Encapsulation of sesamol in phosphatidyl choline micelles: Enhanced bioavailability and anti-inflammatory activity.

Sesamol, the phenolic degradation product of sesamolin, although recognised for its anti-inflammatory
effects, has low bioavailability. In this manuscript, we attempted to improve its bioavailability by encapsulation
in mixed phosphatidylcholine micelles. Sesamol could be solubilised and entrapped in phosphatidylcholine
mixed micelles (PCS) with 96.8% efficiency (particle size 3.0 ± 0.06 nm). Fluorescence
spectra of PCS revealed lower relative fluorescence intensity (RFI 112) compared to ‘free’ sesamol (FS)
(RFI 271). The bioaccessibility, transport across a monolayer of cells and cellular uptake of PCS was
8.58%, 1.5-fold and 1.2-fold better, respectively, compared to FS. The anti-inflammatory effects of FS
and PCS were compared using LPS treated RAW 264.7 cell line and lipoxygenase inhibition. PCS effected
downregulation of iNOS protein expression (27%), NO production (20%), ROS (32%) and lipoxygenase inhibition
(IC50 = 31.24 lM) compared to FS.