Co-delivery of Curcumin and Bioperine via PLGA Nanoparticles to Prevent
Atherosclerotic Foam Cell Formation
Abstract
Cholesterol-rich arterial plaques characterize atherosclerosis, a
significant cause of heart disease. Arterial plaques upregulate
inflammatory cytokines secreted by the macrophages that finally become
cholesterol-laden foam cells. Nutraceuticals have received attention
over the years, demonstrating potential benefits towards treating and
preventing cardiovascular diseases (CVD), including atherosclerosis.
Curcumin, a potent polyphenol present in Curcuma longa, showed
remarkable anti-atherosclerotic activity via anti-inflammatory and
anti-oxidative properties. The bioavailability and low water solubility
of curcumin limit its clinical translational purposes. These issues can
be circumvented effectively by nano-drug delivery systems that can
target atherosclerotic plaque sites. In this work, we chose to use
curcumin and a natural bioenhancer called Bioperine (derived from Piper
nigrum) inside a polymeric nano-drug delivery system for targeting
atherosclerotic plaque sites. We selected two different ratios of
curcumin: Bioperine to study its comparative effect on the inhibition of
oxidized low-density lipoprotein (Ox-LDL) induced foam cell formation
and investigated the therapeutic efficacy in THP-1 monocyte-derived
macrophages via different in vitro cell studies. Our studies
demonstrated that Bioperine administration alongside curcumin via PLGA
nanoparticles (NPs) imparts a reduction in macrophage-mediated foam cell
formation, relative cholesterol content, and the inflammatory pathways
when administered as preventive medicine, highlighting the importance of
natural-based compounds towards the therapeutic intervention against the
atherosclerotic activity.