[关键词]
[摘要]
目的 制备白藜芦醇纳米乳并探讨其在大鼠体内的药动学行为。方法 以油酸乙酯作为油相,聚氧乙烯氢化蓖麻油RH40为乳化剂,无水乙醇为助乳化剂,采用滴定法绘制伪三元相图以优化纳米乳处方,对所制备的白藜芦醇纳米乳进行粒径、透射电镜及红外光谱测定等理化性质的表征。大鼠ig给药后,采用HPLC测定其血药浓度,计算其药动学参数,利用DAS软件分析其药动学特征。结果 白藜芦醇纳米乳处方为药物-油相-混合乳化剂-水的质量比为1∶10∶24∶65,所制备纳米乳的粒径为40 nm左右,电镜观察其形态为圆形球状结构,红外光谱结果表明白藜芦醇以活性的反式结构存在于纳米乳的油相中。与白藜芦醇混悬剂相比,白藜芦醇纳米乳在大鼠体内的血药浓度时间曲线下面积(78.89 h·μg/mL)为混悬剂(54.42 h·μg/mL)的1.45倍,达峰浓度(3.29 μg/mL)是混悬剂(1.70 μg/mL)的1.93倍,可以提高白藜芦醇口服给药的生物利用度。结论 所制备的纳米乳制剂有希望为白藜芦醇的有效递送提供新的给药途径。
[Key word]
[Abstract]
Objective To fabricate resveratrol nanoemulsions and probe their pharmacokinetics profiles in rats in vivo. Methods The nanoemulsions of resveratrol were tailored by using aethylis oleas as the oil phase, Cremophor RH40 as emulsifiers, absolute alcohol as co-emulsifiers, respectively. The formulation was optimized by pseudo-ternary phase diagrams and their physicochemical properties of nanoemulsions were characterized by particle size distribution, transmission electron microscope (TEM), and Fourier transform infrared spectroscopy (FTIR). The pharmacokinetics experiments were also performed in rats after gavage and the plasm concentration of resveratrol were determined by HPLC as well as the profiles of pharmacokinetic parameters were obtained by Drug and Statistics (DAS) software. Results The formula of nanoemulsions were as follows:the ratio of resveratrol-aethylis oleas-mixture surfactant- distilled water was 1:10:24:65. The average particle size diameters of prepared resveratrol nanoemulsions were about 40 nm and the droplets of nanoemulsions were in spherical shape observed by TEM. The results of IR disclosed that the active trans-resveratrol presented in the oil droplet of the nanoemulsions. Compared with resveratrol suspensions, the bioavailability of resveratrol nanoemulsions was increased 1.45-fold, and Cmax reached to 1.93-fold. Conclusion These results indicated that nanoemulsions may be a promising tool for the delivery of resveratrol.
[中图分类号]
R283.6
[基金项目]
山东省中医药科技发展计划项目(2017-240);山东省抗体制药协同创新中心开放课题(CIC-AD1813);广东食品药品职业学院校级课题资助项目(2017ZR022)