Elevating Bioavailability of Curcumin via Encapsulation with a Novel Formulation of Artificial Oil Bodies

Abstract

Utilization of curcumin has been limited due to its poor oral bioavailability. Oral bioavailability of hydrophobic compounds might be elevated via encapsulation in artificial seed oil bodies. This study aimed to improve oral bioavailability of curcumin via this encapsulation. Unfortunately, curcumin was indissoluble in various seed oils. A mixed dissolvent formula was used to dissolve curcumin, and the admixture was successfully encapsulated in artificial oil bodies stabilized by recombinant sesame caleosin. The artificial oil bodies of relatively small sizes (150 nm) were stably solidified in the forms of powder and tablet. Oral bioavailability of curcumin with or without encapsulation in artificial oil bodies was assessed in Sprague-Dawley male rats. The results showed that encapsulation of curcumin significantly elevated its bioavailability and provided the highest maximum whole blood concentration (Cmax), 37 ± 28 ng/mL, in the experimental animals 45 ± 17 min (t(max)) after oral administration. Relative bioavailability calculated on the basis of the area under the plasma concentration-time curve (AUC) was increased by 47.7 times when curcumin was encapsulated in the artificial oil bodies. This novel formulation of artificial oil bodies seems to possess great potential to encapsulate hydrophobic drugs for oral administration.

Recent Developments in Delivery, Bioavailability, Absorption and Metabolism of Curcumin: the Golden Pigment from Golden Spice

“…resulted in 1% bioavailability of curcumin in rat plasma [96]. It has been also observed that oral administration of curcumin (1,000 mg/kg) in rats showed 15 ng/mL in blood plasma at 50 minutes [97]. In contrast to rodents, oral dosing of 4-8 g of curcumin in humans showed peak plasma levels of 0.41-1.75 µM after 1 hour of dosing [98].…”

Curcumin and its allied analogues: epigenetic and health perspectives - a review

“…Likewise, Yang et al (2007) determined that curcumin administration (500 mg/kg) showed the 1% bioavailability of curcumin in the plasma of freely moving rats. Similarly, 15 µg/ml curcumin was reported at the blood plasma level at 50 min after oral curcumin administration (1000 mg/ kg) in rats (Chang et al 2013). Moreover, the orally administered curcumin (4-8 g) in humans exhibited the peak plasma levels of 0.41-1.75 µM (Cheng et al 2001).…”

Dietary Phytochemicals as Cancer Preventive Agents: Efficacy and Mechanisms

“…A previous study has found that a maximum serum level of 1.35 ± 0.23 μg/mL is observed at 0.83 h after oral administration of curcumin (2 g/kg) in rats [122]. Other studies show that oral intake of curcumin results in 1% bioavailability in rat plasma [123,124]. In contrast to rodents, 2 g/kg, the same dosing in the study in rats above, of curcumin administered orally to humans leads to extremely low concentrations (0.006 ± 0.005 μg/mL at 1 h) in serum [122].…”