Novel Biphasic In Vitro Dissolution Method Correctly Predicts the Oral Bioavailability of Curcumin in Humans

• Published in: Journal of agricultural and food chemistry Vol. 71; no. 42; pp. 15632 - 15643
• Main Authors: Brenner, Marvin Benedikt, Flory, Sandra, Wüst, Matthias, Frank, Jan, Wagner, Karl
• Format: Journal Article
• Language: English
• Published: American Chemical Society 25.10.2023
• Subjects: Bioactive Constituents, Metabolites, and Functions; bioavailability; curcumin; food chemistry; humans; pharmacokinetics; pharmacokinetics; in vitro–in vivo relationship; biphasic dissolution; bioavailability; curcumin formulations
• ISSN: 0021-8561; 1520-5118; 1520-5118
• DOI: 10.1021/acs.jafc.3c04990

In vitro dissolution methods correctly predicting in vivo bioavailability of compounds from complex mixtures are lacking. We therefore used data on the in vivo performance of bioavailability-improved curcumin formulations to implement an in vivo predictive dissolution method (BiPHa+). BiPHa+ was applied for the characterization of eight curcumin formulations previously studied in a strictly controlled pharmacokinetic human trial. During dissolution, the dissolved proportion of curcumin in the aqueous medium underwent a formulation-dependent reduction, whereas the proportion remained stable in the organic layer. Compared with conventional dissolution systems, BiPHa+ was superior in terms of in vivo-relevant formulation characterization. All formulations could be precisely categorized according to their bioavailability in humans. In vitro–in vivo relationships for each dissolution method were established, with BiPHa+ providing the highest degree of linearity (r 2 = 0.9975). The BiPHa+ assay correctly predicted the bioavailability of curcuminoids from complex mixtures and provided mechanistic information about formulation-dependent release characteristics.