Piperine inhibits the production of p-glycoprotein and CYP3A4 enzymes that are key in transporting 

and metabolizing xenobiotics and metabolites.

It’s also been found to inhibit enzymes that are key in drug metabolism. In this way, piperine can inhibit the effectiveness of some drugs.

However, it has also been found to assist and enhance the properties of some supplements, making the use of piperine as bioavailability enhancer for supplements a viable application.

Health Benefits of Piperine Absorption

Some of the main mechanisms the body uses to process food and nutrition at a cellular level include assisted exclusion, solubilizer attachment, metabolic conversion and assisted absorption. These processes work as follows:

Assisted Exclusion. Transporter proteins act to move specific substances from the cells so they can be moved by the blood. This pumping mechanism protects cells from toxic overloads but can at times can impede the effectiveness of supplements and beneficial drugs. The most important protein in this group is p-glycoprotein, found in the intestines, liver, kidneys, pancreas, brain and other tissues.

Solubilizer Attachment. This mechanism works to prevent substances from entering the cells through linkage to a highly water-soluble substance. They in effect alter biological processes in addition to making some substances unable to permeate cell membranes. Glucuronic acid is one example; this solubilizer causes substances to be more readily excreted.

Metabolic Conversion. This process uses enzymes to convert substances to less active compounds so that they can be more easily carried within the blood to the kidneys for excretion. 

Assisted Supplement Absorption Rates. This involves transporter proteins in the digestive tract to move substances to the intestinal lining for transference into the blood. It is particularly important for ensuring the availability of essential amino acids in ideal amounts.

Piperine has the ability to participate in and influence all four of these mechanisms. While it can inhibit a number of enzymes that metabolize some drugs and nutritional substances, it is also effective in amino acid transport activity within the intestinal lining.

Also piperine greatly amplifies the pumping effect of p-glycoprotein from removing substances from cells.

It decreases production of glucuronic acid in the intestines as well, allowing more of these substances to enter the body and increasing the duration of their effect within the cells.

When used with substances the body requires, this can dramatically increase the effect of the drug or supplement. However, it can also potentially increase the effect of some drugs to overdose levels, so caution must be taken.

Piperine as Bioavailability Enhancer for Supplements

A positive piperine property is its ability to fuel fat loss. It does so due its capacity to help increase thermogenic action within the body. Thermogenesis refers to the creation of cellular energy which fuels the body’s metabolism.

Piperine is also effective against inflammation in the body. This makes it a viable treatment or complementary treatment for conditions characterized by inflammation, including rheumatoid arthritis and fibromyalgia.

Piperine has also shown viability in helping to fight and prevent cancer. Animal studies showed piperine had a positive impact on lung cancer and was effective in slowing down the formation of tumors.

Piperine is also a known mood enhancer. It improves the production of serotonin, a neurotransmitter associated with positive feelings of well being as well as pain relief.

Again, it is important to be aware of the specific effect piperine has on a drug or supplement, as it can either potentiate or inhibit their effectiveness.  Piperine ’s most noteworthy effect is the inhibiting of metabolic enzymes in some cases while increasing their production in others.

A prime example of piperine as bioavailability enhancer for supplements in a positive way is its interaction with curcumin (extract from turmeric), a supplement known to combat inflammation, infections and various types of cancers.

It’s estimated that just a 20 mg dose of piperine increases the bioavailability of curcumin in the body by as much as 20 times!

Piperine also generally enhances nutrient absorption. It is effective in boosting the bioavailability of nutrients like vitamin B6, beta-carotene, curcumin, selenium, glucose and amino acids. This makes piperine as bioavailability enhancer for supplements an ideal choice to boost their effectiveness.

The partnership between piperine and supplements also promotes the absorption and metabolism of both substances in many cases.

Piperine as bioavailability enhancer for supplements is known to work with the following substances:

• Curcumin 
• CoQ10
• Vitamin B-6
• Amino acids
• Beta-carotene
• Dapsone
• Nalorphine
• Phenytoin
• Propranolol
• Ethambutol
• Isoniazid
• Pyrazinamide
• Rifampicin
• Selenium  
• Sulfadiazine
• Theophylline
• Glucose  

A far larger number of substances are inhibited by the presence of piperine, reducing their bioavailability.

Some of the most common include  acetaminophen, barbiturates, benzodiazepines, caffeine, chlorzoxazone, codeine, fentanyl, St. John’s wort and testosterone, but there are dozens of other substances on this list. 

Other benefits and actions of piperine include:

• Increasing beta-endorphins in the brain
• Pain relief
• Increased serotonin
• Anticonvulsant
• Increasing adrenaline production
• Calms digestive contractions
• Reduces stomach acid production  
• Increases digestive enzyme production  
• Stimulates melanin production
• Reduces inflammation  
• Relieving asthma and allergy symptoms

Since piperine is a natural substance from black pepper that has been in use medicinally for centuries, many are drawn to it. It is not connected with any significant patterns of problems over the years, but caution is always advised when taking this or any other supplement.

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