good.

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Despite good partitioning into the SC, the permeability of highly lipophilic
molecules is always low. This is probably due to the accumulation of lipophilic drugs
in the SC. This phenomenon was not observed with non-ionic resveratrol, which
showed higher permeability via the skin. These results support the superiority of
resveratrol for both topical and transdermal delivery. Resveratrol transport via the skin
was closely related to the vehicle in which it was formulated, with aqueous buffers
with lower pH values exhibiting good permeability/deposition. The viable
epidermis/dermis but not the SC layer acted as a diffusion barrier for resveratrol
permeation. Piceatannol, a more-hydrophilic analogue of resveratrol, showed lower
permeation compared to resveratrol. Resveratrol delivery by skin route may avoid the
degradation because the low metabolism in the skin, resulting in the possible
prolongation of half-life and sufficient concentration in the systemic circulation.
Moreover, resveratrol retained within the skin after topical application can be an
efficient way to be a therapy or prevention of UV exposure and skin carcinogenesis.
Further study is, of course, needed to confirm these efficiencies. This study indicates
the promise of further in vivo and clinical applications of resveratrol delivery via the
skin.


Based upon the new research, I'm curious about what you guys think?


Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)


Halluxander The Great?

#4 sUper GeNius

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Posted 19 April 2008 - 02:19 AM

In my postings in the "Maximize Reservatrol Thread", it was suggested that Transdermal Reservatrol may help maximize the effectiveness of RESV. I did some preliminary calculations based upon a research paper originally quoted by Niner, which allows one to make predictions of the Flux of various compounds based upon their molecular weight. Taking the MW of RESV, I suggested that the predicted effectiveness of Transdermal Resv would be very good.

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Despite good partitioning into the SC, the permeability of highly lipophilic
molecules is always low. This is probably due to the accumulation of lipophilic drugs
in the SC. This phenomenon was not observed with non-ionic resveratrol, which
showed higher permeability via the skin. These results support the superiority of
resveratrol for both topical and transdermal delivery. Resveratrol transport via the skin
was closely related to the vehicle in which it was formulated, with aqueous buffers
with lower pH values exhibiting good permeability/deposition. The viable
epidermis/dermis but not the SC layer acted as a diffusion barrier for resveratrol
permeation. Piceatannol, a more-hydrophilic analogue of resveratrol, showed lower
permeation compared to resveratrol. Resveratrol delivery by skin route may avoid the
degradation because the low metabolism in the skin, resulting in the possible
prolongation of half-life and sufficient concentration in the systemic circulation.
Moreover, resveratrol retained within the skin after topical application can be an
efficient way to be a therapy or prevention of UV exposure and skin carcinogenesis.
Further study is, of course, needed to confirm these efficiencies. This study indicates
the promise of further in vivo and clinical applications of resveratrol delivery via the
skin.


Based upon the new research, I'm curious about what you guys think?


Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)


Halluxander The Great?


Not bad, not bad. I like MiniMax.

#5 TianZi

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Posted 19 April 2008 - 03:15 AM

It isn't clear from this excerpt if transdermal application provides significant benefits anywhere but topically, i.e., on the skin.

#6 Smithy

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Posted 19 April 2008 - 04:25 AM

It seems that many body builders are already using RESV transdermally.

Nano Dispersion Gel

The combination of A1-E, 4-AD-EC, and 1-Diol-EC, in Nano-Dispersion Gel, is almost beyond description. In fact, the Nano-Dispersion Gel complex is right out of science fiction, except it's real. The best way to describe this stuff is to say, if you don't want it in you, don't touch it!


Reservatrol in Nano Dispersion Gel - REZ-V - In this thread, several body builders are saying positive things about transdermal resv.

Edited by Smithy, 19 April 2008 - 04:25 AM.


#7 niner

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Posted 19 April 2008 - 04:50 AM

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Based upon the new research, I'm curious about what you guys think?

Using their best formulation, they measured a flux of 2 nm/cm^2 hr. If you use a rather gigantic 200 square cm patch, that would give you 400 nm per hour, or 0.09 milligrams/hour. So that's not going to work too well. That also doesn't take into account the amount that gets held up in the subcutaneous tissues. During that entire hour, the liver is happily conjugating the resveratrol, so unless you can get it in orders of magnitude faster, you'll never see a significant amount in the plasma.

#8 Smithy

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Posted 19 April 2008 - 05:05 AM

Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)

Maxwatt's big toe already answered that in this thread.

#9 niner

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Posted 19 April 2008 - 05:13 AM

Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)

Maxwatt's big toe already answered that in this thread.

While a transdermal formulation isn't a good way to get a systemic dose, it might work for a localized problem like a joint or a skin lesion. The amount that gets through skin, as small as it is, may result in a local concentration that is higher than you could get from an oral dose.

#10 Smithy

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Posted 19 April 2008 - 05:13 AM

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Based upon the new research, I'm curious about what you guys think?

Using their best formulation, they measured a flux of 2 nm/cm^2 hr. If you use a rather gigantic 200 square cm patch, that would give you 400 nm per hour, or 0.09 milligrams/hour. So that's not going to work too well. That also doesn't take into account the amount that gets held up in the subcutaneous tissues. During that entire hour, the liver is happily conjugating the resveratrol, so unless you can get it in orders of magnitude faster, you'll never see a significant amount in the plasma.


Yes, I've noticed the very low flux of their vehicles. Their best vehicle was 10% glycerol formal in a PH 6 buffer, with a stated flux of 2.32 nm/cm^2 hr. Unfortunately, they did not test DMSO or any other vehicles commonly associated with enhancing transdermal delivery. I am still very curious to know what the flux of RESV dissolved in a DMSO vehicle would be, as there is much anecdotal evidence from members of this forum that DMSO + RESV helps with their inflammation problems.

#11 Smithy

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Posted 19 April 2008 - 05:18 AM

Only one way to find out for sure. Ask Maxwatt's big toe. Have we decided yet on a name for the little guy? :)

Maxwatt's big toe already answered that in this thread.

While a transdermal formulation isn't a good way to get a systemic dose, it might work for a localized problem like a joint or a skin lesion. The amount that gets through skin, as small as it is, may result in a local concentration that is higher than you could get from an oral dose.

You make a good point. Perhaps we need to ask maxwatt to apply DMSO + RESV solution to a large area of skin not near his toe (ie. thighs and chest), and then report whether his big toe gets any relief.

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#12 Hedgehog

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Posted 19 April 2008 - 06:19 AM

In my postings in the "Maximize Reservatrol Thread", it was suggested that Transdermal Reservatrol may help maximize the effectiveness of RESV. I did some preliminary calculations based upon a research paper originally quoted by Niner, which allows one to make predictions of the Flux of various compounds based upon their molecular weight. Taking the MW of RESV, I suggested that the predicted effectiveness of Transdermal Resv would be very good.

Now, there is finally some research on topical and transdermal delivery of RESV. I haven't have a chance to read the entire paper yet, but I'm posting it here.

Despite good partitioning into the SC, the permeability of highly lipophilic
molecules is always low. This is probably due to the accumulation of lipophilic drugs
in the SC. This phenomenon was not observed with non-ionic resveratrol, which
showed higher permeability via the skin. These results support the superiority of
resveratrol for both topical and transdermal delivery. Resveratrol transport via the skin
was closely related to the vehicle in which it was formulated, with aqueous buffers
with lower pH values exhibiting good permeability/deposition. The viable
epidermis/dermis but not the SC layer acted as a diffusion barrier for resveratrol
permeation. Piceatannol, a more-hydrophilic analogue of resveratrol, showed lower
permeation compared to resveratrol. Resveratrol delivery by skin route may avoid the
degradation because the low metabolism in the skin, resulting in the possible
prolongation of half-life and sufficient concentration in the systemic circulation.
Moreover, resveratrol retained within the skin after topical application can be an
efficient way to be a therapy or prevention of UV exposure and skin carcinogenesis.
Further study is, of course, needed to confirm these efficiencies. This study indicates
the promise of further in vivo and clinical applications of resveratrol delivery via the
skin.


Based upon the new research, I'm curious about what you guys think?


You could snort it. :) Just take more of it that way you don't have to worry about the very real dangers of DMSO. I don't even like touching that stuff in the lab w/ gloves on. We are supposed to double glove in the lab while touch DMSO. DMSO is a carrier for almost anything including dangerous compounds. If you do this make sure your skin is free from anything you don't want in your body. As a fun experiement you can try a vitamin (I think it was B vitamin) w/ dmso. You should be able to taste it in your mouth in a couple of mins. At least that is what somebody told me.




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