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Topical Absorption Of Caffeine, Aspirin And Niacinamide

haidut

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Another study, which looked at absorption of these Peat-approved substances through human skin.

http://www.nature.com/jid/journal/v54/n ... 18185a.pdf

Niacinamide absorption in acetone (the solvent used in the study) was only about 10%, however as per another human study I posted some time ago on topical B vitamins, changing the solvent to ethanol increases absorption to 80%. Aspirin absorption was about 21%. Caffeine absorption was highest at almost 50% of the applied dose and the authors noted that:

"...Other [compounds] such as dinitrochlorobenzene (DNCB), caffeine and benzoic acid penetrate so extensively as to suggest that the human skin has little barrier properties to them."

Another important finding was the much much longer half-life with topical absorption. All tested compounds, including caffeine, niacinamide and aspirin have much lower rate of absorption when applied topically. This results in continuous absorption and presence of the substances in human blood several days after administration. It took caffeine about 60 hours for its absorption rate to drop to zero and it took aspirin and niacinamide at least 5 days for their absorption rates to drop to zero. I have attached some diagrams from the study showing the absorption rate over several days.
Thus, it seems that topical administration of these 3 substances may be a good approach for people who would like to prolong the presence of those substances in the blood for increased therapeutic affect. Aspirin and niacinamide are well-known in the medical field for having a very short half life and as such attempts have been made to invent delayed release versions to prolong the effect. However, Peat has spoken against such delayed release versions and it looks like he is right at least on one count. The delayed release version of niacin increased the incidence of strokes.
http://thechart.blogs.cnn.com/2011/05/2 ... -to-risks/

"...A government trial using niacin to raise good cholesterol levels ended early when patients failed to get the expected protection against heart attack and stroke. A small number of patients actually had in increase in stroke."

So, it looks like you can get "extended release" versions of caffeine, niacinamide and aspirin using topical application. Dissolve the substances in water or in low-ish concentration ethanol (as in SolBan).
 

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haidut

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cantstoppeating said:
I'm curious, why the need for ethanol as a solvent if water is adequate?

Good question. Several reasons as far as I am concerned. First of all, with water solution the product will eventually develop mold and the water will be colonized by bacteria. I don't exactly how long that will take but most studies say after one month there is already a level of contamination that may pose danger. Second, with ethanol the rate of absorption is much higher. In the studies I have seen, using ethanol as the solution most of the compound is absorbed within the first 3 hours, while with water absorption rate was low and it took several days to get the full amount absorbed. So, with some substances like caffeine you may never get to the blood levels show in the studies to be protective against things like skin cancer or acting as sunscreen. Third, some substances are much soluble in ethanol than water and this applies to at least one of the 3 mentioned above. So, with ethanol you can deliver higher dose per serving which in most cases is preferable.
There may be other reasons but these are top 3 that come to mind.
 

tara

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haidut said:
cantstoppeating said:
I'm curious, why the need for ethanol as a solvent if water is adequate?
...
First of all, with water solution the product will eventually develop mold and the water will be colonized by bacteria....

I can confirm that a water solution of aspirin and niacinamide goes off after a week or two.
I only remember to use it when I've accidentally let myself get sunburned, and then as soon as the burn has gone I forget about it. So I've had a few little jars go foul on me.
I'll get some caffeine powder at some stage to add to the mix. Slow release caffeine sounds good to me.
 

Blossom

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tara said:
haidut said:
cantstoppeating said:
I'm curious, why the need for ethanol as a solvent if water is adequate?
...
First of all, with water solution the product will eventually develop mold and the water will be colonized by bacteria....

I can confirm that a water solution of aspirin and niacinamide goes off after a week or two.
I only remember to use it when I've accidentally let myself get sunburned, and then as soon as the burn has gone I forget about it. So I've had a few little jars go foul on me.
I'll get some caffeine powder at some stage to add to the mix. Slow release caffeine sounds good to me.
Just curious, did you use distilled water?
 

tara

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Blossom said:
tara said:
I can confirm that a water solution of aspirin and niacinamide goes off after a week or two.
I only remember to use it when I've accidentally let myself get sunburned, and then as soon as the burn has gone I forget about it. So I've had a few little jars go foul on me.
I'll get some caffeine powder at some stage to add to the mix. Slow release caffeine sounds good to me.
Just curious, did you use distilled water?
I used tap water. I have a distiller, and was using that regularly for my drinking water etc for quite awhile, but I've gone back to using tap water the last while and didn't have the distilled water on hand. Maybe that would make a difference. We have a very good water supply most of the time - no chlorine, no fluoride, clean, but has a bit of calcium and maybe other minerals in it. My current plan is to make up no more than I can use in a few days-1 week.
 

Blossom

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Distilled water seems worth it for shelf life if you are going to make your own topical products and use water as the base. I've had things I've made last up to a year using distilled water. It seems to be as close to sterile as you can get for home use.
 

jaa

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I usually bathe in niacinamide and aspirin anyway, so I added coffee to the bath last night. I'm not sure if the dose is high enough, but I can say it did not stain my skin or leave me stinking like coffee.
 

Blossom

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jaa said:
I usually bathe in niacinamide and aspirin anyway, so I added coffee to the bath last night. I'm not sure if the dose is high enough, but I can say it did not stain my skin or leave me stinking like coffee.
Did you brew the coffee first or just put coffee grounds in the bath water? I'm just interested because I might try that out and was wondering how you do it. :P
 

tara

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Blossom said:
Distilled water seems worth it for shelf life if you are going to make your own topical products and use water as the base. I've had things I've made last up to a year using distilled water. It seems to be as close to sterile as you can get for home use.
Thanks blossom, that's an idea.
I'm currently using tap water to make up an week's worth of B vitamins, which I store in the fridge and measure out with breakfast and dinner. I've not noticed any problem with that. Also lets me change my recipe reasonably frequently.
If I want to be more systematic with a water-based skin potion, I guess I could crank up the distiller again and/or see if I can get some suitable ethanol. From what Haidut has written, a bit of ethanol might make it more effective.
 

Blossom

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tara said:
Blossom said:
Distilled water seems worth it for shelf life if you are going to make your own topical products and use water as the base. I've had things I've made last up to a year using distilled water. It seems to be as close to sterile as you can get for home use.
Thanks blossom, that's an idea.
I'm currently using tap water to make up an week's worth of B vitamins, which I store in the fridge and measure out with breakfast and dinner. I've not noticed any problem with that. Also lets me change my recipe reasonably frequently.
If I want to be more systematic with a water-based skin potion, I guess I could crank up the distiller again and/or see if I can get some suitable ethanol. From what Haidut has written, a bit of ethanol might make it more effective.
I wonder if vodka would work?
 

tara

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Blossom said:
I wonder if vodka would work?
Yes, that crossed my mind too - easy to get.
 

haidut

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tara said:
Blossom said:
I wonder if vodka would work?
Yes, that crossed my mind too - easy to get.

Sure, vodka would work as well. It is 40% grain alcohol, usually fairly well-distilled and combined with distilled water.
 

Blossom

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haidut said:
tara said:
Blossom said:
I wonder if vodka would work?
Yes, that crossed my mind too - easy to get.

Sure, vodka would work as well. It is 40% grain alcohol, usually fairly well-distilled and combined with distilled water.
Thanks!
 

jyb

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Caffeine, B vitamin, magnesium...it seems that dumping some instant coffee in a warm bath for topical absorption would be a good idea. It's very diluted compared to a cup of coffee, but the surface skin area is large so maybe...
 
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jyb said:
Caffeine, B vitamin, magnesium...it seems that dumping some instant coffee in a warm bath for topical absorption would be a good idea. It's very diluted compared to a cup of coffee, but the surface skin area is large so maybe...


Seems like a waste of caffeine because so little will be absorbed unless you're willing to add a few buckets of ethanol to your bath.
 

nograde

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I've been using topical Aspirin for over a year now so I thought I might chime in to report my experiences:

- I use water as vehicle only, no need to stress your skin with ethanol
- I dissolve 4 tablets a 500mg in very little water (maybe 4-5 spoons)
- I let the filler settle and use only the clear solution
- I rub it all over my body to maximize absorption (morning ritual after shower)
- I can feel the effects after 15 minutes (mostly by nose clearing up completely,this is in stark contrast to the study, I don't know why)
- Effect wears off after 3 hours (again, very different experience to the study results)
- I get the same effect by using one tablet orally, so I guess transdermal absorption is 25%
- I use transdermal Aspirin because I develop stomach ulcers very quickly when using Aspirin orally
- Topical Aspirin does NOT save you from ulcers: In the beginning I did the above three times a day and developed ulcers within a week or so.
- Topical Aspirin helps somewhat with acne (in my case on my back), but it's by no means a panacea

Regarding topical Niacinamide: Be careful when applying to your face for prolonged time, it's a very efficient skin lightener. Some might like the dull, pinkish look, as a guy I don't. Thankfully the effect is not permanent and skin returns to normal after a few days.
 

uuy8778yyi

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I am confused by the graph and study

it can stay active i nthe blood for 3 to 5 days if applied topically ?
 
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