Dr. Richard Clark Kaufman

Many dietary supplements can be virtually useless when swallowed in pills and capsules. Factors such as insolubility, degradation by digestive chemical enzymes, pre-systemic metabolism, poor intestinal absorption or removal by the liver before reaching the blood stream may prevent them from reaching a high enough level for activity. In other words, there could be very little bioavailability and bioactivity after oral ingestion.

Researchers and scientists over the last decade developed a patent-pending NanoSphere delivery system that can produce desirable exposure of nutraceuticals for optimum biological effects. NanoSphere delivery can overcome the absorption problems of other supplements.

NanoSphere gel encapsulates nutraceuticals is a natural nano-sized and solubilized in protective membrane carrier. Made from the same phospholipids that form the membranes around the cells in the human body, NanoSpheres help shield nutraceuticals from dilution and degradation. They are more efficiently transported intact into the circulatory system and target cells.

NanoSpheres are made of the same essential phospholipid that forms the protective membranes around the cells and tissues in your body, phosphatidylcholine. These carriers can be formed with a nano-sized lipoprotein-like structure to help prevent detection and elimination by the body’s immune system and early destruction to extend their circulation time.

Transports Nutraceuticals into the Blood Stream and Target Cells through Mucosa

Transport across intestinal mucosa is a fundamental step for supplement absorption and systemic availability. The mucosa (also known as mucus membrane) is a membrane of skin that lines the alimentary canal cavity from mouth to the intestines. The problem is the intestinal mucosa creates a series of biological barriers for effective and efficient supplement absorption. The contents of typical supplement pills and capsules are restricted entry and often degraded before entering the circulatory system. This significantly reduces their bioavailability and bioactivity.

Why You Need NanoSpheres

When a nutraceutical is given orally, its bioavailability and ultimately its efficacy depend on the solubility and absorption in the gastrointestinal tract. Many dietary supplements have a very low bioavailability and efficacy when taken due to several interacting reasons.

Many popular supplements are comprised of hydrophobic molecules that are not soluble in aqueous solutions. Due to this water-adverse nature they have poor absorption due to slow or incomplete dissolution in the cavity of the gastro-intestinal tract. Examples include the fat-soluble vitamins (A, D, E and K) and minerals. This is especially true of most phytochemicals in plants and botanical extracts.

Phytochemicals and botanical extracts are increasingly accepted as health promoting, maintaining, and repairing agents in cells, tissues, or the whole human body. Phytochemicals are compounds obtained from plants that exert particular health effects. The unique structure and chemical properties of many phytochemicals, including phenolics, carotenoids, organic acids, and saponins and sterols are poorly transported and absorbed into the plasma.

Most supplements are taken in solid form. Pills must first disintegrate and dissolve into a liquid solution in the gut for their ingredients to be absorbed and enter the bloodstream. Unfortunately, many pills don’t disintegrate properly, can’t dissolve and be absorbed.

Bioavailability Means Reaching the Circulation Intact

NanotechnologyThe composition, shape, size and structure of many nutraceuticals limit their absorption from the intestinal tract into the plasma. Furthermore, the dietary supplement may be metabolized and inactivated in the intestinal wall.

Subsequently, the supplement first enters the portal circulation to the liver. Depending on liver functions it may undergo further inactivation and reduction in concentration before reaching the systemic circulation in the process know as “first-pass effects”. As a result, only a small percent of the supplement actually reaches the blood stream intact.

The Problems of Pills and Capsules

Poor Disintegration – To be useful, supplement pills and capsules must first disintegrate (break apart) and dissolve (go into a liquid solution) in a timely manner for their ingredients to be absorbed through the intestines and enter the bloodstream. Pills that don’t disintegrate properly pass through the body unused. A recent study examined seventeen commercially available vitamin and mineral supplements that were sold in pills. The study showed nine (53%) did not disintegrate within 30 minutes.

Low solubility – A significant and increasing number of active ingredients in pills and capsules may have insufficient aqueous solubility and membrane permeability to significantly be absorbed into blood. Supplements with low aqueous solubility / permeability that includes fat soluble vitamins, fatty acids, minerals, amino acids, peptides phytochemicals and herbs are hard to absorb. Even if absorbed slowly, this may contribute substantially lower oral bioavailability.

Potentially Harmful Excipients – Supplement pills and capsules contain excipients (inactive ingredients) binders, dilutents (fillers), lubricants, stabilizers, colorants and a gelatin or vegetable shell (for capsules). Ideally they are inert, which is not always true. Excipients may decrease disintegration, solubility and active ingredients absorption into the bloodstream. They may contain reactive functional groups that interact with the active supplements and cause their degradation, loss of potency and even side effects. Potential unpleasant side effects of excipients include allergic reactions and toxicity.

Swallowing – 40% of the population has a hard time swallowing pills. A recent Harris poll reported individuals find swallowing pills so difficult that many delay, skip, or discontinue taking the pills or capsules completely.

To facilitate swallowing, they mostly drink lots of liquids, drink in big gulps or tilt their heads back. People having problems taking pills described the sensations as having a pill stuck in their throat, a bad after taste or gagging.

This breakthrough technology can overcome the absorption and use problems of other supplements.

References

  1. Bhadoriya S, Mangal A, et al., Bioavailability and bioactivity enhancement of herbal drugs by “Nanotechnology”: a review Journal of Current Pharmaceutical Research 2011; 8 (1): 1-7
  2. Bharali D, Siddiqui I et al., Nanoparticle Delivery of Natural Products in the Prevention and Treatment of Cancers: Current Status and Future Prospects Cancers 2011, 3, 4024-4045;
  3. Charman, WN.,Lipids, lipophilic drugs, and oral drug delivery—some emerging concepts. J. Pharm. Sci. 2000 89 (8), 967–978.
  4. Dhiman A, Nanda A, et al., Novel Herbal Drug Delivery System (NHDDS): the need of Hour International Conference on Environment, Chemistry and Biology 2012 vol 49 171-175
  5. Drug Delivery to the Oral Cavity: Molecules to Market Tapash K. Ghosh (Editor) Taylor & Francis 2005
  6. Engham H. Intestinal Barriers to Oral Drug Absorption: Cytochrome P450 3A and ABC-transport Proteins.. Acta Universitatis Upsaliensis, 2003
  7. Epriliati I, Ginjom I. Bioavailability of Phytochemicals, Phytochemicals — A Global Perspective of Their Role in Nutrition and Health, Dr. Venketeshwer Rao (Ed.) 2012,
  8. Harris Survey between May 27 and June 4 2003
  9. Hoskins C, Wooei PC, Implementing Nanotechnology and Novel Drug Delivery Systems to Improve Dissolution and Solubilization, American Pharmaceutical Review 2012
  10. Huang Q, Yu H, et al., Bioavailability and delivery of nutraceuticals using nanotechnology. Journal Of Food Science Vol. 75, Nr. 1, 2010 50-57
  11. International Excipients Certification Project: minimize risks – maximize benefits. London: Pharmaceutical Quality Group; 2009.
  12. Islam S, Sameem M. Influence of nanotechnology on herbal drugs: A Review Journal of Advanced Pharmaceutical Technology & Research Jul-Sep 2012 142-146

*These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure or prevent any disease.