口服葛根总黄酮固体脂质纳米粒冻干粉的制备及其4种成分释放度考察

目的制备口服葛根总黄酮固体脂质纳米粒冻干粉并考察其主要有效成分3′-羟基葛根素、葛根素、大豆苷和大豆苷元的释放度。方法采用高压均质法制备葛根总黄酮固体脂质纳米粒混悬液,以甘露醇为冻干保护剂制备冻干粉,以人工胃液(pH 1.2)为溶出介质,考察葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放度。结果正交试验优选制备工艺:脂质-表面活性剂比例及用量为2∶1及2.0%、葛根总黄酮用量2.5%、150 MPa均质15次,并制备葛根总黄酮固体脂质纳米粒冻干粉,其粒径、多分散指数及Zeta电位分别为(517.1±10.3)nm、0.484±0.210及(-21.91±2.03)mV。葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放速率显著低于其物理混合物,具有明显的缓释特征。结论葛根总黄酮固体脂质纳米粒冻干粉制备方法简便,能显著延缓主要有效成分的释放速率,有望成为葛根总黄酮的新型纳米给药系统。

Preparation of lyophilized powder in oral Pueraria flavonoids loaded solid lipid nanoparticles and determination of release rate of its four effective components

Objective To prepare the lyophilized powder of Pueraria flavonoids loaded solid lipid nanoparticles (PF-SLN) and determine the dissolution rate of its four effective components: 3'-hydroxypuerarin, puerarin, daidzin, and daidzein. Methods PF-SLN was prepared by the high pressure homogenization (HPH) technology. The lyophilized formula contained mannitol as cryoprotectant. The release rates of the four effective components from the PF-SLN lyophilized powder as well as the physical mixture were determined, with artificial gastric juice (pH 1.2) as dissolvent. Results The technical parameters of PF-SLN preparation optimized by orthogonal test were as follows: The ratio and the dosage of lipid-surfactant were 2:1 and 2.0%, PF dosage was 2.5%, and 150 MPa homogeneity was 15 cycles. The optimal PF-SLN lyophilized powder was loosen with the particle size of (517.1 ± 10.3) nm, polydisperse index of 0.484 ± 0.210, and Zeta potential of (-21.91 ± 2.03) mV, respectively. The in vitro accumulated dissolution rates of PF-SLN lyophilized powder were slower than those of the physical mixture. Conclusion The method employed to prepare PF-SLN lyophilized powder is feasible. PF-SLN lyophilized powder could delay the in vitro dissolution rate notablely. It might be a novel vehicle potentially for nano-drug delivery system of Pueraria flavonoids.