Bioavailability of Epigallocatechin Gallate Administered with Different Nutritional Strategies in Healthy Volunteers
Por:
Fernández VA, Almeida-Toledano L, Pizarro Lozano N, Tapia EN, Gómez-Roig MD, De la Torre Fornell R and García Algar Ó
Publicada:
1 may 2020
Ahead of Print:
19 may 2020
Resumen:
The flavanol epigallocatechin gallate (EGCG) is being tested for the treatment of several diseases in humans. However, its bioavailability and pharmacokinetic profile needs a better understanding to enable its use in clinical trials. There is no consensus on the most appropriate concentration of EGCG in the body to obtain the maximum therapeutic effects. Therefore, the aim of this study is to analyze the bioavailability of EGCG orally administered alone or with different food supplements after overnight fasting in order to determine its optimal conditions (high concentrations in blood and the lowest interindividual variations) to be used as a pharmacological tool in human trials. Ten healthy volunteers (5 men and 5 women) aged 25 to 35 years were recruited prospectively. Three series of clinical experiments with a washout period of seven days among each were performed: (1) Teavigo((R)) (EGCG extract) alone, (2) Teavigo((R)) with a standard breakfast, and (3) FontUp((R)) (Teavigo((R)) commercially prepared with fats, carbohydrates, proteins, vitamins, and minerals). Blood samples were collected at 0, 30, 60, 90, 120, 180, 240, and 360 min after EGCG intake. Free EGCG in plasma was measured using a liquid chromatography and mass spectrometry UPLC-ESI-MS/MS analytical method. The pharmacokinetic variables analyzed statistically were area under the curve (AUC(0-360)), C-max, C-av, C-min, T-1/2, and T-max. EGCG (Teavigo((R))) alone was the group with higher AUC(0-360,) C-max, and C-av both in men (3.86 +/- 4.11 mu g/mL/kg/6 h; 5.95 ng/mL/kg; 2.96 ng/mL/kg) and women (3.33 +/- 1.08 mu g/mL/kg/6 h; 6.66 ng/mL/kg; 3.66 ng/mL). Moreover, FontUp((R)) was the group with the highest value of T-1/2 both in men (192 +/- 66 min) and women (133 +/- 28 min). Teavigo((R)) intake after fasting overnight revealed the highest concentration of EGCG in plasma according to its pharmacokinetic profile, indicating that this is an excellent alternative of administration if the experimental design requires good absorption in the gastrointestinal tract. Moreover, EGCG taken along with food supplements (FontUp((R))) improved the stability of the molecule in the body, being the best choice if the experimental design wants to reduce interindividual variation.
Filiaciones:
Fernández VA:
Grup de Recerca Infancia i Entorn (GRIE), Institut d'investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), 08036 Barcelona, Spain
Valencian International University (VIU), 46002 Valencia, Spain
Institut de Recerca Sant Joan de Déu (IR-SJD), 08950 Barcelona, Spain
Maternal and Child Health and Development Network II (SAMID II), Instituto de Salud Carlos III (ISCIII), 28029 Madrid, Spain
Almeida-Toledano L:
Institut de Recerca Sant Joan de Déu (IR-SJD), 08950 Barcelona, Spain
Maternal and Child Health and Development Network II (SAMID II), Instituto de Salud Carlos III (ISCIII), 28029 Madrid, Spain
BCNatal - Barcelona Center for Maternal Fetal and Neonatal Medicine, Hospital Sant Joan de Déu, 08950, Esplugues de Llobregat, Barcelona, Spain
Pizarro Lozano N:
Integrative Pharmacology and Systems Neurosciences Research Group, IMIM-Hospital del Mar Medical Research Institute, 08003 Barcelona, Spain
Autonomous University of Barcelona, 08193 Bellaterra, Spain
Tapia EN:
Grup de Recerca Infancia i Entorn (GRIE), Institut d'investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), 08036 Barcelona, Spain
Institut de Recerca Sant Joan de Déu (IR-SJD), 08950 Barcelona, Spain
Maternal and Child Health and Development Network II (SAMID II), Instituto de Salud Carlos III (ISCIII), 28029 Madrid, Spain
Gómez-Roig MD:
Institut de Recerca Sant Joan de Déu (IR-SJD), 08950 Barcelona, Spain
Maternal and Child Health and Development Network II (SAMID II), Instituto de Salud Carlos III (ISCIII), 28029 Madrid, Spain
BCNatal - Barcelona Center for Maternal Fetal and Neonatal Medicine, Hospital Sant Joan de Déu, 08950, Esplugues de Llobregat, Barcelona, Spain
De la Torre Fornell R:
Integrative Pharmacology and Systems Neurosciences Research Group, IMIM-Hospital del Mar Medical Research Institute, 08003 Barcelona, Spain
CIBER of Physiopathology of Obesity and Nutrition (CIBEROBN), University Pompeu Fabra (CEXS-UPF), 08002 Barcelona, Spain
García Algar Ó:
Grup de Recerca Infancia i Entorn (GRIE), Institut d'investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), 08036 Barcelona, Spain
Maternal and Child Health and Development Network II (SAMID II), Instituto de Salud Carlos III (ISCIII), 28029 Madrid, Spain
Department of Neonatology, Hospital Clínic-Maternitat, ICGON, IDIBAPS, BCNatal, 08028 Barcelona, Spain
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