Way to increase the bioavailability/absorption of Ursolic Acid?

[jathan_howe]

I was looking into Ursolic Acid (specifically PA's Pump Spray or UR Spray and found them to be too expensive at the moment). I know UrA, when administered orally has a very poor bioavailability. Capped form appeared to be cheaper than topical, and I was wondering if it's absorption could be increased. I've heard fish oils help but didn't hear an estimate as to how much to use. I was also wondering if soy lecithin granules could potentially emulsify it seeing as they are an emulsifier (not to mention a cheap source of phosphatidic acid)

 

[JeremyNG25]

Idk I use the spray and the capsules. I take the caps with meals and I take 18 a day. I've ran out of the caps for a few days and get more tomorrow in the mail and I don't notice much. However when I've run out of the spray there is a massive difference. I've heard some guys keep it as a staple for its positive effects on blood pressure etc. wish I knew how to make the caps more effective but I think Patrick Arnold said take it with at least 6 grams of fats

 

[jathan_howe]

Thanks for the info, repped!

 

[muscleupcrohn]

Some interesting reads:

A highly water-soluble macromolecular compound of ursolic acid with monomethoxypoly(ethylene
glycol) (mPEG) was prepared. The physicochemical
properties and stabilities under different conditions were investigated. By PEG
conjugation, greatly increased water solubility was obtained, and the results
showed that this conjugate was a potential prodrug for the oral delivery of
ursolic acid.

http://www.scipharm.at/download.asp?id=1516

The results obtained in this study demonstrated improvements in the solubility and dissolution of the lipophilic drug ursolic acid in solid dispersions compared with physical mixtures, which was maintained after 6 months of room temperature storage. This result could be attributed to improved wettability, micellar solubilization caused by the lipid surfactant Gelucire, conversion of ursolic acid from a crystalline to an amorphous structure, or hydrogen bond formation between the carriers and drug. Taken together, these results may explain the improved in vitro trypanocidal activity of ursolic acid in solid dispersion compared to the physical mixture, which were also demonstrated to be safe against mammalian fibroblast cells. Therefore, the results presented in this work are promising for development of a dosage form containing ursolic acid to treat Chagas disease.

Solid Dispersion of Ursolic Acid in Gelucire 50/13: a Strategy to Enhance Drug Release and Trypanocidal Activity

The antitumor efficacy of ursolic acid (UA) was limited by poor hydrophilicity and low bioavailability. To overcome this issue, UA was encapsulated in liposomes modified with folate conjugates for better solubility and bioavailability.

In vitro and in vivo antitumor effects of folate-targeted ursolic acid stealth liposome. - PubMed - NCBI

Liposomes have been utilized as a drug delivery system to overcome the poor solubility of UA, increase the therapeutic efficiency, reduce the side effects, and enhance the bioavailability of drugs that have been broadly applied [13–15]. Currently, ursolic acid liposomes (UALs) have been studied successfully and have been approved by the State Food and Drug Administration (SFDA) of China to enter clinical trials (number 2009L00634).

A Phase I Trial to Evaluate the Multiple-Dose Safety and Antitumor Activity of Ursolic Acid Liposomes in Subjects with Advanced Solid Tumors

Results from this study indicate that SpHL-UA can be an interesting delivery system for the pharmaceutical formulation of UA

Preparation, Physicochemical Characterization, and Cell Viability Evaluation of Long-Circulating and pH-Sensitive Liposomes Containing Ursolic Acid

Unfortunately, the above links don't seem to be quite so simple as taking another common supplement or two with your ursolic acid like you can with something like (-)-Epicatechin.

 

[Olympus Labs]

We are working on this now!

 

[jathan_howe]

Can't wait! Would it be (hopefully) cheaper than the TD spray versions? I don't even mind the spray idea, just the cost.

 

[uubiduu]

the td versions are insanely expensive especially in europe

 

[The_Old_Guy]

So what about SmartPowders Ursolic Acid with either their 'Topical Matrix' or with PhloJel? I may try this. $80 is too rich for my blood for PA's Ur-Spray.

 

[crowbar46]

So what about SmartPowders Ursolic Acid with either their 'Topical Matrix' or with PhloJel? I may try this. $80 is too rich for my blood for PA's Ur-Spray.

Maybe I'm misunderstanding something, but you can get Ur spray online for $39.99/bottle.

Crowbar

 

[T-Bone]

We are working on this now!

Excellent!. I hope you don't have to bathe in your version. UA was good stuff, but way to expensive for mild results at best. Plus no one ever really established proper dosing. With the caps just had to take as much as possible. With the dermal version you had to bathe in it from head to toe.

 

[BCseacow83]

So what about SmartPowders Ursolic Acid with either their 'Topical Matrix' or with PhloJel? I may try this. $80 is too rich for my blood for PA's Ur-Spray.

The form of UA in the sprays is not the same as the one in pills. Pills/powder are either rosemary/loquat extracted for UA. The spray is Arginine Ursolic Acetate. Adding the powder to the phlogel would not be the same. I wish it was.

 

[Woody]

Excellent!. I hope you don't have to bathe in your version. UA was good stuff, but way to expensive for mild results at best. Plus no one ever really established proper dosing. With the caps just had to take as much as possible. With the dermal version you had to bathe in it from head to toe.

Nothing beats a Sunday morning acid bath.

 

[The_Old_Guy]

Maybe I'm misunderstanding something, but you can get Ur spray online for $39.99/bottle.

Crowbar

I've only seen it at PN, where you need to buy 2 in order to get it for $40... that equals $80 Is your price from somewhere else?

 

[Bigdumogre]

We are working on this now!

OL is going to win company of the year 2016

 

[The_Old_Guy]

The form of UA in the sprays is not the same as the one in pills. Pills/powder are either rosemary/loquat extracted for UA. The spray is Arginine Ursolic Acetate. Adding the powder to the phlogel would not be the same. I wish it was.

Yeah, I just did more research - stuff is really damn heavy - almost at the Dalton limit. CURSES! Foiled again! Looks like Ur-Spray if I want to try it. What is E-Pharm spray - same thing? Smart Powders has 8oz for ~$37

 

[The_Old_Guy]

Maybe I'm misunderstanding something, but you can get Ur spray online for $39.99/bottle.

Crowbar

Replying again - I did find E-Pharm for $36.44 at Smart Powders - thanks for prompting me to search more.

 

[jathan_howe]

Replying again - I did find E-Pharm for $36.44 at Smart Powders - thanks for prompting me to search more.

If you're talking about Pump Spray, it's a mix of triacetyl adenosine and less arginine ursolic acetate.

 

[Pec.Major]

Would taking UR with bioperine increase the absorption? Would be 1200mg UR daily.

 

[BlockBuilder]

We are working on this now!

Make it like PA did with the UR tabs. Honestly I literally bathe myself in this morning and night. I bought 100 bottles and poured it all into a blow up tub and I just sit in it twice a day......ok I didn't do THAT but I do cover myself in it like its nobody's business. Hoping you guys make a decent oral product. I'm about to try my first OL product ever. Elim1nate

 

[squirtguns89]

Would taking UR with bioperine increase the absorption? Would be 1200mg UR daily.

OL has been working on an effective absorption method for almost a year and not came up with anything worthwhile. iirc, a brilliant chemist PA didnt even add bioprine to his UA caps...

to the point answer, probably going to have a limited impact at best.

 

[JakeAntaeus]

We've recently finished complexing bulk quantities of Ursolic Acid with HPBCD. (XRD below.)
The results are good -- better solubility, better bioavailability, etc. It's an integral part of our new product HH6, and something we are considering making available as a standalone product.

 

[furion]

We've recently finished complexing bulk quantities of Ursolic Acid with HPBCD. (XRD below.)
The results are good -- better solubility, better bioavailability, etc. It's an integral part of our new product HH6, and something we are considering making available as a standalone product.

View attachment 137123

By the looks of that XRD- it appears you have used a wet complexing method. It's really good to see that a company is manufacturing this using a reliable complexing method and actually quantifying it as well.

For anyone who values my opinion- this would be a very worthwhile product for this ingredient alone.

I've compounded UA-HPCD cyclodextrin complexes for myself before- interested to know what was used as a solvent? ...if you don't mind disclosing?

 

[squirtguns89]

Furion approved antaeus product, ill have my next recomp lined up after the fall it sounds. i do typically prefer standalone ingredients.

 

[JakeAntaeus]

By the looks of that XRD- it appears you have used a wet complexing method. It's really good to see that a company is manufacturing this using a reliable complexing method and actually quantifying it as well.

For anyone who values my opinion- this would be a very worthwhile product for this ingredient alone.

I've compounded UA-HPCD cyclodextrin complexes for myself before- interested to know what was used as a solvent? ...if you don't mind disclosing?

Thanks very much for the kind words.

PM me and I'd be glad to share the details. The solvent's actually not the important thing for bulk production, though. Really lipophilic molecules like UA require some coaxing to get into cyclodextrin complexes...!