García-González, AídaEspinosa-Cabello, Juan ManuelCerrillo, IsabelMontero-Romero, EmilioRivas-Melo, Juan JoséRomero-Báez, AndreaJiménez-Andreu, María DoloresRuíz-Trillo, Carmen AmeliaRodríguez-Rodríguez, AnaMartínez-Ortega, Antonio JesúsRoque-Cuellar, María Del CarmenGarcía-Rey, SilviaJiménez-Sánchez, AndrésMangas-Cruz, Miguel ÁngelPereira-Cunill, José LuisPerona, Javier S.García-Luna, Pedro PabloCastellano, José María2025-01-172025-01-17202310.1039/d3fo02725bhttps://hdl.handle.net/10433/22435R+D+i project PID2019- 107837RB-I00, funded by the Spanish Ministry of Science and Innovation/Spanish National Research Agency, grant number MCIN/AEI/10.13039/501100011033/Evidence of the pharmacological activity of oleanolic acid (OA) suggests its potential therapeutic application. However, its use in functional foods, dietary supplements, or nutraceuticals is hindered by limited human bioavailability studies. The BIO-OLTRAD trial is a double-blind, randomized controlled study with 22 participants that received a single dose of 30 mg OA formulated as a functional olive oil. The study revealed that the maximum serum concentration of OA ranged from 500 to 600 ng mL−1, with an AUC0−∞ value of 2862.50 ± 174.50 ng h mL−1. Furthermore, we discovered a physiological association of OA with serum albumin and triglyceride-rich lipoproteins (TRL). UV absorption spectra showed conformational changes in serum albumin due to the formation of an adduct with OA. Additionally, we demonstrated that TRL incorporate OA, reaching a maximum concentration of 140 ng mL−1 after 2–4 hours. We conjecture that both are efficient carriers to reach target tissues and to yield high bioavailability.application/pdfenAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/Oleanolic acidBioavailabilityOlive oiljournal articleopen access