纳米乳液提高氧化白藜芦醇口服生物利用率及透皮吸收效率

Nanoemulsion Improves Oral Bioavailability and Transdermal Absorption Efficiency of Oxyresveratrol

本研究制备纳米乳液改善氧化白藜芦醇在水溶液中的溶解性能,通过体外药物溶出实验、脂解实验、Caco-2跨膜细胞转运实验、透皮吸收实验评价了纳米乳液对氧化白藜芦醇生物利用率的改善效果。结果表明:氧化白藜芦醇纳米乳液和氧化白藜芦醇化合物自身的生物利用率在进食状态下分别为61.22%和23.47%,禁食状态下为56.12%和22.45%。纳米乳液使氧化白藜芦醇在小肠上皮细胞的扩散速度由中速上升至快速,扩散形式为被动渗透,表观渗透系数Papp(AP-BL)值1.69×10^-5 cm/sec,Papp(BL-AP)值8.94×10^-6cm/sec,ER=Rpapp(AP-BL)/(BL-AP)=1.89。6 h时氧化白藜芦醇纳米乳液和化合物的经皮扩散透过量分别为51.76和5.73μg/cm^2 skin。结论:氧化白藜芦醇纳米乳液比化合物本身的生物利用率提升了3倍,显著提升氧化白藜芦醇在小肠上皮细胞内的吸收转运量(提升2~4倍)和透皮吸收效率(p<0.05),本实验为氧化白藜芦醇的应用奠定研究基础,为其有效地发挥生物活性提供理论依据。

In this study,a nanoemulsion was prepared to improve the solubility of oxyresveratrol(OXY)in aqueous solutions.The effect of nanoemulsion on the bioavailability of OXY was evaluated through in vitro dissolution test,lipolysis test transmembrane transport test in Caco-2 monolayer model,and transdermal absorption test.The results showed that the bioavailability of OXY-loaded nanoemulsion and OXY itself was61.22%and 23.47%,respectively,in the fed state,and 56.12%and 22.45%,respectively,during the fasting state.The nanoemulsion increased the diffusion rate of OXY in the epithelial cells of the small intestine from medium to rapid,and the diffusion type was passive diffusion with an apparent permeability coefficient Papp(AP-BL)as 1.69×10^-5 cm/sec,Papp(BL-AP)value as 8.94×10^-6 cm/sec,and ER=Rpapp(AP-BL)/(BL-AP)as 1.89.The transdermal absorption of OXY-loaded nanoemulsion and OXY at the 6 h was 51.76 and 5.73 g/cm2skin,respectively.Conclusions:The bioavailability of the OXY-loaded nanoemulsion was 3 times higher than that of the compound itself.Nanoemulsion significantly improved the absorption(by 2~4 times)and transmembrane transport efficiency of OXY(p<0.05)in the small intestinal epithelia cells.This study laid a research foundation for the application of OXY and provided a theoretical basis for enabling its efficacy.