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Oral Bioavailability of Curcumin Forms and Differences between Sexes

curcumin oral bioavailability bcm-95 longvida theracurmin meriva micellar delivery

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#1 LexLux

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Posted 03 April 2014 - 10:53 PM


Im not sure if this recent study from 2014 has been discussed here yet. The bioavailability data on brands is interesting, until now I was most interested in getting some BCM-95 but it looks like Theracurmin (27 fold increase) is looking good. Anyone know more about the "micellar delivery system" (See Full text!)?

Schiborr, C., Kocher, A., Behnam, D., Jandasek, J., Toelstede, S. and Frank, J. (2014), The oral bioavailability of curcumin from micronized powder and liquid micelles is significantly increased in healthy humans and differs between sexes. Mol. Nutr. Food Res., 58: 516–527. doi: 10.1002/mnfr.201300724
http://onlinelibrary....201300724/full

"The use of adjuvants, such as piperine [28] or turmeric essential oils [37], enhanced curcumin bioavailability (based on AUC) 20- or 7-fold, respectively (Table 5). Incorporation of curcumin into lecithin (mainly phosphatidylcholine) liposomes resulted in a ca. fourfold better absorption (based on AUC) than native curcumin in nine healthy volunteers [38]. The bioavailability of a micronized form of crystalline curcumin (“Theracurmin™,” prepared from curcumin, ghatti gum, and water), compared to native curcumin, was 27-fold increased (Table 5) [39]. Thus, our micellar delivery system, which enhanced curcumin bioavailability 185-fold (all subjects), appears to be superior to all hitherto tested formulations, while our micronisate (ninefold increase in AUC) is similarly effective as previously reported strategies (Table 5). Furthermore, the Cmax achieved with a single oral dose of 410 mg curcumin from our micellar formulation (women, 3.7 μmol/L; men 2.6 μmol/L) are higher than those observed after the intake of 8 g of native curcumin [31].

The present study revealed sex differences with respect to the plasma AUC of curcumin. Women absorbed curcumin to a larger extent (higher Cmax and AUC) than men (Table 2). This could be due to the reportedly higher expression and activity of the hepatic drug efflux transporter P-glycoprotein (MDR1) and some isoforms of the glucuronosyltransferases and sulfotransferases, enzymes involved in curcumin biotransformation, in men [47]. However, the differences in bodyweight (Table 1), blood volume, and body fat, which ultimately lead to smaller volumes of distribution in women, may also account for the observed differences [47].

Less than 0.2% of the oral dose of curcumin was excreted with urine within 24 h. Thus, >98.8% of the ingested curcumin was either excreted via the bile and feces or may have been distributed to body tissues where it may potentially exert biological activities.

Free curcumin concentrations as low as 100 nmol/L reversed disease state and reduced IL-1β in Alzheimer's disease models [48, 49], therefore our newly developed curcumin formulations may be suitable vehicles for the delivery of pharmacologically relevant doses of the phytochemical in human intervention trials."
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#2 LexLux

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Posted 03 April 2014 - 11:56 PM

The "micellar delivery system" showed outstanding results! (185-fold increase):

"Curcumin formulations
The curcumin micronisate was produced by RAPS GmbH & Co. KG (Kulmbach, Germany) using their “concentrated powder form” technology [43] by mixing 25% curcumin powder with 58.3% triacetin and 16.7% panodan (E472e) and spraying the solution onto the porous excipient silicon dioxide. The resulting curcumin micronisate contained 17.2% curcumin powder, which is equivalent to 14.1% curcumin. Curcumin micelles were composed of 7% curcumin powder (equivalent to 6% curcumin) and 93% Tween-80 (Kolb, Hedingen, Switzerland) and manufactured by AQUANOVA AG (Darmstadt, Germany). All percentages refer to weight."

In addition see the funding:

"Funded by

German Federal Ministry of Education and Research (BMBF). Grant Number: 01EA1334A"

Edited by LexLux, 04 April 2014 - 12:07 AM.


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#3 niner

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Posted 04 April 2014 - 12:32 AM

Longvida curcumin is claimed to have 65 times the bioavailability of unformulated curcumin. They use some sort of liposome-related technology.

Curcumin is a great compound but it can be a libido killer.
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#4 LexLux

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Posted 04 April 2014 - 12:55 AM

Looking at the data presented, it seems that in that study 30mg Theracurmin corresponded to 80 ± 35 Cmax (nmol/L) and 307 ± 166 AUC (nmol/L × h), wheras 2g BCM-95 corresponds to 1240 Cmax (nmol/L) and 8690 AUC (nmol/L × h). Some BCM-95 bands contain more or less 60 x 500mg capsules, wouldn't that convert to 310 Cmax (nmol/L) and 2172.5 AUC (nmol/L × h) per 500mg?

Correct me if I'm wrong, but it seems the study was stating that the bioavailability of Theracurmin is better on the basis of a mass to bioavailability ratio. But to get to the same effects as 500mg BCM wouldn't I need to consume more or less 150mg Theracurmin?

The amount of theracurmin varries with the supplier but Integrative Therapeutics states that a product they sell contains 1.8g Theracurmin® (water-dispersible turmeric (Curcuma longa) rhizome) / 3 capsules, so like 600mg// capsule. That's quite a decent dosage.

Wouldn't that equate to about 1600 Cmax (nmol/L) and 18420 AUC (nmol/L × h) per capsule based on the figures taken from the study above?

Edited by LexLux, 04 April 2014 - 01:21 AM.


#5 LexLux

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Posted 04 April 2014 - 02:12 AM

this seems to be a good article on Theracurmin http://truttmd.com/c...te-theracurmin/

But I think the real story in the OP was the "micellar delivery system" and the sex differences:

"A significant gender effect was observed for AUC; women had significantly higher plasma AUC than men for all three curcuminoids, with the only exception of total plasma curcumin AUC for native curcumin, which was numerically higher due to the large interindividual differences in absorption of native curcumin in men (Table 2). The relative systemic availability of curcumin, as determined by comparing the plasma AUC, was 14, 5, and 9 times higher in women, men, and all subjects, respectively, after ingestion of curcumin micronisate, and 277-, 114-, and 185-fold higher, respectively, following the ingestion of curcumin micelles compared to the native form (Table 2). Relative to native curcumin, Cmax following micronisate ingestion were 11-, 3-, and 6-fold higher in women, men, and all subjects, respectively, and 806-, 251-, and 453-fold higher after ingestion of curcumin micelles."

[...]

"Cumulative urinary excretion of total curcumin, DMC, and BDMC over 24 h was significantly increased following the consumption of curcumin micronisate and micelles compared to native curcumin and both the formulation and sex significantly affected curcumin excretion (Table 3). The excretion of all three curcuminoids was approximately two to three times higher in women than men (Table 3). The mean percentages of the oral curcumin dose recovered as total curcumin in the 24 h urine samples of all subjects (n = 23) were 0.002 ± 0.012, 0.007 ± 0.005, and 0.151 ± 0.082% for native, micronized, and micellar curcumin, respectively."

Edited by LexLux, 04 April 2014 - 02:24 AM.


#6 ta5

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Posted 05 April 2014 - 02:51 PM

Comparing costs:

The absorption numbers used below did not come from the study above. I first tried to use that study, but I couldn't figure out how to convert those to multiples. The numbers did not make sense to me.

2880mg of 95% curcumin per day = 2736mg curcumin. This costs $386/year from PureBulk.
At 27x absorption, you need 4 caps of x 300mg Theracurmin = 102mg Curmumin x 27 = 2754mg equivalent. This costs $486/year from Swanson.
At 65x absorption, you need less than 1 cap of 500mg Longvida = 115mg Curcumin x 65 = 7475mg equivalent. This costs $218/year from Nutrivene.
At 7x absorption, you need 1 cap of 400mg BCM-95 = 380mg Curcumin x 7.29 = 2772mg equivalent. This costs $173.38/year from iHerb.
At 18x absorption, you need 2 caps of 500mg Meriva = 180mg Curcumin x 18 = 3240mg equivalent. This costs $133.71/year from Swanson.
At 10x absorption, you need 3 caps of 500mg Meriva = 270mg Curcumin x 10 = 2700mg equivalent. This costs $200.57/year from Swanson.

There are several different numbers reported for Meriva. The Meriva study found 29x absorption, but that was for all curcuminoids, where they found 18x for just curcumin. For some reason Swanson advertises 10x absorption.

I don't know if the advertised absorption multiples were always comparing only curcumin or all curcuminoids, or if they compared area-under-the-curve, or peak concentration.

If you always take curcumin with omega 3, other fatty acids, a meal including fat, and/or with pepper, that should result in much higher absorption compared to taking it with water on an empty stomach. I think the participants in the studies took the curcumin with water on an empty stomach. I believe this will take away from the advertised absorption multiples. Who knows how much?
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#7 LexLux

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Posted 06 April 2014 - 11:37 AM

What about Longvida vs Meriva?
Both of those brands use some form of phospholipid, but the two formulas do not have identical absorption.
Meriva (sold by Thorne) has a small human study showing benefit using two capsules twice a day for osteoarthritis, but that is only based on subjective data (pain and functionality scales rather than serum inflammatory markers).
Usana (a large supplement company) analyzed Meriva bioavailability and here is what they said:


Free curcumin could not be detected in any plasma samples, in accordance with previous studies that have mostly failed to detect unconjugated curcumin in human plasma even after the administration of megadoses of curcumin.

However, Usana did find some metabolites of curcumin (referred to as ‘curcuminoids’):
The peak plasma total curcuminoid concentration (Cmax) reached with the high dosage of Meriva was 206.9 ng/mL…. [However] Within the context of curcumin human absorption, the >200 ng/mL concentration of conjugated curcuminoids is still lower than the low micromolar concentration of free curcumin required for direct activity against its various targets. 6
In addition, some studies suggest that although some of the curcuminoid metabolites have anti-inflammatory effects (and thus may be helpful against arthritis, which is what Meriva is marketed for), only curcumin, not its metabolites, will work against Alzheimer’s:


Despite dramatically higher drug plasma levels after administering [the curcuminoid metabolite] tetrahydro-curcumin… only curcumin was effective in reducing amyloid plaque burden. Tetrahydro-curcumin had no impact on [Alzheimer’s] plaques or insoluble Amyloid-β… Curcumin, but not tetrahydro-curcumin, prevented Amyloid β aggregation. 7

Therefore, for prevention of Alzheimer’s, Longvida is the better choice.- See more at: http://truttmd.com/c...h.48D20tis.dpuf

What about Longvida vs Meriva?
Both of those brands use some form of phospholipid, but the two formulas do not have identical absorption.
Meriva (sold by Thorne) has a small human study showing benefit using two capsules twice a day for osteoarthritis, but that is only based on subjective data (pain and functionality scales rather than serum inflammatory markers).
Usana (a large supplement company) analyzed Meriva bioavailability and here is what they said:


Free curcumin could not be detected in any plasma samples, in accordance with previous studies that have mostly failed to detect unconjugated curcumin in human plasma even after the administration of megadoses of curcumin.

However, Usana did find some metabolites of curcumin (referred to as ‘curcuminoids’):
The peak plasma total curcuminoid concentration (Cmax) reached with the high dosage of Meriva was 206.9 ng/mL…. [However] Within the context of curcumin human absorption, the >200 ng/mL concentration of conjugated curcuminoids is still lower than the low micromolar concentration of free curcumin required for direct activity against its various targets. 6
In addition, some studies suggest that although some of the curcuminoid metabolites have anti-inflammatory effects (and thus may be helpful against arthritis, which is what Meriva is marketed for), only curcumin, not its metabolites, will work against Alzheimer’s:


Despite dramatically higher drug plasma levels after administering [the curcuminoid metabolite] tetrahydro-curcumin… only curcumin was effective in reducing amyloid plaque burden. Tetrahydro-curcumin had no impact on [Alzheimer’s] plaques or insoluble Amyloid-β… Curcumin, but not tetrahydro-curcumin, prevented Amyloid β aggregation. 7

Therefore, for prevention of Alzheimer’s, Longvida is the better choice.- See more at: http://truttmd.com/c...h.48D20tis.dpuf

What about Longvida vs Meriva?
Both of those brands use some form of phospholipid, but the two formulas do not have identical absorption.
Meriva (sold by Thorne) has a small human study showing benefit using two capsules twice a day for osteoarthritis, but that is only based on subjective data (pain and functionality scales rather than serum inflammatory markers).
Usana (a large supplement company) analyzed Meriva bioavailability and here is what they said:


Free curcumin could not be detected in any plasma samples, in accordance with previous studies that have mostly failed to detect unconjugated curcumin in human plasma even after the administration of megadoses of curcumin.

However, Usana did find some metabolites of curcumin (referred to as ‘curcuminoids’):
The peak plasma total curcuminoid concentration (Cmax) reached with the high dosage of Meriva was 206.9 ng/mL…. [However] Within the context of curcumin human absorption, the >200 ng/mL concentration of conjugated curcuminoids is still lower than the low micromolar concentration of free curcumin required for direct activity against its various targets. 6
In addition, some studies suggest that although some of the curcuminoid metabolites have anti-inflammatory effects (and thus may be helpful against arthritis, which is what Meriva is marketed for), only curcumin, not its metabolites, will work against Alzheimer’s:


Despite dramatically higher drug plasma levels after administering [the curcuminoid metabolite] tetrahydro-curcumin… only curcumin was effective in reducing amyloid plaque burden. Tetrahydro-curcumin had no impact on [Alzheimer’s] plaques or insoluble Amyloid-β… Curcumin, but not tetrahydro-curcumin, prevented Amyloid β aggregation. 7

Therefore, for prevention of Alzheimer’s, Longvida is the better choice.- See more at: http://truttmd.com/c...h.48D20tis.dpuf
I've read that Meriva doen't actually significantly elevate free curcumin; only its metabolite curcuminoids.
  • http://truttmd.com/curcumin-caveat-emptor-not-all-brands-are-created-equal/

According to the same source, Longvida increases curcumin levels and Theracurmin is useful because its absorbtion increases progressively with increased dose as opposed to Longvida.
  • http://truttmd.com/curcumin-update-theracurmin/


#8 LexLux

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Posted 06 April 2014 - 02:35 PM

lol Ok I didn't think that quote was posted, its a quote from Trutt on Meriva. Read the bottom starting at "I've" for what I actually intended to post!

#9 hav

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Posted 07 April 2014 - 04:30 PM

Looks like a really good study ranking the relative performance of capsuled products with the BCM95 dosage of 2 grams tops followed by Meriva with a mere dosage of 376 mg and Longvida trailing even with a dosage of 4 grams.

Not sure what to make of their micelles/tween 80 results which topped everything. I can't tell from the way this is worded if they administered everything they tested mixed into that German syrup:

All participants orally ingested in random order a single dose of 500 mg curcuminoids (containing 410 mg curcumin, 80 mg DMC, and 10 mg BDMC) as native powder, micronized powder, or liquid micelles mixed into 50 g woodruff syrup.


Haven't been able to track down the chemical composition of Woodruff Syrup but I've seen references to it being sweet and being used to make a kind of beer.

Howard

Edited by hav, 07 April 2014 - 04:32 PM.


#10 krillin

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Posted 04 August 2014 - 12:20 AM

The micellar product appears to be NovaSOL. Note that one 500 mg capsule brings you into the mTOR inhibition concentration range, so it should be taken cyclically. While taking it, stem cells will become resensitized to mTOR, but will be fairly dormant. During the break you get youthful cell proliferation. Here's a reference for the rejuvenating effect on stem cells of inhibiting mTOR with rapamycin, and here's a reference for increased lifespan while cycling rapamycin 2 weeks on, 2 weeks off.



#11 gavino

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Posted 05 August 2014 - 06:26 PM

Yay!  Krillin is back.  Where have you been?  As a longtime lurker, I've noticed quite a decline in the quality of posts here and, frankly, a lot of the "mental health" posts worry me - misguided anecdotally based experimentation that seems incredibly irresponsible. 

 

Anyways, as I get busier in my life and have less and less time to read for "pleasure" I consider myself very fortunate to be able to read posts by the niners, maxwatts, and krillins of the world.  When I see a post from those of your ilk, I know it's gonna be worth my time.  Thank you

 


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#12 gavino

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Posted 05 August 2014 - 06:34 PM

Also, I can not find a vendor for the above mentioned NovaSol/Frutarom product.  If you have any leads it would be greatly appreciated.  Thanks



#13 krillin

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Posted 06 August 2014 - 04:15 AM

I was hanging out in chemical sensitivity groups, but they eventually petered out and I ran out of experiments to try.

 

I don't think NovaSOL is carried by anyone yet, so I've been emailing supplement companies requesting they look into it.



#14 Anthony_Loera

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Posted 09 February 2015 - 08:14 PM

MetaCurcumin uses micellar curcumin,

 

We use it in a pump... here is a squirt from the pump on top of a corn chip at a restaurant I was at...

that is equivalent to about 2 grams... (avg men and women)

 

Attached File  RevGenetics Liquid Curcumin on a chip.jpg   89.04KB   7 downloads

 

cheers

A


Edited by Anthony_Loera, 09 February 2015 - 08:15 PM.


#15 Darryl

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Posted 10 February 2015 - 02:45 AM

This paper (on another polyphenol, quercetin) caused me to wonder about some unanticipated effects of the microsomal formulations. Not so worried about the supplement bypassing enterocytes into lymphatic circulation, but about fellow travellers.

 

Guo, Y., Mah, E., & Bruno, R. S. (2014). Quercetin bioavailability is associated with inadequate plasma vitamin C status and greater plasma endotoxin in adultsNutrition30(11), 1279-1286.

 

Greater quercetin absorption and bioavailability may be associated with poor vitamin C status and increased intestinal permeability in healthy adults.

 


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#16 Thomas Blakeslee

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Posted 22 December 2015 - 01:41 AM

Novasol is available from delta as curcumin on Amazon



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#17 joelcairo

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Posted 26 December 2015 - 06:48 AM

 

This paper (on another polyphenol, quercetin) caused me to wonder about some unanticipated effects of the microsomal formulations. Not so worried about the supplement bypassing enterocytes into lymphatic circulation, but about fellow travellers.

 

Guo, Y., Mah, E., & Bruno, R. S. (2014). Quercetin bioavailability is associated with inadequate plasma vitamin C status and greater plasma endotoxin in adultsNutrition30(11), 1279-1286.

 

Greater quercetin absorption and bioavailability may be associated with poor vitamin C status and increased intestinal permeability in healthy adults.

 

 

 

Topic got bumped so I am just now following up on this... Note that the study you quote is saying that individuals who absorb greater quantities of quercetin tend to have the characteristics mentioned. If I understand the abstract correctly, the differences in quercetin bioavailability aren't the cause, they're the effect.







Also tagged with one or more of these keywords: curcumin, oral, bioavailability, bcm-95, longvida, theracurmin, meriva, micellar delivery

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