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Bioavailability of fisetin in mouse and human studies question

fisetin bioavailability mouse studies human studies

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#1 osris

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Posted 04 November 2019 - 09:23 AM


Many people believe that fisetin has low bioavailability, and so I was wondering if in the mouse and human studies of fisetin, was fisetin taken with another substance to enhance its bioavailability?
 
If not, then how come the mouse study showed good results for fisetin in mice? 
 
In other words, if bioavailability is a problem, and the mice were not given another substance to compensate for it, how come fisetin worked well on the mice?
 
I asked this question in another thread but no one could answer it?
 
 

Edited by osris, 04 November 2019 - 09:24 AM.

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#2 Rays

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Posted 06 November 2019 - 09:08 AM

There were two mice studies in the study of the "Fisetin: Senolytic!" thread:
  • "For diet studies, mice were fed Teklad 2020 chow (Envigo, Madison, WI) prepared with or without 500 ppm (500 mg/kg) of fisetin"
  • "For oral administration of fisetin, mice were dosed with 100 mg/kg of fisetin in 60% Phosal 50 PG:30% PEG400:10% ethanol or vehicle only by gavage."
 
The ingredients of the Teklad chow (wheat, corn and soy oil) you can find here:
Maybe the mixing of the fisetin with the soy oil in the chow is beneficial for bio availability.
 
The mice in the oral gavage group were administered fisetin in: 
  • 60% Phosal 50 PG
  • 30% PEG400
  • 10% ethanol
 
Phosal 50 PG is used as a "bioavailability-enhancer in oral drug delivery". See link below.
It contains at least 50% Phosphatidylcholine.
Phosphatidylcholine (PC) is "a phospholipid attached to a choline particle. Phospholipids contain fatty acids, glycerol, and phosphorous. The phosphorous part of the phospholipid substance — the lecithin — is made up of PC".
 
PEG400 "is very hydrophilic, which renders it a useful ingredient in drug formulations to augment the solubility and bioavailability of weakly water-soluble drugs". See link below.
 
Together with the ethanol it reminds me of making a liposomal. It may be possible to do that yourself using the process described here:
 
 
References:
 

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#3 osris

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Posted 06 November 2019 - 12:56 PM

Thanks. That gives me something to work on. 

 

Is it possible to buy Teklad chow? Maybe humans could take it with fisetin. I know that sounds silly, but could it work?


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#4 Rays

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Posted 06 November 2019 - 02:54 PM

Maybe the special chow works in humans as well. It was prepared with 500 ppm (500 mg/kg) of fisetin by Envigo. Co. (Tampa, FL). You could contact them. They have a special team for the Teklad diet.

https://www.envigo.com/contact-envigo/

 

But I will go for the self made liposomal fisetin using the process mentioned. I'm ordering an ultrasound machine for that.

 

 

 



#5 QuestforLife

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Posted 06 November 2019 - 03:29 PM

Maybe the special chow works in humans as well. It was prepared with 500 ppm (500 mg/kg) of fisetin by Envigo. Co. (Tampa, FL). You could contact them. They have a special team for the Teklad diet.

https://www.envigo.com/contact-envigo/

 

But I will go for the self made liposomal fisetin using the process mentioned. I'm ordering an ultrasound machine for that.

 

I'm pretty good at making Vitamin C liposomes using this method, and I can tell you it is MUCH trickier to do this with substances that don't dissolve well in water. You'll need to up the alcohol content considerably.

 

One test to see how (un-)successful you are is to leave your liposomal mix in the fridge overnight and see how much fisetin settles out at the bottom. You're aiming for none.

 

Let us know how you get on. 


Edited by QuestforLife, 06 November 2019 - 03:30 PM.


#6 osris

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Posted 06 November 2019 - 05:58 PM

Making fisetin bioavailable in these ways seems a bit of a hassle to me. Is there a quicker way?



#7 Florin

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Posted 06 November 2019 - 08:08 PM

To determine how to take fisetin, the researchers running the human clinical trials could be asked, or one can wait for the results (and methods) of those trials to be published.

 

https://clinicaltria...ts?term=fisetin



#8 QuestforLife

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Posted 07 November 2019 - 09:53 AM

Making fisetin bioavailable in these ways seems a bit of a hassle to me. Is there a quicker way?

 

Same as with other poorly bioavailable flavonoids like resveratrol - dissolve in oil (or alcohol) and most of all - take large quantities. Of course this increases the chances of unintended side effects. 



#9 osris

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Posted 07 November 2019 - 03:13 PM

Thanks, but is the dissolving essential? Can't you just take it along with a spoonful of olive oil or a fish oil capsule? It all ends up in the stomach at the same time anyway, and is digested together. 



#10 Rays

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Posted 08 November 2019 - 10:22 AM

I'm pretty good at making Vitamin C liposomes using this method, and I can tell you it is MUCH trickier to do this with substances that don't dissolve well in water. You'll need to up the alcohol content considerably.

 

One test to see how (un-)successful you are is to leave your liposomal mix in the fridge overnight and see how much fisetin settles out at the bottom. You're aiming for none.

 

Let us know how you get on. 

 

Thanks for the advice.

I will report back about my liposomal creation success.



#11 sphere

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Posted 06 December 2019 - 08:17 PM

anyone aware of a source for 

  • Phosal 50 PG
  • other than the lab houses that do not take "regular" folks orders? used in cosmetics but did not see any sellers
  • worthwhile using to increase bioavailabilty I think.  Thanks!


#12 mstrathern

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Posted 01 January 2020 - 05:18 PM

In a Journal of Pharmacological Sciences, Jan 2018

https://www.scienced...347861317302116

Wen-bin He,Kazuho Abe & Tatsuhiro Akaishi report on the bio-availability of orally administered Fisetin.in mice using 10% Tween 80 (polysorbate 80) in saline to deliver fisetin. They showed strong evidence of fisetin entering the blood stream and passing the blood brain barrier in mice. This would seem an easier method of delivery than Teklad and the Phosal mix as polysorbate 80 is widely available, cheap and is an FDA approved food and cosmetics additive.

I have also thought about DMSO patches given fisetin's solubility in it. DMSO's FDA approval for skin conditions and it's ability to carry drugs through the skin. Perhaps a useful way for local application in problems like knee arthritis.


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#13 poonja

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Posted 02 January 2020 - 10:29 AM

From a practical standpoint, how would one utilize polysorbate 80 to improve bioavailability.  Could you just take some polysorbate 80 with  your fisitin capsules. It says in a saline solution.  Does this mean putting the contents of your capsules in a mixture od polysorbate 80 and saline solution for oral consumption.  Sorry, it this seems like a simple matter but for me, nothing is simple.


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#14 mstrathern

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Posted 10 January 2020 - 12:57 AM

I think that the fisetin is dissolved the polysorbate 80 and then that diluted 1 part polysorbate/fisetin solution to 9 parts saline. At least that's my reading of  the original paper. What concentration of fisetin  in polysorbate I couldn't see. My presumption would be about 25% fisetin.


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