Adipose Vasculature Targeted Nanotherapy Leads to a Novel Strategy of Obesity Treatment

Abstract

Worldwide obesity has been nearly doubled since 1980. However, anti-obesity medications that have been developed so far have limited efficacies and considerable side effects. To solve this problem, we focused on the vascular endothelial cells in adipose tissue as a new therapeutic target, since the blood vessels play a crucial role for adipose tissue development and hypertrophy. Thus, we attempted to develop a novel platform for drug delivery based on the active targeting, and succeeded in in vivo obesity treatment via the Prohibitin-Targeted Nano Particle (PTNP) modified with the high affinity peptide (KGGRAKD) to prohibitin expressed on the surface of vascular endothelial cells in adi pose tissue. In addition, we found that the accumulation of long circulating nanoparticles into adipose tissue was passively enhanced by the enhanced permeability and retention (EPR) effect, when they were administered to obese animals. On the basis of these results, we firstly proposed the strategy of adipose vasculature targeted nanotherapy for obesity treatment.