Ursolic Acid Spray

[D3Baseball]

Ursolic Acid had some unbelievably promising research, but results of ursolic acid products so far has been mixed. Could this be due to poor absorption?

PA seems to think so and is releasing a topical of the sodium salt:

Ur Spray contains a soluble derivative of the amazing natural repartitioning compound ursolic acid. By transforming the poorly absorbed parent ursolic acid into its acetic acid ester, and then into the sodium salt of that ester, a form is acquired that can be effectively delivered via topical formulation.
This allows a much higher percentage of ursolic acid to enter the body than with oral formulations of straight ursolic acid. It also allows for a sustained release effect, so that blood levels of ursolic acid can be maintained throughout the day

Would like to see what everyone thinks of this. If PA has a product that can put that great looking research into practice, we might have a groundbreaking supplement on our hands.

[Younglifter16]

I was just about to make this thread lol. The mixed reviews do indeed seem to be dose dependant. Those who have taken in the upper spot of 12+ caps have noticed results, while others taking too little notice nothing.

This spray looks like it might do the trick. I'm still a bit iffy though due to the sperm damaging issue (unless someone has cleared this up that I'm unaware of?)

[PinchTheBear]

It's heavy... but otherwise its properties are near-ideal for transdermal application. I'd still rather dissolve it in neutral oil. Still don't see why he didn't do liquicaps.

[Right_Hook]

Solubility is **** with this stuff. Anything to improve it doesnt hurt.

Nice blog Andy. Never seen it.

[PinchTheBear]

Solubility is **** with this stuff. Anything to improve it doesnt hurt.

Nice blog Andy. Never seen it.

Thanks

[NO HYPE]

It's heavy.

Yeah I'd say Mr. Dalton is rather close to the stratum corneum threshold.

but otherwise its properties are near-ideal for transdermal application.

Since UA's solubility is retarded, would its acetic acid ester mitigate the effects of transdermal first-pass metabolism, diffusional barriers, ect.?

I'd still rather dissolve it in neutral oil. Still don't see why he didn't do liquicaps.

When considering the lipophilicity of pentacyclic triterpenes, I'd have to agree.

[Nailbomb9]

Yeah I'd say Mr. Dalton is rather close to the stratum corneum threshold.





Since UA's solubility is retarded, would its acetic acid ester mitigate the effects of transdermal first-pass metabolism, diffusional barriers, ect.?





When considering the lipophilicity of pentacyclic triterpenes, I'd have to agree.

Checking another NoHype thread out before it gets deleted. Oh, and check you PM's please...

[PinchTheBear]

Since UA's solubility is retarded, would its acetic acid ester mitigate the effects of transdermal first-pass metabolism, diffusional barriers, ect.?

Calling it an acetic acid ester derivative is misleading to me because I would assume he's esterifying the alcohol. In transdermal application, that would alter its pharmacology because the conditions to remove it require concentrated aqueous acid/base or anhydrous base.

Technically it's a sodium carboxylate surface group, and any partition complications largely transcend its poor oral bioavailability; viz., it's worth it. I think it's a clever fix.

[NO HYPE]

~



Ethosome-encapsulated transdermal ursolic acid?

Zhongguo Zhong Yao Za Zhi. 2011 Apr;36(8):988-91.
[Preparation and transdermal diffusion of ursolic acid ethosomes].
Chen Y, Wiu Q, Zhang Z, Zhou L, Liu X, Du M, Jia X.

To prepare ursolic acid ethosomes and investigate the penetration characteristics of ursolic ethosomes as a transdermal vehicle.

METHOD:

Ursolic acid ethosomes were prepared by injection method, and the shape and particle size of the ethosomes were analyzed. Ursolic acid permeation tests in vitro through the skin of rats were performed in TP-3 diffusion cell. The accumulated permeation amounts of ursolic acid 10% isopropanol solution, ursolic acid liposomes, ursolic acid ethosomes were compared.

RESULT:

The average encapsulation percentage, particle size, and Zeta potential of the ethosomes were (95.83 +/- 0.86)%, (87.5 +/- 7.5) nm and - (38.4 +/- 3.6) mV, respectively. The accumulated permeation amount of the ethosomes in 12 h was 146.49 microg x cm(-2), and its transdermal permeability in 12 h was 12.17 microg x cm(-2) x h(-1).

CONCLUSION:

The encapsulation percentage of the ethosomes is good, and the stability of the ursolic acid ethosomes is fine. Ethosomes can significantly enhance the diffusion rate of ursolic acid through the skin of rats.

[Right_Hook]

PA is making this stuff by hand in his lab. He mentioned doing a liquid capsule run would be too costly for him.

the runs you need to do for liquid caps are extraordinarily high. hell the runs for regular caps are like minimum 100K caps

OTOH we can make as few bottles of spray at a time as we wish. I only processed a kilo of this sodium ursolic acetate

[PinchTheBear]

~



Ethosome-encapsulated transdermal ursolic acid?

I'm not exactly sure of how expensive that would be, but it's definitely somewhere in range of "as fuck".

PA is making this stuff by hand in his lab. He mentioned doing a liquid capsule run would be too costly for him.

Figured it was a cost thing

[SwolenONE]

^^^ lmao at that price category

[NO HYPE]

I'm not exactly sure of how expensive that would be, but it's definitely somewhere in range of "as fuck".

I heard a Transdermal "Dextrocyclodized" Ethosomal Ursolic Acid Patch was in the works as we speak.

[lordgt1]

What kind of dosages were people running who were getting noticeable results. Compared to those who did not get positive results?

[kochbros2012]

Since UA's solubility is retarded, would its acetic acid ester mitigate the effects of transdermal first-pass metabolism, diffusional barriers, ect.?

i never heard of the term "first pass" metabolism used in regards to transdermal delivery. i mean, there is no second pass when it comes to skin. its a one way street.

anyway, what kinds of metabolism do you imagine happens to ursolic acid or other pentacyclic terpenes when it passes through the skin? I cant think of anything obvious

not sure if its just the acetylation of the ursolic acid that improves its properties. being made into the salt form may help too. theoretically that could give it some cool dual water and lipid solubility which would facilitate its transport

[kochbros2012]

Calling it an acetic acid ester derivative is misleading to me because I would assume he's esterifying the alcohol. In transdermal application, that would alter its pharmacology because the conditions to remove it require concentrated aqueous acid/base or anhydrous base..

i dont see what is misleading about calling it an acetic acid ester. acetic acid plus the alcohol leads to ester

esters are very quickly cleaved in the body by esterases. your body doesnt need a lab with nasty chemicals to make chemical alterations, its got enzymes

[kochbros2012]

I heard a Transdermal "Dextrocyclodized" Ethosomal Ursolic Acid Patch was in the works as we speak.

sound like a band aid solution to me

get it? patch, band aid

[NO HYPE]

i never heard of the term "first pass" metabolism used in regards to transdermal delivery.

Transdermal bioavailability and first-pass skin metabolism: a preliminary evaluation with nitroglycerin.

The fraction of drug lost during absorption is not exclusive to oral administration & first-pass hepatic metabolism. In reguards to transdermal delivery and the stratum corneum, there are limitations [e.g. molecular structure/weight of the compound, diffusional barriers, enzymatic degradation, ect].

[kochbros2012]

The fraction of drug lost during absorption is not exclusive to oral administration & first-pass hepatic metabolism. In reguards to transdermal delivery and the stratum corneum, there are limitations [e.g. molecular structure/weight of the compound, diffusional barriers, enzymatic degradation, ect].

i understand the concept, it just seems that the term "first pass" in regards to the skin is silly. cuz there is only one pass. unless you count an infinitessimally small amount which somehow might get sweated out or something

for liver of course there are many many passes

[NO HYPE]

i understand the concept, it just seems that the term "first pass" in regards to the skin is silly. cuz there is only one pass. unless you count an infinitessimally small amount which somehow might get sweated out or something

Perhaps initial-pass would be more ideal?

I probably used the term out of context however, I believe it was implemented for certain compounds [primarily xenobiotics] and their metabolites that may undergo biotransformation following dermal application, thus altering their pharmacologic profile, toxicity status, ect.

[kochbros2012]

Perhaps initial-pass would be more ideal?

i would opt for simply "pass"

whatever they wanna call it is fine though