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Buccal delivery superior?


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#31 Anthony_Loera

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Posted 19 February 2009 - 05:42 AM

We are looking at Xylitol with possibly a little Stivia... as sweeteners.

Initial consideration was around 50mg-100mg a piece... I am not sure we can add more than this.
Time frame?... 2-3 months (The packaging appears to be the holdup on this...)

I am just not sure about the flavors... and of course, you heard it here first.

Hi Anthony, I was just wondering what happened to this idea? I can't see a gum product on your website, and wondered if you're still working on it, or if the idea was dropped for some reason?


I just couldn't see folks buying a $8 - $10 pack of gum...

It's still being considered, but other things have come up after our initial research into this.

Cheers
A

#32 AlexanderII

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Posted 12 March 2009 - 04:19 AM

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"



I wanted to comment that there is a company in Miami Beach that already has Resveratrol film strips, like the Listerine breath strips, but with Resveratrol. (And also works as a breath strip).
I know they make them with different Resveratrol content. The Company name is Affair Co or Affair something, in Miami Beach. No other info. But I tried them last week in a party, and they tasted and smelled great, like grape.

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#33 Ringostarr

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Posted 12 March 2009 - 04:51 AM

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"



I wanted to comment that there is a company in Miami Beach that already has Resveratrol film strips, like the Listerine breath strips, but with Resveratrol. (And also works as a breath strip).
I know they make them with different Resveratrol content. The Company name is Affair Co or Affair something, in Miami Beach. No other info. But I tried them last week in a party, and they tasted and smelled great, like grape.


That's interesting Alexander: I might check them out.
I have been putting about 150 mg. of micronized resveratrol between by gum and lip - like I am "dipping" skoal or copenhagen. I swear I can feel the effects. I get a bit dizzy and definitly feel more energy. I then dissolve whats left in my mouth with water and swallow after about ten minutes. I have been taking resveratrol (through the GI tract) since 2003 but have never felt these kinds of effects. I know this stuff is reaching my bloodstream now. Buccal is the efficient way to go as far as I can tell.

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#34 niner

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Posted 12 March 2009 - 05:25 AM

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

I wanted to comment that there is a company in Miami Beach that already has Resveratrol film strips, like the Listerine breath strips, but with Resveratrol. (And also works as a breath strip).
I know they make them with different Resveratrol content. The Company name is Affair Co or Affair something, in Miami Beach. No other info. But I tried them last week in a party, and they tasted and smelled great, like grape.

I looked at the Wikipedia entry, and while they still mention buccal delivery, there is no reference to it. Reference 21 here, which is now [25] in the current Wikipedia article, is irrelevant. A search for buccal and resveratrol in pubmed turns up zero hits. Google doesn't show anything obvious. Transdermal penetration of resveratrol has been shown to be very low. I'm beginning to wonder if this wasn't planted on Wikipedia by someone trying to sell buccal formulations of small quantities of resveratrol for lots of money... Maybe I'm being too cynical. Can anyone find a reference to the 37ng/ml measurement?

#35 maxwatt

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Posted 12 March 2009 - 03:41 PM

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

I wanted to comment that there is a company in Miami Beach that already has Resveratrol film strips, like the Listerine breath strips, but with Resveratrol. (And also works as a breath strip).
I know they make them with different Resveratrol content. The Company name is Affair Co or Affair something, in Miami Beach. No other info. But I tried them last week in a party, and they tasted and smelled great, like grape.

I looked at the Wikipedia entry, and while they still mention buccal delivery, there is no reference to it. Reference 21 here, which is now [25] in the current Wikipedia article, is irrelevant. A search for buccal and resveratrol in pubmed turns up zero hits. Google doesn't show anything obvious. Transdermal penetration of resveratrol has been shown to be very low. I'm beginning to wonder if this wasn't planted on Wikipedia by someone trying to sell buccal formulations of small quantities of resveratrol for lots of money... Maybe I'm being too cynical. Can anyone find a reference to the 37ng/ml measurement?


Buccal is similar to sublingual. There is a limit to the amount that can be absorbed into the blood this way, and it is a low enough amount I suspect the effects reported are a placebo. There is not enough surface area to absorb a significant amount into the blood. Even accounting for bypassing the liver for first-pass metabolism, blood levels are lower than a large dose administered orally. A bolus administered anally would be superior in this regard. Another option for some is vaginal delivery.

It is unfortunate the search function provided is inefficient, because this has been covered, with references, in the past. I'll see if I can dig it up.

Edited by maxwatt, 12 March 2009 - 03:50 PM.


#36 hmm

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Posted 12 March 2009 - 09:31 PM

Has someone posted about this yet?

http://en.wikipedia....iki/Resveratrol

"The most efficient way of administering resveratrol in humans appears to be buccal delivery, that is without swallowing, by direct absorption through the inside of the mouth. When 1 mg of resveratrol in 50 mL solution was retained in the mouth for 1 min before swallowing, 37 ng/ml of free resveratrol were measured in plasma 2 minutes later. This level of unchanged resveratrol in blood can only be achieved with 250 mg of resveratrol taken in a pill form.[21]"

I wanted to comment that there is a company in Miami Beach that already has Resveratrol film strips, like the Listerine breath strips, but with Resveratrol. (And also works as a breath strip).
I know they make them with different Resveratrol content. The Company name is Affair Co or Affair something, in Miami Beach. No other info. But I tried them last week in a party, and they tasted and smelled great, like grape.

I looked at the Wikipedia entry, and while they still mention buccal delivery, there is no reference to it. Reference 21 here, which is now [25] in the current Wikipedia article, is irrelevant. A search for buccal and resveratrol in pubmed turns up zero hits. Google doesn't show anything obvious. Transdermal penetration of resveratrol has been shown to be very low. I'm beginning to wonder if this wasn't planted on Wikipedia by someone trying to sell buccal formulations of small quantities of resveratrol for lots of money... Maybe I'm being too cynical. Can anyone find a reference to the 37ng/ml measurement?


Buccal is similar to sublingual. There is a limit to the amount that can be absorbed into the blood this way, and it is a low enough amount I suspect the effects reported are a placebo. There is not enough surface area to absorb a significant amount into the blood. Even accounting for bypassing the liver for first-pass metabolism, blood levels are lower than a large dose administered orally. A bolus administered anally would be superior in this regard. Another option for some is vaginal delivery.

It is unfortunate the search function provided is inefficient, because this has been covered, with references, in the past. I'll see if I can dig it up.


Oh. I thought you guys determined that trans dermal delivery was inefficient but for some reason i thought the jury was still out on buccal. I guess it makes sense that the same principles of surface area would apply. In a way this makes me feel less inadequate because I was never able to get anything positive out of attempting buccal.

#37 2tender

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Posted 13 March 2009 - 05:34 AM

Im glad you bumped this old thread, it does sound like a good idea, but I think the sublingual product has been replaced by the more practical 99% pure micronized Resveratrol combined with a liquid delivery vehicle called "Tween 80".

#38 Lufega

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Posted 16 March 2009 - 06:12 AM

How about a resveratrol nasal spray? Should get good absorption there as well. Someone already did this for curcumin. Google "curecumin".

#39 maxwatt

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Posted 16 March 2009 - 12:18 PM

How about a resveratrol nasal spray? Should get good absorption there as well. Someone already did this for curcumin. Google "curecumin".


It burns in any significant amount.

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#40 mikeinnaples

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Posted 19 March 2009 - 05:17 PM

How about a resveratrol nasal spray? Should get good absorption there as well. Someone already did this for curcumin. Google "curecumin".


It burns in any significant amount.




This is why I usually precede nasal resveratrol with a line of coke. Numbs it up real nice.

#41 maxwatt

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Posted 19 March 2009 - 07:44 PM

How about a resveratrol nasal spray? Should get good absorption there as well. Someone already did this for curcumin. Google "curecumin".


It burns in any significant amount.




This is why I usually precede nasal resveratrol with a line of coke. Numbs it up real nice.


Don't try this at home.

#42 bigsend

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Posted 19 March 2009 - 11:02 PM

Resveratrol chewing tobacco! Or just add nicotine to the gum, get everyone addicted to being healthy.

#43 2tender

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Posted 20 March 2009 - 12:41 PM

Seriously speaking, a transdermal may have equal delivery potential as buccal or sublingual. perhaps. even superior in some ways. when combined with the right solution.

Edited by 2tender, 20 March 2009 - 12:42 PM.


#44 eugenius

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Posted 20 March 2009 - 11:04 PM

Seriously speaking, a transdermal may have equal delivery potential as buccal or sublingual. perhaps. even superior in some ways. when combined with the right solution.

What would be the right solution?

#45 2tender

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Posted 21 March 2009 - 01:41 AM

Check your messages, I hope that helps you.

#46 niner

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Posted 21 March 2009 - 02:09 AM

Seriously speaking, a transdermal may have equal delivery potential as buccal or sublingual. perhaps. even superior in some ways. when combined with the right solution.

This has been looked at, and transdermal delivery of resveratrol is pretty terrible. At best it could be made less terrible with the right vehicle, but it's pretty much a no-go.

#47 2tender

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Posted 22 March 2009 - 11:42 AM

Thanks for your comment, but I used a Res. transdermal, that I felt did was it was supposed to do, the problem is the vehicle causes some irritation if used for a prolonged period. I am of the opinion now that the TD combined with a micronized 99% pure Res. (250) is pretty much outstanding in terms of absorbtion and effect. JMO

#48 maxwatt

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Posted 22 March 2009 - 12:21 PM

Thanks for your comment, but I used a Res. transdermal, that I felt did was it was supposed to do, the problem is the vehicle causes some irritation if used for a prolonged period. I am of the opinion now that the TD combined with a micronized 99% pure Res. (250) is pretty much outstanding in terms of absorbtion and effect. JMO


Measured absorption of transdermal delivery shows the maximum amount that can be delivered systemically is far too low to do much of anything. Do not discount the placebo effect. Local levels may be elevated in the epidermis and may have an effect there. Are you sure the skin irritation is due to the vehicle, or the resveratrol? Have you tried the vehicle with no resveratrol to be sure?

Resveratrol skin creams and lotions likely have a beneficial on skin health without irritation, and can be used where a patch is not effective; animal studies have shown increased skin thickness in older mice, and decreased skin cancer. There are a lot of resveratrol creams being market now, but it is uncertain which of them have a significant amount of resveratrol. Revlon seems to have an insignificant amount of a 50% P. cuspidatum extract in one product; More than a couple of milligrams in a 2 oz jar would make the product green instead of white. The amount of resveratrol used in the animal skin studies much higher than what the cosmetic companies have been using. I don't know what concentration Anthony has been using in his skin cream. Anthony?

#49 2tender

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Posted 22 March 2009 - 10:12 PM

Good thoughts , Maxwalt. I havent tried the vehicle by itself and it is the only Res. TD I have used. I have used the vehicle combined with other supplements and yes, there is some irritation. I cannot rule out placebo affect particularly when I have no means of scientific measurement.

Edited by 2tender, 22 March 2009 - 10:21 PM.


#50 Ben K

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Posted 26 March 2009 - 01:00 AM

Here are my questions about this method:

Would it irritate your mouth? (Continual irritation of mouth tissue, or gums, is unhealthy.)

Would it stain your teeth or affect the enamel over time? Could it cause tooth decay?

#51 maxwatt

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Posted 26 March 2009 - 01:35 AM

Here are my questions about this method:

Would it irritate your mouth? (Continual irritation of mouth tissue, or gums, is unhealthy.)

Would it stain your teeth or affect the enamel over time? Could it cause tooth decay?


What next? Resveratrol toothpaste?

From experience, direct contact with resveratrol helps heal canker sores. It does not stain teeth, and seems to reduce plaque. But I've not used it this way for more than a few days at a time. Resveratrol is anti-fungal, and may have anti-bacterial action as well.

#52 niner

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Posted 26 March 2009 - 04:07 AM

Would it irritate your mouth? (Continual irritation of mouth tissue, or gums, is unhealthy.)

Would it stain your teeth or affect the enamel over time? Could it cause tooth decay?

This might depend on purity. A 98+% product should not cause a problem. A 50% product might stain your teeth. Don't know about irritation.

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#53 Ringostarr

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Posted 26 March 2009 - 04:20 AM

Would it irritate your mouth? (Continual irritation of mouth tissue, or gums, is unhealthy.)

Would it stain your teeth or affect the enamel over time? Could it cause tooth decay?

This might depend on purity. A 98+% product should not cause a problem. A 50% product might stain your teeth. Don't know about irritation.


I have been "dipping" (like tobacco) micronized resveratrol between my cheek and gum for about 3 months. The cavities I had at my gum line have all but disappeard from sight. (I know, sounds a bit gross but it is true) (I did not have dental insurnace). Also my gums, which were receeding, look more healthy now.

#54 2tender

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Posted 26 March 2009 - 11:02 AM

I had been using Resveratrol TD and oral (capsules) for months and my dentist remarked that my gums were in great shape compared to my previous visit. How do you measure the amount you use for "dipping" and how much do you use, how many times daily etc.? Is that the only method you currently use?

#55 maxwatt

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Posted 26 March 2009 - 11:21 AM

I had been using Resveratrol TD and oral (capsules) for months and my dentist remarked that my gums were in great shape compared to my previous visit. How do you measure the amount you use for "dipping" and how much do you use, how many times daily etc.? Is that the only method you currently use?


Gingivitis is inflammation of the gums, with a bacterial cause. Resveratrol is ant-inflammatory, and seems to be antibacterial, Anthony, when are you coming out with resveratrol toothpaste?

#56 Anthony_Loera

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Posted 26 March 2009 - 12:40 PM

I had been using Resveratrol TD and oral (capsules) for months and my dentist remarked that my gums were in great shape compared to my previous visit. How do you measure the amount you use for "dipping" and how much do you use, how many times daily etc.? Is that the only method you currently use?


Gingivitis is inflammation of the gums, with a bacterial cause. Resveratrol is ant-inflammatory, and seems to be antibacterial, Anthony, when are you coming out with resveratrol toothpaste?



He he,

from toothpaste to athlete's foot spray... all good products for resveratrol.

A

#57 tunt01

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Posted 26 March 2009 - 01:11 PM

I had been using Resveratrol TD and oral (capsules) for months and my dentist remarked that my gums were in great shape compared to my previous visit. How do you measure the amount you use for "dipping" and how much do you use, how many times daily etc.? Is that the only method you currently use?


do you feel more healthy on a mental basis? i would imagine ingesting resveratrol TD near your brain would lead to higher circulating values and improved mental acuity there.



i use CoQ10 TD (in the mouth) just before i go work out and i tend to get a little bit of a rush before i go jog. it's quite pleasant.

#58 Ringostarr

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Posted 26 March 2009 - 02:39 PM

I had been using Resveratrol TD and oral (capsules) for months and my dentist remarked that my gums were in great shape compared to my previous visit. How do you measure the amount you use for "dipping" and how much do you use, how many times daily etc.? Is that the only method you currently use?


I use about 400 mg. between the cheek and gum usually once per day. I start out with a 15 minute "dip" for any buccal benefits. I then pour grape, apple, or orange juice into my mouth and swish for about a minute and then swallow. This is the only resveratrol I use all day.

Edited by Ringostarr, 26 March 2009 - 02:40 PM.


#59 treonsverdery

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Posted 26 March 2009 - 05:43 PM

I've read at pubmed.org that percutaneous absorption of drugs is as much as 40 times higher with the presence of FDA recognized detergents I have also read that the kind of molecule matters with Na alginate more effective than sodium lauryl sulfate



This reference is pro goo

Boll Chim Farm. 2002 May-Jun;141(3):210-7.Links
Buccoadhesive tablets for insulin delivery: in-vitro and in-vivo studies.Hosny EA, Elkheshen SA, Saleh SI.
Dept. of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

In the present work, insulin (6 U/kg) was formulated into bioadhesive buccal tablets using Carbopol 934, Hydroxypropyl cellulose (HPC) or Hydroxypopylmethyl cellulose (HPMC) and different absorption promoters. The effect of different ratios of HPC or HPMC to Carbopol on the rate of water uptake was studied. The axial and radial detachment force as well as the duration of adhesion of tablets to a porcine buccal tissues were also investigated. Furthermore the hypoglycemic effect of some formulations containing HPMC and Carbopol in different ratios with different additives and enhancers was studied using diabetic male beagle dogs. The rate of water uptake of tablets prepared with 3:1, 1:1 or 1:3 of HPC or HPMC: Carbopol was directly proportion to the Carbopol content of the tablet. The incorporation of enhancers (10%) to tablets prepared with HPMC: Carbopol of 1:1 ratio did not affect to a great extent the rate of tablets hydration. On the other hand, coating one side of the tablet with 50 mg of the impermeable cutina led to a significant reduction in the rate of tablets' water uptake reaching 50% to 75% in comparison with the uncoated tablets. Carbopol had the most influential effect on both mucoadhesion force and duration followed by HPMC. Tablets prepared with 100% HPC completely eroded within 6 hours during the measurement of the duration of adhesion. The incorporation of Carbopol with this polymer significantly improved its mucoadhesion duration reaching more than 24 hours with the 1:3 HPC: Carbopol. Ten percent of either sodium salicylate (NaSal) or sodium deoxycholate (NaDC) did not affect the duration of mucoadhesion of tablets prepared with 1:1 HPMC: Carbopol while 10% of Witepsol or Cacao butter and 1% of polyoxyethylene-9-lauryl ether (POELE) significantly reduced it. Tablets made using a polymer mixture of HPMC: Carbopol 934, 1:3 resulted in improved pharmacodynamic parameters producing a relative hypoglycemia (RH) of 6.72%. Furthermore, tablets made using polymer mixture of HPMC: Carbopol 934 in a ratio of 1:1 and containing 1% POELE resulted in 26% reduction in plasma glucose levels and producing 9.42% RH. Inclusion of other promoters such as 10% sodium deoxycholate or 10% sodium salicylate gave rise to RH values of 7.93 and 8.65% respectively.

This reference is pro sodium dodecyl sulfate like detergent

AAPS PharmSciTech. 2009 Mar 12. [Epub ahead of print] Links
Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study.Dhiman MK, Dhiman A, Sawant KK.
TIFAC Center of Relevance and Excellence in NDDS, Pharmacy Department, The M.S. University of Baroda, G.H. Patel Building, Donor's Plaza, Fatehgunj, Vadodara, 390002, Gujarat, India, dhiman.munish@gmail.com.

The purpose of this study was to determine the effect of permeation enhancers on the transbuccal delivery of 5-fluorouracil (FU). The effect of permeation enhancers on in vitro buccal permeability was assessed using sodium deoxycholate (SDC), sodium dodecyl sulphate (SDS), sodium tauroglycocholate (STGC), and oleic acid and their concentrations for absorption enhancement were optimized. STGC appeared to be most effective for enhancing the buccal permeation of FU than the other enhancers. These enhancements by STGC were statistically significant (p < 0.05) compared to control. The order of permeation enhancement was STGC > SDS > SDC > oleic acid. Histological investigations were performed on buccal mucosa and indicated no major morphological changes. The enhancing effect of STGC on the buccal absorption of FU was evaluated from the mucoadhesive gels in rabbits. The absolute bioavailability of FU from mucoadhesive gels containing STGC increased 1.6-fold as compared to the gels containing no permeation enhancer. The mean residence time and mean absorption time considerably increased following administration of gel containing penetration enhancer compared with the gel without penetration enhancer.


Biol Pharm Bull. 2008 May;31(5):955-62.Links
Delivery of resveratrol, a red wine polyphenol, from solutions and hydrogels via the skin.Hung CF, Lin YK, Huang ZR, Fang JY.
School of Medicine, Fu Jen Catholic University, Taipei County 242, Taiwan.

Resveratrol, the main active polyphenol in red wine, has been demonstrated to show benefits against skin disorders. The bioavailability of orally administered resveratrol is insufficient to permit high enough drug concentrations for systemic therapy. In this study, we examined the feasibility of the topical/transdermal delivery of resveratrol. The effects of vehicles on the in vitro permeation and skin deposition from saturated solutions such as aqueous buffers and soybean oil were investigated. The general trend for the delivery from solutions was: pH 6 buffer=pH 8 buffer>10% glycerol formal in pH 6 buffer>pH 9.9 buffer>pH 10.8 buffer>soybean oil. A linear relationship was established between the permeability coefficient (K(p)) and drug accumulation in the skin reservoir. Viable epidermis/dermis served as the predominant barrier for non-ionic resveratrol permeation. On the other hand, both the stratum corneum (SC) and viable skin acted as barriers to anionic resveratrol. Several prototype hydrogel systems were also studied as resveratrol vehicles. The viscosity but not the polarity of the hydrogels controlled resveratrol permeation/deposition. Piceatannol, a derivative of resveratrol with high pharmacological activity, showed 11.6-fold lower skin permeation compared to resveratrol. The safety profiles of resveratrol suggested that the hydrogel caused no SC disruption or skin erythema. It was concluded that delivery via a skin route may be a potent way to achieve the therapeutic effects of resveratrol. This is the first report to establish the permeation profiles for topically applied resveratrol.




thus whatever the legal oral surfactants plus gels are I strongly urge putting them with any oral absorption longevity product just look up buccal absorption at pubmed

Edited by treonsverdery, 26 March 2009 - 05:55 PM.


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#60 JLL

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Posted 27 March 2009 - 09:48 AM

So what about opening resv caps and sticking the stuff on your gums? Better or worse than just taking the caps orally?




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