Bioenhancer

Curry powder contains the bioenhancers curcumin and piperine.

Black Pepper contains high concentrations of piperine.

The bioenhancer quercetin is inter alia included in the peel of apples and grapes.

The gingerols from ginger act as bioenhancers.

Allicin from garlic enhances the effect of a fungicide.

Bioenhancers or bioavailability enhancers is a new chapter in medical science first scientifically established in 1979 after the discovery of world's first bioenhancer Piperine. It is a pocket friendly drug technology which reduces the destruction, wastage and elimination of several orally administered drugs inside the body.

Definition Bioenhancers are defined as substances that increase the bioavailability and bioefficacy of active substances with which they are combined without having any activity of their own at the dose used. Besides several classes of modern drugs like antibiotics, anti cancer drugs, cardiovascular drugs, anti inflammatory, central nervous drugs, etc, they also increase the bioavailability of vitamins and nutrients.

Significance of Bioenhancers Due to an increased bioavailability, the dose and cost of active drug can be reduced,making the formulation cheaper and safer. Safer formulation also means better tolerated, having better compliance and therefore having lesser risk of developing drug resistance as in case of antibiotics.As it benefits the dose economy,it is particularly of great value to poor ill diseased segment of society.For example, by reducing the required dose of expensive toxic Rifampicin by 60 percent,it correspondingly reduces the cost and side effects of Rifampicin while treating the dreaded disease Tuberculosis.^[1]

History The term bioavailability enhancers was first coined in 1979 at Indian Institute of Integrative medicine, Jammu, formerly RRL,Jammu, by Indian scientists (Atal, C. K and coworkers) who discovered and scientifically validated Piperine as world's first bioenhancer.^[2][3][4]

Classification bioenhancers can be classified according to their source of origin,either plant based or animal based or else according to their site of action.

Bioenhancers so far almost exclusively discovered in plants, increase the bioavailability of other substances in different ways:

• Increase of absorption in the intestine
• Inhibition of degradation in the intestine and the liver
• Increase of permeability of pathogens
• Inhibition of defense mechanisms of pathogens or tumor tissue (such as efflux of drugs)
• Increasing binding possibilities on binding sites (such as DNA and proteins) of the pathogen
• Improving overcoming of the blood-brain barrier

Examples of bioenhancers

The following examples of bioenhancers give an insight into the current pharmacological research and show how with pepper, curry, ginger and other herbal ingredients in food a lack of nutrients or insufficient effects of active agents can be prevented:

Piperine, an ingredient of pepper, promotes intestinal absorption by activation of the γ-glutamyltranspeptidase and inhibits the degradation of many compounds, by inhibiting different enzymes: aryl hydrocarbon hydroxylase (AHH), ethylmorphine N-demethylase, Uridine diphosphate (UDP) glucuronyltransferase (UGT), P-glycoprotein and CYP3A4. Especially the latter two enzymes contribute significantly to the first-pass effect.

Piperine acts as bioenhancer to vitamins (A, B1, B2, B6, C, D, E, K), amino acids (lysine, isoleucine, leucine, threonine, valine, tryptophan, phenylalanine, and methionine), minerals (iodine, calcium, iron, zinc, copper, selenium, magnesium, potassium, manganese), herbal compounds (including ginsenosides, Pycnogenol), and drugs (such as ibuprofen, diclofenac, rifampicin, ampicillin, tetracycline, vasicine, pyrazinamide, fexofenadine, resveratrol, epigallocatechin, curcumin).

Allicin from garlic enhances the effect of the fungicide amphotericin B on yeast cells by affecting the transport of the fungicide into the yeast vacuole.

Curcumin which inter alia is found in curry inhibits like piperine the enzyme CYP3A4 and affects the transport function of P-glycoprotein. In combination with curcumin an increased bioavailability of the active compounds celiprolol and midazolam was detected.

Ginger promotes due to the gingerols the intestinal absorption of many compounds (including drugs) and elements. In most cases, ginger acts synergistically with piperine.

Glycyrrhizin, a saponin of the liquorice plant, promotes the action of numerous antibiotics and the antifungal agent clotrimazole.

Quercetin, a flavonoid from fruits and leaves, acts like curcumin and piperine. It increases the bioavailability of the active agent paclitaxel used to treat cancer.

Application of research results

The bioenhancer technology is primarily targeted for toxic drugs, expensive drugs, scarce drugs,poorly bioavailable drugs or drugs which need to be given for prolonged periods. However it can also be used in any drugs influenced by bioenhancers. The discovery and characterization of bioenhancers has led to several patent applications.^{[5] [6]} Piperine is marketed as bioenhancer in mono preparations and as a component of dietary supplements that contain different vitamins, curcumin, resveratrol or Coenzyme Q₁₀.

Since bioenhancers can reduce the dosage and cost of expensive medication while making treatment safer, its application has for the first time been done in humans in treating tuberculosis for which the existing drugs are toxic and expensive and need to be administered over prolonged periods. In India where low treatment costs for medical care are essential, the drug Risorine is approved against tuberculosis. Besides the antibiotics rifampicin and isoniazid it contains piperine.^[7]

Footnotes

References

Ghanshyam B. Dudhatra, Shailesh K. Mody, Madhavi M. Awale, Hitesh B. Patel, Dr. Yury Kronn, Chirag M. Modi, Avinash Kumar, Divyesh R. Kamani, Bhavesh N. Chauhan. "A Comprehensive Review on Pharmacotherapeutics of Herbal Bioenhancers". The Scientific World Journal. Jan 2012, Vol. 2012: 1-33. http://www.ncbi.nlm.nih.gov/pubmed/23028251