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

AIM:Furanodiene(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.METHODS:FDE-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.RESULTS:The 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.CONCLUSIONS:These 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.