When food meets pharma – the future?

Posted on: 30th November 2019
Author: Dr Marcia Philbin, Chief Executive, FPM

Some time ago I attended an interesting lecture at the Royal Society of Chemistry which considered how food can be used to develop new medicines. As the new Chief Executive at FPM, I thought I would share my summary of this fascinating area.

The lecture was given by John Gleeson who was completing the final year of his PhD based in the School of Veterinary Medicine at University College Dublin. His lecture focused on the rise in the design and use of nutraceuticals which are bioactive compounds isolated from food which provide a physiological benefit beyond basic nutrition. The work was being undertaken as a response to the rise in lifestyle associated diseases such as Type 2 diabetes, obesity and cardiovascular disease and the urgent need to prevent the onset of these conditions.

The use of food to develop medical treatments is not new, e.g. penicillin was developed from bread mould, aspirin is based on salicylates which can be found in things like apples, grapefruit, spinach etc. The techniques that are now becoming available have enabled scientists to look at designing bespoke molecules that will treat specific conditions.

There are four groups of nutraceuticals:

Table 1: The four groups of nutraceuticals
Fatty Acids Fish oil, omega 3 capsules EPA, DHA Brain development, anti-inflammatory We do not consume enough fats
Bioactive peptides Milk, chicken muscle, fish muscle, seaweed Peptide chains Lower blood pressure and inflammation Peptides are broken down in digestive system
Micronutrients Various sources Iron, Calcium, Vitamin D, Vitamin B, Selenium Selenium needed for sperm generation Not consuming enough
Phytochemicals From plants Curcumin (red wine), turmeric, carotene (vitamin A) Numerous Not consuming enough

Nutraceuticals have been developed to aid the delivery of bioactive ingredients into the bloodstream whilst navigating the body’s natural chemical processes:

Table 2
Bioaccessibility / Solubility If something is soluble in water, then is absorption into the bloodstream is hindered by too much fat and alcohol in the gut Fatty acids are fat soluble and do not readily permeate intestinal wall
Degradation Food degradation starts in the mouth and continues as it journeys through the gut
Permeability Many things stop the permeation of key products to cross the intestinal wall into blood stream

Nanoparticles have therefore been developed as nanodelivery vehicles to transport bioactive ingredients through the body.

  1. Nanoemulsions are solid lipid nanoparticles and usually derived from eggs.
  2. Polyeletrolytes are waterbase hydrogels (i.e. polymer).

Examples of uses of nutraceuticals include the following:

Coenyzme Q10 is needed by cells to make energy and is important particularly for liver, heart and kidneys as they are the powerhouses of the body. It is sold as a health supplement in the form of a pill, but data show that only a tiny fraction gets into the blood stream. When Coenzyme A is put in a nanoemulsion, 30 x more is delivered into the bloodstream compared to what is delivered via supplements.

Reseveratol is derived from urine and is a good anti-inflammatory agent which has been shown to reduce the rate of colorectal cancer. It is not soluble in water or fat but solubilises in ethanol. When put into a nanoparticle based on corn protein, there is a huge increase in the volume that goes into the bloodstream compared to the usual mode of administration by ordinary pill.

EGCG is another anti-inflammatory agent that is found in green tea. Data shows that EGCG taken in the form of green tea does not provide the benefit as claimed by suppliers. To derive the benefit, one would be better to eats lots of green tea leaves. Green tea is green due to having lots of conjugation in the molecular structure (i.e. C= C double bonds) and it is this which is responsible for its bioactivity. Low grade inflammation leads to pre-diabetes (type2) and pre-obesity and ECGC has been found to halt the onset of these conditions. ECGC is water soluble and has been encased in a nanoparticle based on a long sugar found in crab shell. This sugar enables the slow release of EGCG direct into the blood stream and this has been shown to reduce the inflammation leading to pre-diabetes and pre-obesity. This treatment is not suitable for Type 1 diabetes if a patient has been born with it. The treatment is applicable to preventing the onset of diseases.

In summary, the design of nutraceuticals to combat disease is a growing and fascinating field. Many claims about the benefits of green tea and red wine are true to a point. However, it needs to be understood that unless the active ingredient can be dispensed into the right place in the body, then the benefits will not be realised.

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