Creatine ethyl ester, is the latest breakthrough in creatine delivery technology, it is by far the most bioavailable form of creatine and totally negates the need for large dosing protocols. But many people are asking what is an ester and how does it improve the delivery of creatine?
An ester is a chemical compound that is formed by the reaction of an organic or inorganic acid with an alcohol or with another organic compound containing the hydroxyl (-OH) radical. The reaction involves replacement of the hydrogen of the acid with a hydrocarbon group. The name of the ester indicates its derivation; e.g., the ester resulting from the reaction of ethyl alcohol and ascetic acid is called ethyl acetate.
Esters are used in the formulation of numerous Pro-Drugs, -drugs which have been chemically modified to improve their delivery and stability. This modification involves the bonding of a “delivery molecule” (e.g. an ester) to a substance that cannot penetrate the lipid (fat) cellular membranes. Once the substance has successfully reached the target tissues intact, the ester is hydrolyzed by esterases, leaving the parent drug to be released over a sustained period of time. By varying the ratio of water solubility to fat solubility within the ester, it is possible to influence the rate of release.
Ironically, creatine is a water-based molecule that is not very water soluble. On top of this, once it comes into contact with any liquid, creatine monohydrate loses its hydrogen part and becomes a zwitterion (negatively charged on one end, positively on the other). The problem here is that water-based zwitterions cannot penetrate muscle cell membranes that are made up of lipids (fat). Thus, this zwitterion (creatine) is forced to use creatine transporters. However, compared to the amount of creatine that needs transporting, there are only a limited number of transporters. Thus, while waiting in line, most of these creatine molecules rapidly start decomposing into inert creatinine. Also, because they wait in the space outside muscle cells (extra-cellular spaces), they pull water with them and cause edema, -that puffy look that many experience from creatine use. Worse still, over an extended period of use, this forces the transporters that allow creatine to enter muscle cells to shut down.
By bonding an ester to the creatine molecule, these inherent problems are side-stepped. In this case, esterification masks the negatively charged portion of the zwitterion, allowing the creatine ethyl ester to bypass creatine transporters and gain direct access to the bloodstream and muscle cells. Once this unique form of creatine enters the muscle cell, the ethyl ester is cleaved off by the estrases, leaving creatine in its salt form. The net result is that water is pulled inside the muscle cells, creating a bona-fide and dramatic cell-volumizing effect.
Recent research by the University of Nebraska indicates that by giving creatine this powerful lipophilic (fat-penetrating) property, not only is bioavailability increased by nearly 4000%, but numerous other benefits not normally achieved through oral supplementation may be realized.
Pro-Creatine E2 is the new creatine ester product from CNP, it is set to take the British creatine market by storm. It makes creatine an option for those who may suffer adverse effects (stomach discomfort, bloating, cramp, etc) from large doses of creatine monohydrate. Now all athletes can reap the benefits of creatine supplementation with none of the negatives.
