A Transdermal Delivery System to Enhance Quercetin Nanoparticle Permeability

Abstract

Targeting oxidative stress with inhibiting or boosting the endogenous levels of antioxidants potentially has an outstanding effect in the treatment of oxidative-stress-related diseases. The present work demonstrates the synthesis of quercetin nanoemulsion as one of the potential antioxidants for the treatment of oxidative- stress-related diseases. A quercetin nanoemulsion was prepared using poly(lactic-co-glycolic acid) (PLGA), hyaluronic acid (HA) and emulsifier (Tween-20) through a solvent evaporation technique. The efficiency of the nanoemulsion was evaluated with and without chemical permeation enhancer (CPE). The FT-IR result shows no interaction between quercetin and polymer that proves excellent compatibility. The transdermal delivery ability was evaluated using in vitro release and ex vivo permeation analysis. The transdermal drug-release mechanism was studied by the mathematical model and was found to obey a zero-order, diffusion-controlled mechanism. In vitro toxicity and cell behavior, including cell adhesion, proliferation and cell death of quercetin-nanoemulsion-treated L929 cells, were elucidated by the electrical cell-substrate impedance sensing (ECIS) technique. The produced nanoemulsion showed a high encapsulation efficiency, less toxicity, controlled delivery with enhanced transdermal drug permeation and effective scavenging of free radicals. (C) Koninklijke Brill NV, Leiden, 2012