Resveratrol-loaded folate targeted lipoprotein-mimetic nanoparticles with improved cytotoxicity, antioxidant activity and pharmacokinetic profile.

The aim of present study was to develop folate receptor targeted lipoprotein-mimetic nanoparticles of resveratrol (RSV). Lipoprotein-mimicking nanocarrier (RSV-FA-LNPs) comprising of phosphatidyl choline, cholesterol, stearyl amine and folic acid-tagged bovine serum albumin (FA-BSA) were prepared. Folic acid was conjugated to bovine serum albumin by amide bond at a binding rate of 9.46 ± 0.49 folate molecules per bovine serum albumin. The particle size and entrapment efficiency of the developed nanoparticles was found to be 291.37 ± 3.81 nm and 91.96 ± 1.83%, respectively. The in vitro release study depicted that developed nanocarrier prolonged the drug release till 72 h in phosphate buffer saline (pH 7.4). The anticancer potential of RSV in case of RSV-FA-LNPs was found to be substantially improved against MCF-7 cells overexpressing folate receptors compared to non-targeted nanoparticles. The pharmacokinetics studies after intravenous administration in healthy Wistar rats depicted that lipoprotein mimicking nanoparticles presented the longer circulation time (>48 h) compared to free drug which disappeared in few hours (6 h). The in vitro and preclinical findings of the present study demonstrated the applicability of lipoprotein mimicking nanocarriers for the safer and effective delivery of bioactives.