甘草酸为稳定剂的葛根素纳米乳冻干粉的制备及体外评价

Preparation and in vitro evaluation of puerarin nanoemulsion lyophilized powder with glycyrrhizic acid as stabilizer

目的以天然表面活性剂甘草酸为稳定剂制备葛根素纳米乳冻干粉(puerarinnanoemulsionlyophilizedpowder,Pue-NE-LP),并对其进行体外评价。方法采用高速剪切联合高压均质法制备葛根素纳米乳(Pue-NE),进一步结合冷冻干燥法制备Pue-NE-LP。以平均粒径和多分散指数(PDI)作为评价指标,通过单因素试验筛选出最优处方及工艺参数。并对制备的Pue-NE-LP进行理化性质表征和体外溶出度测定。结果以5%辛癸酸甘油酯为油相,2.0 mg/mL甘草酸为稳定剂,7%葡萄糖为冻干保护剂制得的Pue-NE-LP平均粒径为(215.1±0.7)nm,PDI为0.133±0.024。扫描电镜显示Pue-NE-LP呈不规则的小片状,大小较均匀;X射线衍射显示Pue-NE-LP呈无定型状态存在。体外释放结果表明Pue-NE-LP的溶出度明显高于物理混合物。结论以天然表面活性剂甘草酸为稳定剂制备的Pue-NE-LP,不仅制备方法简单,而且能显著改善Pue的溶解性和生物利用度,为Pue-NE制剂的多元开发提供参考。

Objective Puerarin nanoemulsion lyophilized powder(Pue-NE-LP) was prepared using natural surfactant glycyrrhizic acid as stabilizer and evaluated in vitro. Methods Pue-NE was prepared by high-speed shear and high-pressure homogenization method, and further combined with freeze-drying method to prepare Pue-NE-LP. Taking the average particle size and polydispersity index(PDI) as the evaluation indexes, the optimal prescription and process parameters of this experiment were screened out through a single factor test. The prepared Pue-NE-LP was characterized by physicochemical properties and dissolution in vitro. Results The average particle size and PDI of Pue-NE-LP prepared with 5% glyceryl caprylate as oil phase, 2.0 mg/mL glycyrrhizic acid as stabilizer, and 7% glucose as lyophilization protectant was(215.1 ± 0.7) nm and(0.133 ± 0.024), respectively. Scanning electron microscopy showed that Pue-NE-LP was irregularly small and uniform in size;X-ray diffraction showed that Pue-NE-LP existed in an amorphous state. In vitro release results showed that the dissolution rate of Pue-NE-LP was significantly higher than the physical mixture. Conclusion Pue-NE-LP prepared with natural surfactant glycyrrhizic acid as a stabilizer is not only simple to prepare, but also can significantly improve the solubility and bioavailability of puerarin. It provides a reference for the multiple development of Pue-NE formulations.