不同配伍比例的葛根素-甘草酸自组装纳米粒在Caco-2细胞单层模型的转运研究OA

[Objective]To enhance the solubility and intestinal absorption of puerarin(Pue),the study investigated the absorption and transport characteristics of self-assembled puerarin-glycyrrhizic acid nanoparticles(Pue-GA NPs)prepared at different molar ratios using a Caco-2 cell monolayer model.The research was inspired by the component interactions occurring during the decoction of the traditional Chinese herbal pair Radix Puerariae-Radix Glycyrrhizae.[Methods]Pue-GA NPs were prepared via a solvent evaporation method,and their particle size and morphology were characterized.The interactions between Pue and glycyrrhizic acid(GA)were evaluated through UV-visible spectroscopy and molecular docking.Transwell assays were employed to compare the transmembrane transport of physical mixtures versus self-assembled nanoparticles at different molar ratios.Additionally,four endocytic inhibitors were applied to elucidate the underlying absorption mechanisms.[Results]Pue-GA NPs with different molar ratios formed stable spherical nanoparticles,and hydrogen bonding was involved in their self-assembly.Caco-2 transport studies revealed that Pue-GA NPs at a 1∶1 molar ratio exhibited the highest transmembrane transport efficiency,which was significantly greater than that of the physical mixture.All four endocytic inhibitors reduced nanoparticle transport,with chlorpromazine showing the most pronounced inhibitory effect.[Conclusion]Glycyrrhizic acid and puerarin can efficiently self-assemble into stable nanoparticles.The Pue-GA NPs notably improved the transport efficiency of Pue across the Caco-2 cell monolayer,with the 1∶1 molar ratio formulation exhibiting the best performance.The enhanced absorption was primarily mediated via a clathrin-dependent endocytic pathway.