The vectorization of nutraceutical actives

Formulating with the best actives, produced under the best conditions, is useless if the formulation is not absorbed nor correctly used by the body. Improving actives delivery efficiency is therefore a perfect optimization leverage which is both technical and economical as far as innovation is concerned.

There are various encapsulation techniques. They encompass quite various aspects. Indeed, the assimilation of an active passes through several stages.

First of all, it is necessary to make sure that the active actually gets to the “entry gate” of the body – namely as the enterocytes in the wall of the digestive tube – in good condition: neither oxidized, nor degraded by the acid pH in the stomach, for instance. The encapsulation techniques used based on gums, alginates, yeasts etc. are the ones that play the first physical protection role for the encapsulated active.

Second stage: the active must then pass through this entry gate. An active’s bioavailability is defined by its capacity of doing so. This is why an active must be sufficiently shrinked to allow it to cross this barrier. Techniques, such as cyclodextrins, are used to allow an increase of the solubility of non-hydrosoluble actives, as well as liposome/phytosome complexes derived from phospholipids, which are also going to serve as vehicles by merging with the enterocytes’s wall. Also it is necessary to mention the micelles technology (patented by Aquanova).

Finally, the third and last stage: once this gate is passed through, the active arrives in the lymphatic system – which is not yet the final destination. It is again necessary to make sure that the active will be used for its intended purpose… Please note that another barrier must be crossed, possibly more selective than the intestinal wall: the blood-brain barrier, which isolates the brain from the rest of the body. This barrier is also composed of phospholipids… Long is the road before an active is delivered to the right location.

The concept of vectorization, as such, has been used for a few years now in cosmetics and nutrition, including for phospholipids.

Phospholipids have a triple interest for vectorization. They have an amphiphilic character and they are naturally involved in the emulsion of molecules in the bowel as they form micelles. They are also an essential element of the enterocyte membranes and are able to merge with them while also delivering the active they are carrying.

Their third interest, that has not been explored yet, is that, in some cases, they can act themselves as actives. They actually play an essential role in a wide number of metabolic processes. It is therefore possible, if the types of phospholipids used for the active’s vectorization is well choosed, to exert the synergetic activity of the encapsulated active and its vehicle.

By using marine phospholipids for the vectorization of an active targeting “memory”, it is possible not only to optimize the bioavailability of the active subject to vectorization, but also to provide, via the same phospholipids, the phosphatidylcholine involved in the transmission of the nervous message, as well as DHA – which is, moreover, in its most effective form for the body.

Using and putting forward this “synergetic” dimension of the vector and the active it delivers, is a novelty no one has previously considered. But it also implies a good knowledge of phospholipids, whose diversity does not end with soy lecithin.

A new breathe

The interest of the vectorization’s concept lies in the possibility of a new breathe for the “aging” or little used actives due to their low natural bioactivity by optimizing their efficacy.

It opens up a wide array of possibilities in terms of innovation both for the active ingredients manufacturers and the formulators. Moreover it opens the door to a “sustainable” use of resources: a more efficient active can be more precisely dosed. Its value could shift from “quantitative” to “qualitative”…

Source : Novastell

Philippe Millet

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