During studies on the effect of piperine on the absorption of active substances in the body, it has been demonstrated that it enhances absorption by interacting with the cell membrane of the intestines (e.g., weakening the hydrophobic effect).
The piperine molecule
Years of research on the effects of administering black pepper extracts standardized to piperine have shown its significant efficacy in enhancing the absorption of various substances by the body.
For example, increased bioavailability of drugs such as nevirapine (an HIV-1 reverse transcriptase inhibitor), phenytoin (an antiepileptic drug), propranolol (a non-selective β-blocker for hypertension), and theophylline (a bronchodilator) has been demonstrated.
🔬 Clinical Research Findings – Increased Bioavailability
Below are the results of three out of many studies demonstrating increased absorption of phytonutrients, minerals, and vitamins as shown during clinical trials of Bioperine® – standardized to 95% piperine content from black pepper extract.
Vitamin C
In a double-blind, cross-over study, the bioavailability of vitamin C (500 mg/day) administered with the heart medication, propranolol hydrochloride (HCl) (10 mg), with or without Bioperine®, was evaluated. Serum concentration measurements showed that administering vitamin C with propranolol HCl in the presence of Bioperine® resulted in a 52.3% increase in serum vitamin C concentration (Cmax = 110.6 μg/ml) compared to the control group (Cmax = 72.6 μg/ml, Fig. 6). The absorption increased by 39.2% with Bioperine® compared to the control group (361.2 μg/hr/ml and 259.5 μg/hr/ml, respectively).
On the other hand, serum levels of propranolol HCl did not show a significant increase. The maximum concentration of propranolol hydrochloride in serum with Bioperine® (Cmax = 3.8 μg/ml) was only 9.4% higher than the concentration in serum without Bioperine® (Cmax = 3.4 μg/ml). The absorption for propranolol hydrochloride with Bioperine® was 11.6 μg/hr/ml and did not differ significantly from that without Bioperine® (10.6 μg/hr/ml).
A 53% increase in the absorption of vitamin C.
Coenzyme Q10
The bioavailability of coenzyme Q10 (120 mg) was assessed with and without supplementation of Bioperine®. As CoQ10 is an endogenous component, volunteers underwent screening to obtain comparable baseline values of CoQ10 (0.30-0.60 μg/ml). After 21 days of supplementation, simultaneous administration of Bioperine® resulted in an absolute increase in serum CoQ10 concentration of 1.12 μg/ml compared to an absolute increase of 0.85 μg/ml in the control group (absolute increase defined as the difference between final values and the baseline value, which was set at 0.50 μg/ml). A 30% increase in the bioavailability of coenzyme Q10 supported by Bioperine® was observed compared to the control group.
30% increase in the bioavailability of coenzyme Q10
β-Carotene
The relative bioavailability of beta-carotene supplement with and without Bioperine® was evaluated in a double-blind, crossover study. Beta-carotene serum concentrations were measured during two separate 14-day study phases. The mean baseline values of beta-carotene in serum were statistically similar at the beginning of both the control supplementation phase (beta-carotene + placebo) and the experimental supplementation phase (beta-carotene + Bioperine®). However, a 60% increase in bioavailability was observed in the experimental group (beta-carotene + Bioperine®) compared to the control group after 14 days of supplementation.
🔵 Conclusion:
The results of these studies clearly demonstrate a significant improvement in the absorption of vitamins and phytonutrients when supplements are taken with black pepper extract standardized to 95% piperine.
References:
1. Srinivasan K. Black pepper and its pungent principle-piperine: a review of diverse physiological effects. Crit Rev Food Sci Nutr. 2007;47(8):735-748.
2. Hiwale AR, Dhuley JN, Naik SR. Effect of co-administration of piperine on pharmacokinetics of beta-lactam antibiotics in rats. Indian J Exp Biol. Mar 2002;40(3):277-281.
3. Lambert JD, Hong J, Kim DH, Mishin VM, Yang CS. Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice. J Nutr. Aug 2004;134(8):1948-1952.
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8. Khajuria A, Zutshi U, Bedi KL. Permeability characteristics of piperine on oral absorption–an active alkaloid from peppers and a bioavailability enhancer. Indian J Exp Biol. Jan 1998;36(1):46-50.
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10. Allameh A, Saxena M, Biswas G, Raj HG, Singh J, Srivastava N. Piperine, a plant alkaloid of the piper species, enhances the bioavailability of aflatoxin B1 in rat tissues. Cancer Lett. Jan 31 1992;61(3):195-199.
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Q&A
which means frequently asked questions and answers…
What is piperine?
Piperine is an organic compound that belongs to the alkaloid group, found in the outer layer of black pepper (Piper nigrum L.) fruit. It is characterized by its sharp, bitter taste, creamy yellow color (it can also be colorless), and crystalline form.
Piperine was discovered by Hans Christian Ørsted in 1819, who extracted it from black pepper fruit. It exhibits many medicinal properties.
What properties does piperine exhibit?
Many ancient sources describe the medicinal properties of organic black pepper extract.
Ayurveda recommends taking this spice for fevers, various digestive ailments, and respiratory problems. Traditional Chinese medicine, on the other hand, used it to relieve headaches, muscle pain, and rheumatic pains and treat viral and bacterial infections.
Modern research has shown the health benefits of black pepper extract:
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- influences better absorption of nutrients and vitamins
- stimulates metabolism
- improves the functioning of the digestive system
- relieves joint pain with its anti-inflammatory effect
- supports the immune system
- provides antibacterial, antiviral, and antifungal effects
- helps prevent cancer
- prevents the onset of heart disease
- stimulates the nervous system
- gives a positive effect on memory and concentration
- acts as an antidepressant
How does piperine affect the absorption of phytonutrients, minerals, and vitamins?
Fat cells can block the absorption of nutrients in the intestines. Piperine interacts with fat cells, increasing the absorptive surface area of the small intestine and allowing more phytonutrients, minerals, and vitamins to enter the system.
Which nutrients and vitamins are worth combining with piperine?
Taking piperine significantly affects the absorption of certain nutrients and vitamins, including:
- vitamin C: Studies have shown a 53% increase in bioavailability
- coenzyme Q10: 30% increase in bioavailability
- β-Carotene: 60% increase in bioavailability
- curcumin: 10-fold increase in bioavailability
Does piperine improve the bioavailability of drugs?
Yes. Studies have shown that taking (piperine) black pepper extract increases the bioavailability of drugs such as:
- nevirapine (an antiviral drug used to treat people infected with HIV-1)
- phenytoin (an anti-epileptic drug)
- propranolol (a drug for hypertension, angina, migraines, and many others)
- theophylline (a drug that dilates the bronchi and makes breathing easier)
Can piperine treat cancer?
Scientific studies have shown that piperine has antimutagenic potential, meaning it can inhibit the action of chemicals responsible for the formation of genetic mutations.
Researchers from the University of Michigan conducted a study in which they added piperine to breast cancer cell cultures, finding that the substance blocked the growth of cancer cells. This gives hope for the invention of an effective drug to prevent breast cancer in the future.
Does piperine cause unwanted side effects?
Piperine does not exhibit any toxic properties and is perfectly safe to use as directed. However, it is worth noting that in large quantities, it has a strong diuretic effect and accelerates digestion, which can cause diarrhea.
