Uptake and transport of furanodiene in Caco-2 cell monolayers: a comparison study between furanodiene and furanodiene loaded PLGA nanoparticles

AimFuranodiene (FDE) possesses diverse pharmacological activities with high lipophilicity and poor stability. This study prepared FDE loaded PLGA nanoparticles (FDE-PLGA-NPs) and PEGylated PLGA nanoparticles (FDE-PEG-PLGA-NPs) by the spontaneous emulsion solvent diffusion method to improve the stability and bioavailability of FDE.MethodsFDE-PLGA-NPs and FDE-PEG-PLGA-NPs were characterized for size and size distribution, surface morphology, zeta-potential and entrapment efficiency. The stability of FDE, FDE-PLGA-NPs and FDE-PEG-PLGA-NPs in physiological fluids (PBS and artificial gastrointestinal fluids) was evaluated. In vitro cellular uptake and transport studies were performed using Caco-2 cell monolayers.ResultsThe size of FDE-PLGA-NPs and FDE-PEG-PLGA-NPs ranged from 110-140 nm, the entrapment efficiencies were 87.3% and 89.2%, respectively, and the stabilities were enhanced significantly compared with FDE. FDE-PLGA-NPs and FDE-PEG-PLGA-NPs could be taken up by Caco-2 cells freely and transported across the monolayers. While FDE hardly reached to the receptor side, it could be taken up into Caco-2 cell monolayers.ConclusionsThese results indicated that FDE-PLGA-NPs, especially FDE-PEG-PLGA-NPs, could enhance the stability and hydrophilicity of FDE and increase the permeation of FDE across Caco-2 cell monolayers.