AMINO ACIDS-PEGYLATED UBIQUINOL ADDUCTS CONTROLLED RELEASE BEHAVIOUR AND ANTIOXIDANT ACTIVITY EVALUATION

The term nutraceutical can be applied to any food or active principle able to determine positive effects on health, including any preventive effect and treatment of diseases. One of the areas of most interest involves the use of nutraceuticals in cardiovascular prevention. The ubiquinol (UBI), also considered the CoQ10 of next generation, is a raw material for food supplements with antioxidant activity; it plays a key role in energy production and in increasing body resistance1. In recent years nutraceuticals constituted by branched chain amino acids (Branch Chain Amino Acids, BCCA) have found increasing use as anti-fatigue active elements1. The muscle can directly use the BCAA for protein synthesis (plastic function) can also for gluconeogenesis (energy function). The main objective of this work is to increase the water solubility and the ubiquinol stability through chemical modifications with polyethylene glycol (PEG) using spacer arms, consisting of specific amino acids, alanine, valine, isoleucine and leucine. The polyethylene glycol (PEG) is a synthetic polymer approved by the Food and Drug Administration, highly water-soluble, biocompatible, non-teratogenic, non-immunogenic, antigenic and non-toxic, easily eliminated from the human body and widely used in drug delivery system2. Conjugates PEG-BCAA-UBI should have a possible synergistic action in energy production in muscles. The synergistic action could be extremely interesting when applied, particularly, to the heart muscle. The carboxylate polymer is the starting building block for the preparation of mPEG-UBI, mPEG-Ala-UBI and mPEG-BCAA-UBI. Pharmacokinetic studies show that the adducts deliver the corresponding beneficals amino acids together with ubiquinol giving a good antioxidant action.