Few know what it is. Even less suggest ways to improve it. Among those few are biotechnologists and Ayurveda therapists. Here's why!
Natural Medicine – Our why plant substances could be much more powerful
Natural substances, which are rooted as remedies in numerous cultures’ traditions, not uncommonly show an equally impressive effect under the magnifying glass of science.
The laboratory environment and testing on simple cell systems provide clues to the properties of the molecule itself, but often not to the effect in complex organisms like ours.
The low in vivo activity (tested in living organisms) of otherwise active plant ingredients is due to several structural properties of those molecules.
The most important factor, however, is the following:
Many substances extracted from plants and taken for health promotion purposes show a greatly reduced bioavailability in in vivo studies.
This means: The amount of active substance that arrives in the bloodstream and reaches its site of action is greatly reduced by absorption problems (pharmacological term: bioavailability).
The theoretical potential of the active substance is therefore of secondary importance because it does not reach the cells.
Of course, this does not apply to all secondary plant substances. However, for those of them who have been confirmed as beneficial to health, low absorption is a problem.
What can influence bioavailability?
A major problem of plant substances is their water insolubility!
Some secondary plant compounds are difficult to dissolve in water. To be absorbed by the intestinal wall, substances must be divided into smaller portions, which are then gradually absorbed by diffusion in conjunction with dietary fats.
Other obstacles can be caused by sensitivities of the natural products to the environment of our digestive system, a defective uptake mechanism or by a diseased intestine or liver.
- Due to the popularity of active plant ingredients, lipid-based transport systems have been developed which can be used to introduce a much higher proportion of secondary plant substances into the cells.
- In Ayurveda, this same concept has been known for thousands of years. Bio-enhancers (from bioavailability enhancer) offer another possibility to make nutraceuticals many times more effective through their interaction with absorption supporting substances.
Traditional medicine and drug development?
Ancient knowledge from Ayurveda and TCM often contributes to the discovery of "new" active substances (example: Artemisinin). Conventional drug development in Western pharmacy, however, relies largely on the physicochemical properties of molecules and creates slight variations of a promising substance.
The safety and efficacy of the active ingredient are then analyzed in subsequent multiple-stage, intensive studies.
Skipping the first screening phase of potential drug candidates and working with already known plant compounds as the basis for clinical studies would save years in research.
The Science of Bio-enhancers
Bioenhancers, too, originally came from traditional medicine until they were scientifically described and validated in 1979 by researchers at the Indian Institute of Integrative Medicine.
A typical bioenhancer, including the three representatives of the Trikatu from Ayurveda, shows no particular biological activity itself.
But when taken together with specific medication or nutraceuticals, they increase the effect of this primary substance by:
1. enhancing solubility
2. structural interactions with the drug or its receptor
3. by making target cells more receptive to it1.
What is piperine?
Piperine is an active ingredient from long pepper and black pepper. It represents the first- and best-described bio-enhancer. Since its discovery in India in 1979, piperine has been shown to increase the bioavailability of various drugs. The bioavailability of curcumin is increased tenfold by combining them3.
What does absorption mean?
At the interface of the outside world and the inside of the body, the intestinal absorption stands guard: The uptake of molecules through the intestinal cells or enterocytes into the bloodstream.
In our body, bile salts are responsible, e.g. for binding food lipids and to increase their surface area for improved uptake. Certain chelators, fatty acids and polymers also help in absorption at the intestinal walls.
In supplementation, insoluble substances can be introduced into liposomes or other emulsions. In addition to the charge of a substance, its molecular size is also crucial for its uptake.
But botanical substances are often not only too big due to their complexity, but also difficult to break down.
What possibilities does the use of bio-enhancers offer?
Effectiveness of various plant extracts from traditional medicine is often only a theoretical value. Especially when the active ingredient is administered in its isolated form.
While whole plant powders contain additional substances that support absorption, the extraction of a single substance during pharmaceutical processing is usually weakening its uptake.
Since an effective dose of ingested pharmaceuticals or nutraceuticals is to enter the bloodstream, more and more methods have been developed to improve the effect of plant active substances in recent years.
Bio-enhancers and lipid-based approaches dominate the nutraceuticals market and are in the process of making nutraceuticals more attractive than pharmaceuticals.
Nutraceuticals could become products for therapeutic and preventive usage with:
· fewer side effects
· high absorption rate and efficiency
In the future, their optimization could lead to less wasted resources.
For the same effect, less of a plant compound could be consumed and therefore less produced. Costs can also be reduced in this way. Due to the reduced, active dose required, dangers due to toxicity and resistance formation are eliminated.
Bio-enhancers open up new possibilities for drugs and nutraceuticals.
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 Khajuria A, Zutshi U, Bedi KL. Permeability characteristics of piperine on oral absorption - An active alkaloid from peppers and a bioavailability enhancer. Ind J Exp Biol. 1998;36:46–50.
 Ghanshyam B. Dudhatra, Shailesh K. Mody, Madhavi M. Awale, et al., “A Comprehensive Review on Pharmacotherapeutics of Herbal Bioenhancers,” The Scientific World Journal, vol. 2012, Article ID 637953, 33 pages, 2012.
 Shaikh J, Ankola DD, Beniwal V, Singh D, Kumar MN. Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer. Eur J Pharm Sci. 2009;37:223–230.
 Patel HM, Ryman BE. The gastrointestinal absorption of liposomally entrapped insulin in normal rats. Biochem Soc Trans. 1977;5:1054–1055.