Dose Delivery, Old & New

Imagine a zinc supplement tablet emulsified in a proprietary mixture of plant lipids, beeswax, and starch to optimize absorption. Sounds modern and scientific, right? Actually, this supplement is 2,000 years old, the oldest ever discovered, just recently found in a shipwreck off the coast of Italy.

Yes, dose delivery sciences (and pirates) is nearly as old as medicine itself. It makes sense to dissolve water-soluble actives in water, and fat-soluble actives in fats, in order to improve their dispersion and assimilation into the body. However, our gut is designed to neutralize, degrade, and digest anything we put in it. If it’s not a fat, protein, or carbohydrate, chances are that the gut and the liver will do their best to excrete what we consume through feces as well as urine, breath and, sweat.

There are 101 “enhanced absorption” technologies offered in the supplement industry today, and nearly all of the credible ones were first introduced in the pharmaceutical industry. In fact, PubMed lists more than 154,000 studies for "drug delivery." Nearly all of these studies were tested in test tube or animal models; only about 10 percent of these studies are in humans. Remove intravenous, transdermal, subcutaneous, buccal, and other modes of delivery, leaving only oral dosage studies – and relatively few pharmaceutical innovations remain proven in humans.  

These numbers suggest the ease with which test-tube proof can be achieved, and how difficult it can be to prove human absorption and efficacy.  

Meanwhile, the supplement field is awash in enhanced delivery forms inspired by pharmaceutical science and PubMed abstracts. While many supplement ingredients and products leveraging the technological advances hold promise, many remain relatively unproven on the level of human efficacy.  

Assuming improved human bioavailability can be proven using appropriate methodologies and metabolites, through appropriate blood compartments at meaningful intervals with replicable results, what do the results "10x higher bioavailability" actually mean for the health of the consumer? This paradigm assumes that correlation between dose and human efficacy is direct and linear, but what if more is not better?

While bioavailability may be a path to easily accessible claims that consumers understand, the end goal is improving health in a measurable and predictable way. The standard will always be well-designed, controlled clinical trials and long-term dosing safety trials; bioavailability is simply a small but important means to the ultimate end of supporting consumer health.  

After all, the shipwrecked supplementers were looking for a noticeable effect on their health, not some abstract benefit like “10x.” Why should the goals of today’s consumers be any different?