Reconstituted HDL containing apolipoprotein E3 is a potential 'nanovehicle' for transport and targeted delivery of bioflavonoids.

摘要

The objective of this study is to develop a "nanovehicle" to transport resveratrol in the plasma and to targeted intracellular sites. Resveratrol is a bioflavonoid possessing a variety of biological activities. We incorporated resveratrol into reconstituted high-density lipoproteins (rHDL), which are water-soluble lipid/protein complexes. rHDL was prepared using apolipoprotein E3 (apoE3) N-terminal domain and phospholipids. The role of apoE3 NT domain is to mediate cellular uptake of lipoproteins via the low-density lipoprotein receptor (LDLr). Biochemical, biophysical and functional studies using glioblastoma cells indicate that (i) resveratrol has partitioned into the hydrophobic milieu of rHDL, and is shielded from the aqueous environment, and, (ii) the presence of resveratrol does not alter the overall structural integrity of rHDL and the ability of LDLr to mediate cellular uptake of rHDL. Our results suggest that rHDL containing apoE3 can serve as an effective "nanovehicle" to transport and potentially deliver resveratrol to targeted intracellular sites.