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NanoScience and Nutraceuticals
The New Nutrition
"...four of the defining technologies of the 21st century will be nanotechnology, biotechnology, information technology, and environmental science...the potential both for improving the quality and increasing the length of life has never been greater." - Malcom Gillis, President, Rice University.
"If I were asked for an area of science and engineering that will most likely produce the breakthroughs of tomorrow, I would point to nanoscale science and engineering." - Neal Lane, Assistant to President George Bush, Science and Technology
"By 2010, half of all drugs will be made with nanotecnology..."- The National Science Foundation
"If I were just setting out today to make that drive to the West Coast to start a new business, I would be looking at biotechnology and nanotechnology."-- Jeff Bezos, Founder of Amazon.com
So what is NanoScience?
A nanometer is one billionth of a meter, one millionth of a millimeter, or one thousandth of a micron. Therefore it is typically accepted that nanoscience involves the manufacture and manipulation of molecules from 0.1-200 nanometers in size! Specifically, nanotechnology is the development of methods for fabrication, synthesis and characterization of materials at the nanometer scale.
Glenn McGee, associate director of the University of Pennsylvania's Center for Bioethics states, "the two fundamentally different approaches to nanotechnology are graphically termed 'top down' and 'bottom up'. 'Top-down' (AKA incremental) refers to making nano-scale structures by machining and etching techniques, whereas 'bottom-up' ( AKA evolutionary) ...applies to building organic and inorganic structures ...molecule-by-molecule. Top-down or bottom-up is a measure of the level of advancement of nanotechnology. Most nanotechnology, as applied today, is still in the main at what may be considered the more primitive 'top-down' stage."(1
Nonetheless, primitive may be too humble a description! Indeed a whole burgeoning industry of "Nano-bio-technology", as an interface technology integrating elements of both nanotechnology and biotechnology, has set the stage for establishing methods by which physiologically harmless and biocompatible materials can be made applicable to biology, medicine, cosmetics and the food sector. (2
Hielcher, a German nanotech company writes in its web site"...the reduction of primary particles into micron and submicron range (nano-powders) is required in many processes in the pharmaceutical (and) chemical...industries...nano-scale particles, such as biodegradable micro-spheres and nano-spheres, are very potent drug and antigen delivery systems ...micron-size and nano-size materials down to the size of several nanometers are favored for many applications due to their large surface area. (3
In March 2004 Dow Chemical renewed a collaboration with the University of Texas at Austin developing nanotechnologies to improve the solubility and bioavailability of often poorly bio-available drugs. Their BioAqueous Solubilisation Services focuses on altering the particle size, surface area, or morphology of drugs to create nano-structured particles that can improve their ability to dissolve in the body. These processes produce extremely fine, readily absorbed particles - with a high surface area and good 'wetability'. (4
Dow's states that its Solubilization Solutions can help pharmaceutical companies increase bio-availability and dissolution rate, improve onset of activity, reduce variability, and /or decrease dose size.(5
Shakil A. Saghir, M.S.P.H., Ph.D. Senior Research Toxicologist at the Dow Chemical Co. in a Pham PK discussion group writes,"...we are running bio-availability studies for some of the old drugs... just by...nano-sizing and comparing different nano-sizing methods with original micro-sized formulations... We are not only seeing higher (plasma) AUC for nano-sized drug... but also for (each) method of nano-sizing." (6
The use of a nano-emulsion to deliver either recombinant proteins or inactivated organisms to a mucosal surface to produce an immune response has been demonstrated at the University of Michigan, School of Medicine. The results indicate the basis of a platform vaccine delivery system. The first applications, an influenza vaccine and an HIV vaccine, can now proceed to clinical trials. (7
Quite naturally, there has been keen interest in processing nutraceuticals in nano-sized particles. One such nutraceutical is Co-Q10, of interest because of both its expense and poor absorbability. An article in The New Zealand Medical Journal compared the bioavailability of seven different Coenzyme Q10 brands. There were significant differences in bioavailability between the seven brands tested. Of note here is that the "winner" was formulated via a patented process which reduces the Coenzyme Q10 particles to the nano-range and renders them hydro-soluble as well as lipo-soluble. (8
One of the participants involved stated,"what makes (our C0 Q-10) so powerful is the fact that we have simply made the CoQ10 particles very small (sub-micron size) so that they seem to go into solution in water. The large surface area afforded by the smaller particle size facilitates much greater absorption in the gut." (9
The "NanoTech Wire" announced clinical studies carried out in human subjects at the Weitzman Institute in Israel which compared the relative bioavailability of yet another CoQ10, processed with a different nanotechnology, with other currently available dosage forms. The results demonstrated the CoQ10 processed through "nano-emulsion" technology was vastly superior, resulting in a free flowing powder with a 100% dissolution rate and exhibiting a six-fold increase in plasma CoQ10 values over baseline and several-fold greater relative bioavailability over other dosage forms tested! (10
There are many other nutraceuticals that are poorly absorbed, such as Vit BV12, Vit K2, Vit E many phytonutrients, especially the polyphenols and terpenes, the latter of which includes the carotenoids, chromonols, limonoids and saponins. (Actually, if discovered today, vitamin K complex and vitamin E complex would not be classified as vitamins but as phytochemicals, as a subclass of the terpenes called the chromanols, namely the phyloquinones and tocopherols / tocotrionols, respectively, along with Co Q10.) (11
Maximizing bioavailability of phytonutrients is of vital importance today. To quote Jean Mayer of the USDA Human Nutrition Research Center on Aging, Tufts University, Boston, MA "...the effort to understand the health benefits of plant foods... is the characterization of their physiologically active constituents, the phytochemicals...As our knowledge grows...we will learn how best to create new products through altering their concentrations, combinations and/or their bioavailability." (12
The importance of delivery systems when formulating nutraceuticals is further underlined in the Journal of Drug Targeting, "...antioxidants, which are found in many phytochemicals,... are biologically unstable, poorly soluble in water, and poorly distributed to target sites... we strongly advocate serious consideration of the bioavailability of dietary supplements... to improve their bioavailability using delivery systems such as liposomal formulations." (13 Liposomal delivery systems have been safely employed for many decades. Indeed, Dr Brain Keller, Executive VP of a California based company that creates, "technologies that enhance the performance and delivery of active ingredients" has patented a "bottom up" evolutionary nano-bio-technology that gently encapsulates poorly absorbed nutrients and nutraceuticals in nanosized multilayered lipid vesicles that, when ingested, are selectively taken up by enterocytes in the small intestine, bypassing portal circulation! (14. Safely used in FDA approved pharmaceuticals and cosmetics for years, BioPharma has garnered the exclusive rights to this natural liposomal technology under the registered trademark NanoSorb®.
Therefore health professionals who recommend nutraceuticals to their clients may well desire to stay informed as relates to recent advances and in nano-bio-delivery technologies. How new all this is may be best demonstrated by the fact that most of my footnotes are from the web! Nonetheless, such enhanced bioavailability thru nanotechnology, when proven, not merely hyped, may well lead to greater efficacy, smaller dosing, with resultant long sought for effects on economy, compliance, and clinical efficacy.
John H Maher, DC, DCCN, FAAIM
1. http://www.nano.org.uk/nano.htm
2. NanoBioNet - The Center of Excellence of Nanobiotechnology http://www.nanobionet.de/eng.htm
3. http://www.hielscher.com/ultrasonics/nano_01.htm
4. http://www.in-pharmatechnologist.com/news/news-ng.asp?n=55824-dow-extends-ut&ip=1
5. http://www.dow.com/bioaqua/res/press/20021111b.htm
6. PharmPK Discussion - Human bioavailability values, PharmPK Discussion List Archive Index http://www.boomer.org/pkin/PK02/PK2002157.html
7. http://www.nanobio.com/vaccine.html
8. New Zealand Medical Journal, The bioavailability of coenzyme Q10 supplements available in New Zealand differs markedly, October 8, 2004 Vol 117 No 1203 ( The study was approved by the Canterbury Ethics Committee, per The Ministry of Health of New Zealand and was completed November 2003 thru January 2004.)
9. http://www.epic4health.com/biofcoq10sua.html
10. http://nanotechwire.com/news.asp?nid=874&ntid=117&pg=2
11. Maher, J, Physiological Functions of Phytonutrients, A Brief Introduction, Dynamic Chiropractic, July 2003 http://www.chiroweb.com/archives/21/16/11.html
12. Mayer, J, -Functional Foods for Health Program, USDA Human Nutrition Research Center on Aging, Tufts University, Boston, MA
13. Yoko Shojia,b, and Hideki Nakashimaa, Nutraceutics and Delivery Systems, Journal of Drug Targeting, 12(6):385-391, 2004
14. Personal communication
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