Enhanced absorption of curcuminoids and 3-Acetyl-11-keto-β-boswellic acid from fenugreek galactomannan hydrogel beadlets: A natural approach to the co-delivery of lipophilic phytonutrients
2021
Abhilash, Maliakkal Balakrishnan | Kumar, Dinesh | Deepti, Ayswaria | Nair, Aswathi | Greet, Vanheule | An-Katrien, Vynckier | Mieke, Van Den Driessche | Das Sivadasan, Syam | Maliakel, Balu | Chakrapani PS, Baby | Illathu Madhavamenon, Krishnakumar
Simultaneous oral delivery of bioactive molecules with enhanced bioavailability is of great significance, especially when delivered from single beadlets. Here, we report the formulation, characterization, and pharmacokinetic properties of two poorly bioavailable lipophilic phytonutrients with synergistic effects, curcuminoids and 3-Acetyl-11-keto-β-boswellic acid (AKBA), following their co-delivery using fenugreek dietary fiber (Galactomannans)-based hydrogel beadlets (CGM-BSW). These beadlets are capable of extensive swelling and sustained-release of self-emulsified colloidal particles (150 – 200 nm) containing curcuminoids and AKBA allowing for improved absorption. The results of our double-blinded 4-way crossover, 4-sequence study (n = 14) demonstrated that a single dose of 250 mg of these beadlets enhanced the absorption of unconjugated curcuminoids (24.8-fold) and AKBA (6.9-fold) compared to their unformulated counterparts. The absorption of CGM-BSW formulated curcuminoids was also 5.6-fold higher than that of those formulated with turmerones (UCT). UPLC-ESI-QQQ-MS/MS was used to quantify both the curcuminoids and AKBA concentration in the plasma samples and this data was used to determine their pharmacokinetic characteristics.
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