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

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AMINO ACIDS-PEGYLATED CoQ10 ADDUCTS CONTROLLED RELEASE BEHAVIOUR AND

ANTIOXIDANT ACTIVITY EVALUATION

Zacchigna M.a, Cateni F.aand Procida G.a

aDepartment of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy

INTRODUCTION

Polyethylene glycol (PEG, HO-(CH2CH2O)n-CH2CH2OH) is a polyether polymer easily available at low cost, soluble in both water and organic solvents and

biocompatible. PEG is used as inert polymeric support in organic synthesis, as conjugating agent of bioactive molecules of pharmacological interest and its use is approved by FDA1.

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 resistance2. In recent years nutraceuticals constituted by branched chain amino acids (Branch Chain Amino

Acids, BCCA) have found increasing use as anti-fatigue active elements. 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.

1. Pasut, G., Veronese, F.M., State of the art in PEGylation: The great versatility achieved after forty years of research. J. Control. Rel. 2012,161, 461–472. 2. Novellino, E., Iadevaia V., Alimenti e nutraceutica; Edizioni Punto Effe Srl: Milano, 2012; pp. 75-78.

RESULTS

The aim of the present conjugation is to obtain an amphiphilic soluble mixed conjugates.

Pharmacokinetic studies in vitro show that the adducts deliver the corresponding beneficals amino acids together with ubiquinol giving a good antioxidant action.

Study in vitro

Synthesis of

mPEG-amino acids

The hydrolytic stability of the mPEG-conjugates was evaluated in mouse plasma

Release of CoQ10 from in plasma from adducts (mediated by esterase and amydase enzymes) at 37C (blu: mPEG-BCAA-CoQ10, red mPEG-CoQ10)

SAMPLE PREPARATION

Plasma + mobile phase + FeCl30.1%

Vortex Centrifugation

Filtration (Millex-LH 0.22μm)

ANALYSIS

Mobile phase: H2O, ACN, THF

5: 55: 40 (v/v) Column : RP C18 Gemini, 25 x 4 mm, 5μm, Supelco Flow: 1 ml/min λ: 275nm HPLC 0 5 10 15 20 25 0 20 40 60 80 100 % r e le a s e Time (h)

Synthetic route of mPEG-

amino acid-

CoQ10

conjugates

DPPH scavenging ability of CoQ10 when the assay was carried out in different samples of adducts

The scavenging activity is the some for standard CoQ10 and CoQ10 released from the adducts by enzymatic reactions in plasma. The scavenging activity was absent in the all adducts but gradually increases on the basis of drug delivery. mPEG-CoQ10 adducts does not present activity, because the phenolic group in eugenol is engaged in polymer bond

Riferimenti

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