Piperine Enhances the Serum Concentration, Extent of Absorption and Bioavailability of Curcumin

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The consumption of curcumin powder, a very lipophilic (fat soluble) substance, which has been obtained from the tumeric root (Curcuma longa L.), has poor bioavailability due to the following factors:

  • low intestinal absorption rate
  • rapid metabolism in the liver and intestinal wall due to glucuronidation
  • rapid systemic elimination

Because of this poor bioavailability, even with large amounts of consumed curcumin, there is low levels in the blood plasma and tissues.  The majority of consumed curcumin is excreted via the feces. This is why consuming large amounts of the curcumin powder may lead to diarrhea.

Glucuronidation

Glucuronidation is a Phase II process in metabolic detoxification which consists of the transfer of the glucuronic acid component of uridine diphosphate glucuronic acid to a toxic substrate resulting in substances known as glucuronides which are water-soluble.  These water-soluble glucuronides are subsequent eliminated from the body through urine or feces (via bile from the liver).

In the case of curcumin (without augmenting absorption), it is rapidly metabolised by glucuronic acid in the liver and intestinal wall and made water-soluble and mostly excreted via the feces. 

There are a number of ways in which to improve the bioavailability of curcumin by augmenting its absorption.  Some of the approaches that have been taken are:  1

  • adjuvant like piperine that interferes with glucuronidation
  • curcumin nanoparticles
  • curcumin phospholipid complex
  • liposomal curcumin
  • structural analogues of curcumin

Piperine

Piperine, which is derived from Black pepper (Piper nigrum) and a number of different varieties of pepper species, has many physiological effects.   Piperine, by favorably stimulating the digestive enzymes of the pancreas, enhances the digestive capacity and significantly reduces the gastrointestinal food transit time. Piperine has been demonstrated in in vitro studies to protect against oxidative damage by inhibiting or quenching free radicals and reactive oxygen species.  2

For more in-depth information on the current research into Piperine, read this article from Healthy But Smart entitled:  Does Piperine Have Health Benefits? The Current Research Examined

Piperine has been documented to enhance the bioavailability of curcumin by modifying the rate of glucuronidation by lowering the endogenous UDP-glucuronic acid content and strongly inhibiting hepatic and intestinal aryl hydrocarbon hydroxylase and UDP-glucuronyl transferase.  Piperine’s bioavailability enhancing property is also partly attributed to increased absorption as a result of its effect on the ultrastructure of intestinal brush border.  3

A study published in 1998, researchers examined the effect of combining piperine, a known inhibitor of hepatic and intestinal glucuronidation, on the bioavailability of curcumin in rats and healthy human volunteers. 

Humans were administered a dose of 2 grams of curcumin by itself and serum levels were either undetectable or very low. They then administered the same dosage of curcumin (2 grams) with a concomitant administration of piperine at 20 mg.  The result was a much higher concentrations from 0.25 to 1 h post drug (P < 0.01 at 0.25 and 0.5 h; P < 0.001 at 1 h), and an increase in bioavailability of 2000% or a 20-fold increase in bioavailability.

The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in humans with no adverse effects.  4

This study may lead to the conclusion to add some ground-up black pepper kernals with your curcumin powder.  Unfortunately, the consumption of black pepper directly with curcumin will not help achieve enhanced nutrient absorption, as was found in the above referenced study. 

In fact, one would have to consume large quantities of black pepper to achieve even a modest amount of piperine bioavailability, which is impractical.  The reason for this is that piperine remains captive in the form of raw black pepper and it takes time for its bioavailability enhancing property to be released.

Therefore, a purified extract of piperine is necessary to get the increased absorption.  This is where BioPerine® is useful. 

BioPerine®, a natural bioavailability enhancer from Sabinsa Corporation, received Generally Recognized As Safe (GRAS) status after a comprehensive review of safety and toxicology data by an independent panel of scientists with international repute.  Based on scientific procedures and available comprehensive scientific literature, including human and animal data determined the safety-in-use for black pepper extract (BioPerine®).

BioPerine® significantly improved the uptake of Curcumin—the healthful extract from turmeric roots with clinically validated efficacy in a wide range of health conditions ranging from inflammation to cancer.

Bioavailability of Curcumin (2000 mg) when co-administered with BioPerine® (20 mg) was enhanced by 20-fold or 2000% compared to bioavailability of Curcumin alone at doses that were devoid of adverse side effects.

piperinegraph

BioPerine® also increases the bioavailability of other natural substances:

Applications of BioPerine®

The nutritional materials which may be co-administered with BioPerine® are as follows:

Herbal Extracts   Curcuma longa, Boswellia serrata, Withania somnifera, Ginkgo biloba and Capsicum annuum
Water-soluble Vitamins    Vitamin B1, Vitamin B2, Niacinamide, Vitamin B6, Vitamin B12, Folic acid and Vitamin C
Fat-­soluble Vitamins   Vitamin A, Vitamin D, Vitamin E and Vitamin K
Antioxidants   Vitamin A, Vitamin C, Vitamin E, alpha-carotene, beta-carotene, beta-cryptoxanthin, lycopene, lutein/zeaxanthin, pine bark bioflavonoids complex, germanium, selenium and zinc
Amino Acids   Lysine, isoleucine, leucine, threonine, valine, tryptophan, phenylalanine, and methionine
Minerals   Calcium, iron, zinc, vanadium, selenium, chromium, iodine, potassium, manganese, copper and magnesium

Source:  BioPerine®

Informational References:

Health But Smart:  Does Piperine Have Health Benefits? The Current Research Examined

Cover Photo:  Black Pepper tree (piper nigrum)