In-vitro/in-vivo characterization of trans-resveratrol-loaded nanoparticulate drug delivery system for oral administration

Abstract

Objectives The current studies entail successful formulation of systematically optimized (OPT) nanoparticulate drug delivery system to increase the oral bioavailability using Eudragit RL 100 of trans-resveratrol (t-RVT), and evaluate their in-vitro/in-vivo performance. Methods t-RVT-loaded Eudragit RL 100 nanoparticles (t-RVT NPs) were prepared by nanoprecipitation method. The nanoparticles (NPs) were systematically optimized using 32 central composite design and the OPT formulation located using overlay plot. The pharmacokinetic and in-vivo biodistribution of t-RVT NPs were investigated in rats, and various levels of in-vitro/in-vivo correlation (IVIVC) were established. Key findings The OPT formulation (mean particle size: 180nm) indicated marked improvement in drug release profile vis-à-vis pure drug and marketed formulation (MKT). Augmentation in the values of Ka (5.64-fold) and AUC0-24 (7.25-fold) indicated significant enhancement in the rate and extent of bioavailability by the optimized trans-resveratrol- loaded Eudragit RL 100 nanoparticles (OPT-t-RVT NPs) compared with pure drug. Level A of IVIVC was successfully established. OPT-t-RVT NPs showed 4.11-fold rose in the values of t-RVT concentrations in liver. In-situ single pass intestinal perfusion studies construed remarkable enhancement in the absorptivity and permeability parameters of OPT-t-RVT NPs. Conclusions The results, therefore, insight into the role of solubility enhancement and trounce enterohepatic recirculation for improving the oral bioavailability of t-RVT. © 2014 Royal Pharmaceutical Society.